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Prof. Rafik Karaman
Al-Quds University

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0 Ab Initio
0 Activated Carbon
0 Wastewater
0 Wastewater Treatment
0 DFT calculations

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prodrugs
proton transfer
Wastewater
Wastewater Treatment
DFT calculations
Ab Initio
Activated Carbon
micelle–clay complex
Proton Transfer Reaction
enzyme catalysis

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Short Biography

Professor Rafik Karaman is currently a distinguished professor of pharmaceutical sciences. He received his PhD, MS, and bachelor's degree in Pharmacy from the Hebrew University. Professor Karaman has more than 200 peer-reviewed manuscripts and books; 150 of them were published in the last 8 years. He is currently an editor and an editorial board member of 50 international journals in the area of pharmaceutical sciences. His research includes: (1) design and synthesis of anticancer prodrugs having targeted properties determined on the linker’s type, (2) design and synthesis of prodrugs having inefficient bioavailability (dopamine), (3) design and synthesis of prodrugs for masking bitter sensation of commonly used drugs, and (4) removal of pharmaceuticals from wastewater by novel adsorbents.

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Review
Published: 28 May 2021 in Molecules
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Enzymes are highly specific biological catalysts that accelerate the rate of chemical reactions within the cell. Our knowledge of how enzymes work remains incomplete. Computational methodologies such as molecular mechanics (MM) and quantum mechanical (QM) methods play an important role in elucidating the detailed mechanisms of enzymatic reactions where experimental research measurements are not possible. Theories invoked by a variety of scientists indicate that enzymes work as structural scaffolds that serve to bring together and orient the reactants so that the reaction can proceed with minimum energy. Enzyme models can be utilized for mimicking enzyme catalysis and the development of novel prodrugs. Prodrugs are used to enhance the pharmacokinetics of drugs; classical prodrug approaches focus on alternating the physicochemical properties, while chemical modern approaches are based on the knowledge gained from the chemistry of enzyme models and correlations between experimental and calculated rate values of intramolecular processes (enzyme models). A large number of prodrugs have been designed and developed to improve the effectiveness and pharmacokinetics of commonly used drugs, such as anti-Parkinson (dopamine), antiviral (acyclovir), antimalarial (atovaquone), anticancer (azanucleosides), antifibrinolytic (tranexamic acid), antihyperlipidemia (statins), vasoconstrictors (phenylephrine), antihypertension (atenolol), antibacterial agents (amoxicillin, cephalexin, and cefuroxime axetil), paracetamol, and guaifenesin. This article describes the works done on enzyme models and the computational methods used to understand enzyme catalysis and to help in the development of efficient prodrugs.

ACS Style

Zeinab Breijyeh; Rafik Karaman. Enzyme Models—From Catalysis to Prodrugs. Molecules 2021, 26, 3248 .

AMA Style

Zeinab Breijyeh, Rafik Karaman. Enzyme Models—From Catalysis to Prodrugs. Molecules. 2021; 26 (11):3248.

Chicago/Turabian Style

Zeinab Breijyeh; Rafik Karaman. 2021. "Enzyme Models—From Catalysis to Prodrugs." Molecules 26, no. 11: 3248.

Review
Published: 05 February 2021 in Toxins
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For thousands of years, Cannabis sativa has been utilized as a medicine and for recreational and spiritual purposes. Phytocannabinoids are a family of compounds that are found in the cannabis plant, which is known for its psychotogenic and euphoric effects; the main psychotropic constituent of cannabis is Δ9-tetrahydrocannabinol (Δ9-THC). The pharmacological effects of cannabinoids are a result of interactions between those compounds and cannabinoid receptors, CB1 and CB2, located in many parts of the human body. Cannabis is used as a therapeutic agent for treating pain and emesis. Some cannabinoids are clinically applied for treating chronic pain, particularly cancer and multiple sclerosis-associated pain, for appetite stimulation and anti-emesis in HIV/AIDS and cancer patients, and for spasticity treatment in multiple sclerosis and epilepsy patients. Medical cannabis varies from recreational cannabis in the chemical content of THC and cannabidiol (CBD), modes of administration, and safety. Despite the therapeutic effects of cannabis, exposure to high concentrations of THC, the main compound that is responsible for most of the intoxicating effects experienced by users, could lead to psychological events and adverse effects that affect almost all body systems, such as neurological (dizziness, drowsiness, seizures, coma, and others), ophthalmological (mydriasis and conjunctival hyperemia), cardiovascular (tachycardia and arterial hypertension), and gastrointestinal (nausea, vomiting, and thirst), mainly associated with recreational use. Cannabis toxicity in children is more concerning and can cause serious adverse effects such as acute neurological symptoms (stupor), lethargy, seizures, and even coma. More countries are legalizing the commercial production and sale of cannabis for medicinal use, and some for recreational use as well. Liberalization of cannabis laws has led to increased incidence of toxicity, hyperemesis syndrome, lung disease cardiovascular disease, reduced fertility, tolerance, and dependence with chronic prolonged use. This review focuses on the potential therapeutic effects of cannabis and cannabinoids, as well as the acute and chronic toxic effects of cannabis use on various body systems.

ACS Style

Zeinab Breijyeh; Buthaina Jubeh; Sabino Bufo; Rafik Karaman; Laura Scrano. Cannabis: A Toxin-Producing Plant with Potential Therapeutic Uses. Toxins 2021, 13, 117 .

AMA Style

Zeinab Breijyeh, Buthaina Jubeh, Sabino Bufo, Rafik Karaman, Laura Scrano. Cannabis: A Toxin-Producing Plant with Potential Therapeutic Uses. Toxins. 2021; 13 (2):117.

Chicago/Turabian Style

Zeinab Breijyeh; Buthaina Jubeh; Sabino Bufo; Rafik Karaman; Laura Scrano. 2021. "Cannabis: A Toxin-Producing Plant with Potential Therapeutic Uses." Toxins 13, no. 2: 117.

Review
Published: 08 December 2020 in Molecules
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Alzheimer’s disease (AD) is a disorder that causes degeneration of the cells in the brain and it is the main cause of dementia, which is characterized by a decline in thinking and independence in personal daily activities. AD is considered a multifactorial disease: two main hypotheses were proposed as a cause for AD, cholinergic and amyloid hypotheses. Additionally, several risk factors such as increasing age, genetic factors, head injuries, vascular diseases, infections, and environmental factors play a role in the disease. Currently, there are only two classes of approved drugs to treat AD, including inhibitors to cholinesterase enzyme and antagonists to N-methyl d-aspartate (NMDA), which are effective only in treating the symptoms of AD, but do not cure or prevent the disease. Nowadays, the research is focusing on understanding AD pathology by targeting several mechanisms, such as abnormal tau protein metabolism, β-amyloid, inflammatory response, and cholinergic and free radical damage, aiming to develop successful treatments that are capable of stopping or modifying the course of AD. This review discusses currently available drugs and future theories for the development of new therapies for AD, such as disease-modifying therapeutics (DMT), chaperones, and natural compounds.

ACS Style

Zeinab Breijyeh; Rafik Karaman. Comprehensive Review on Alzheimer’s Disease: Causes and Treatment. Molecules 2020, 25, 5789 .

AMA Style

Zeinab Breijyeh, Rafik Karaman. Comprehensive Review on Alzheimer’s Disease: Causes and Treatment. Molecules. 2020; 25 (24):5789.

Chicago/Turabian Style

Zeinab Breijyeh; Rafik Karaman. 2020. "Comprehensive Review on Alzheimer’s Disease: Causes and Treatment." Molecules 25, no. 24: 5789.

Editorial
Published: 28 June 2020 in Molecules
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Breakthroughs in Medicinal Chemistry

ACS Style

Michael Gütschow; Jean Jacques Vanden Eynde; Josef Jampilek; Congbao Kang; Arduino A. Mangoni; Paola Fossa; Rafik Karaman; Andrea Trabocchi; Peter J. H. Scott; Jóhannes Reynisson; Simona Rapposelli; Stefania Galdiero; Jean-Yves Winum; Chiara Brullo; Katalin Prokai-Tatrai; Arun K. Sharma; Matthieu Schapira; Yasu-Taka Azuma; Laura Cerchia; Mariana Spetea; Giangiacomo Torri; Simona Collina; Athina Geronikaki; Alfonso T. García-Sosa; M. Helena Vasconcelos; Maria Emília Sousa; Ivan Kosalec; Tiziano Tuccinardi; Iola F. Duarte; Jorge A. R. Salvador; Massimo Bertinaria; Maurizio Pellecchia; Jussara Amato; Giulio Rastelli; Paula A. C. Gomes; Rita C. Guedes; Jean-Marc Sabatier; Ana Estévez-Braun; Bruno Pagano; Stefano Mangani; Rino Ragno; George Kokotos; Margherita Brindisi; Florenci V. González; Fernanda Borges; Mariarosaria Miloso; Jarkko Rautio; Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–7. Molecules 2020, 25, 2968 .

AMA Style

Michael Gütschow, Jean Jacques Vanden Eynde, Josef Jampilek, Congbao Kang, Arduino A. Mangoni, Paola Fossa, Rafik Karaman, Andrea Trabocchi, Peter J. H. Scott, Jóhannes Reynisson, Simona Rapposelli, Stefania Galdiero, Jean-Yves Winum, Chiara Brullo, Katalin Prokai-Tatrai, Arun K. Sharma, Matthieu Schapira, Yasu-Taka Azuma, Laura Cerchia, Mariana Spetea, Giangiacomo Torri, Simona Collina, Athina Geronikaki, Alfonso T. García-Sosa, M. Helena Vasconcelos, Maria Emília Sousa, Ivan Kosalec, Tiziano Tuccinardi, Iola F. Duarte, Jorge A. R. Salvador, Massimo Bertinaria, Maurizio Pellecchia, Jussara Amato, Giulio Rastelli, Paula A. C. Gomes, Rita C. Guedes, Jean-Marc Sabatier, Ana Estévez-Braun, Bruno Pagano, Stefano Mangani, Rino Ragno, George Kokotos, Margherita Brindisi, Florenci V. González, Fernanda Borges, Mariarosaria Miloso, Jarkko Rautio, Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–7. Molecules. 2020; 25 (13):2968.

Chicago/Turabian Style

Michael Gütschow; Jean Jacques Vanden Eynde; Josef Jampilek; Congbao Kang; Arduino A. Mangoni; Paola Fossa; Rafik Karaman; Andrea Trabocchi; Peter J. H. Scott; Jóhannes Reynisson; Simona Rapposelli; Stefania Galdiero; Jean-Yves Winum; Chiara Brullo; Katalin Prokai-Tatrai; Arun K. Sharma; Matthieu Schapira; Yasu-Taka Azuma; Laura Cerchia; Mariana Spetea; Giangiacomo Torri; Simona Collina; Athina Geronikaki; Alfonso T. García-Sosa; M. Helena Vasconcelos; Maria Emília Sousa; Ivan Kosalec; Tiziano Tuccinardi; Iola F. Duarte; Jorge A. R. Salvador; Massimo Bertinaria; Maurizio Pellecchia; Jussara Amato; Giulio Rastelli; Paula A. C. Gomes; Rita C. Guedes; Jean-Marc Sabatier; Ana Estévez-Braun; Bruno Pagano; Stefano Mangani; Rino Ragno; George Kokotos; Margherita Brindisi; Florenci V. González; Fernanda Borges; Mariarosaria Miloso; Jarkko Rautio; Diego Muñoz-Torrero. 2020. "Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–7." Molecules 25, no. 13: 2968.

Review
Published: 23 June 2020 in Molecules
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The discovery of antibiotics has created a turning point in medical interventions to pathogenic infections, but unfortunately, each discovery was consistently followed by the emergence of resistance. The rise of multidrug-resistant bacteria has generated a great challenge to treat infections caused by bacteria with the available antibiotics. Today, research is active in finding new treatments for multidrug-resistant pathogens. In a step to guide the efforts, the WHO has published a list of the most dangerous bacteria that are resistant to current treatments and requires the development of new antibiotics for combating the resistance. Among the list are various Gram-positive bacteria that are responsible for serious healthcare and community-associated infections. Methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and drug-resistant Streptococcus pneumoniae are of particular concern. The resistance of bacteria is an evolving phenomenon that arises from genetic mutations and/or acquired genomes. Thus, antimicrobial resistance demands continuous efforts to create strategies to combat this problem and optimize the use of antibiotics. This article aims to provide a review of the most critical resistant Gram-positive bacterial pathogens, their mechanisms of resistance, and the new treatments and approaches reported to circumvent this problem.

ACS Style

Buthaina Jubeh; Zeinab Breijyeh; Rafik Karaman. Resistance of Gram-Positive Bacteria to Current Antibacterial Agents and Overcoming Approaches. Molecules 2020, 25, 2888 .

AMA Style

Buthaina Jubeh, Zeinab Breijyeh, Rafik Karaman. Resistance of Gram-Positive Bacteria to Current Antibacterial Agents and Overcoming Approaches. Molecules. 2020; 25 (12):2888.

Chicago/Turabian Style

Buthaina Jubeh; Zeinab Breijyeh; Rafik Karaman. 2020. "Resistance of Gram-Positive Bacteria to Current Antibacterial Agents and Overcoming Approaches." Molecules 25, no. 12: 2888.

Journal article
Published: 18 May 2020 in Catalysts
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Commercial non-steroidal anti-inflammatory drugs (NSAIDs) are considered as toxic to the environment since they induce side effects when consumed by humans or aquatic life. Ibuprofen is a member of the NSAID family and is widely used as an anti-inflammatory and painkiller agent. Photolysis is a potentially important method of degradation for several emerging contaminants, and individual compounds can undergo photolysis to various degrees, depending on their chemical structure. The efficiency oftitanium dioxide (TiO2) and photocatalysis was investigated for the removal of ibuprofen from the aquatic environment, and the performance of these different processes was evaluated. In heterogeneous photocatalysis, two experiments were carried out using TiO2 as (i) dispersed powder, and (ii) TiO2 immobilized on the active surface of commercial coated glass. The kinetics of each photoreaction was determined, and the identification of the photoproducts was carried out by liquid chromatography coupled with Fourier-transform ion cyclotron resonance mass spectrometry (LC-FTICR MS). The overall results suggest that the TiO2 active thin layer immobilized on the glass substrate can avoid recovery problems related to the use of TiO2 powder in heterogeneous photocatalysis and may be a promising tool toward protecting the environment from emerging contaminants such as ibuprofen and its derivatives.

ACS Style

Samer Khalaf; Jawad H. Shoqeir; Filomena Lelario; Sabino A. Bufo; Rafik Karaman; Laura Scrano. TiO2 and Active Coated Glass Photodegradation of Ibuprofen. Catalysts 2020, 10, 560 .

AMA Style

Samer Khalaf, Jawad H. Shoqeir, Filomena Lelario, Sabino A. Bufo, Rafik Karaman, Laura Scrano. TiO2 and Active Coated Glass Photodegradation of Ibuprofen. Catalysts. 2020; 10 (5):560.

Chicago/Turabian Style

Samer Khalaf; Jawad H. Shoqeir; Filomena Lelario; Sabino A. Bufo; Rafik Karaman; Laura Scrano. 2020. "TiO2 and Active Coated Glass Photodegradation of Ibuprofen." Catalysts 10, no. 5: 560.

Review
Published: 28 March 2020 in Molecules
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Bacterial resistance to present antibiotics is emerging at a high pace that makes the development of new treatments a must. At the same time, the development of novel antibiotics for resistant bacteria is a slow-paced process. Amid the massive need for new drug treatments to combat resistance, time and effort preserving approaches, like the prodrug approach, are most needed. Prodrugs are pharmacologically inactive entities of active drugs that undergo biotransformation before eliciting their pharmacological effects. A prodrug strategy can be used to revive drugs discarded due to a lack of appropriate pharmacokinetic and drug-like properties, or high host toxicity. A special advantage of the use of the prodrug approach in the era of bacterial resistance is targeting resistant bacteria by developing prodrugs that require bacterium-specific enzymes to release the active drug. In this article, we review the up-to-date implementation of prodrugs to develop medications that are active against drug-resistant bacteria.

ACS Style

Buthaina Jubeh; Zeinab Breijyeh; Rafik Karaman. Antibacterial Prodrugs to Overcome Bacterial Resistance. Molecules 2020, 25, 1543 .

AMA Style

Buthaina Jubeh, Zeinab Breijyeh, Rafik Karaman. Antibacterial Prodrugs to Overcome Bacterial Resistance. Molecules. 2020; 25 (7):1543.

Chicago/Turabian Style

Buthaina Jubeh; Zeinab Breijyeh; Rafik Karaman. 2020. "Antibacterial Prodrugs to Overcome Bacterial Resistance." Molecules 25, no. 7: 1543.

Review
Published: 16 March 2020 in Molecules
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Antimicrobial resistance represents an enormous global health crisis and one of the most serious threats humans face today. Some bacterial strains have acquired resistance to nearly all antibiotics. Therefore, new antibacterial agents are crucially needed to overcome resistant bacteria. In 2017, the World Health Organization (WHO) has published a list of antibiotic-resistant priority pathogens, pathogens which present a great threat to humans and to which new antibiotics are urgently needed the list is categorized according to the urgency of need for new antibiotics as critical, high, and medium priority, in order to guide and promote research and development of new antibiotics. The majority of the WHO list is Gram-negative bacterial pathogens. Due to their distinctive structure, Gram-negative bacteria are more resistant than Gram-positive bacteria, and cause significant morbidity and mortality worldwide. Several strategies have been reported to fight and control resistant Gram-negative bacteria, like the development of antimicrobial auxiliary agents, structural modification of existing antibiotics, and research into and the study of chemical structures with new mechanisms of action and novel targets that resistant bacteria are sensitive to. Research efforts have been made to meet the urgent need for new treatments; some have succeeded to yield activity against resistant Gram-negative bacteria by deactivating the mechanism of resistance, like the action of the β-lactamase Inhibitor antibiotic adjuvants. Another promising trend was by referring to nature to develop naturally derived agents with antibacterial activity on novel targets, agents such as bacteriophages, DCAP(2-((3-(3,6-dichloro-9H-carbazol-9-yl)-2-hydroxypropyl)amino)-2(hydroxymethyl)propane1,3-diol, Odilorhabdins (ODLs), peptidic benzimidazoles, quorum sensing (QS) inhibitors, and metal-based antibacterial agents.

ACS Style

Zeinab Breijyeh; Buthaina Jubeh; Rafik Karaman. Resistance of Gram-Negative Bacteria to Current Antibacterial Agents and Approaches to Resolve It. Molecules 2020, 25, 1340 .

AMA Style

Zeinab Breijyeh, Buthaina Jubeh, Rafik Karaman. Resistance of Gram-Negative Bacteria to Current Antibacterial Agents and Approaches to Resolve It. Molecules. 2020; 25 (6):1340.

Chicago/Turabian Style

Zeinab Breijyeh; Buthaina Jubeh; Rafik Karaman. 2020. "Resistance of Gram-Negative Bacteria to Current Antibacterial Agents and Approaches to Resolve It." Molecules 25, no. 6: 1340.

Review
Published: 17 February 2020 in Molecules
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Background: The design and development of prodrugs is the most common and effective strategy to overcome pharmacokinetic and pharmacodynamic drawbacks of active drugs. A respected number of prodrugs have been reached the drugs market throughout history and the recent years have witnessed a significant increase in the use of prodrugs as a replacement of their parent drugs for an efficient treatment of various ailment. Methods: A Scan conducted to find recent approved prodrugs and prodrugs in development. Results: Selected prodrugs were reported and categorized in accordance to their target systems. Conclusions: the prodrug approach has shown many successes and still remains a viable and effective approach to deliver new active agents. This conclusion is supported by the recent approved prodrugs and the scan of clinical trials conducted between 2013–2018.

ACS Style

Anas Najjar; Abderrahman Najjar; Rafik Karaman. Newly Developed Prodrugs and Prodrugs in Development; an Insight of the Recent Years. Molecules 2020, 25, 884 .

AMA Style

Anas Najjar, Abderrahman Najjar, Rafik Karaman. Newly Developed Prodrugs and Prodrugs in Development; an Insight of the Recent Years. Molecules. 2020; 25 (4):884.

Chicago/Turabian Style

Anas Najjar; Abderrahman Najjar; Rafik Karaman. 2020. "Newly Developed Prodrugs and Prodrugs in Development; an Insight of the Recent Years." Molecules 25, no. 4: 884.

Editorial
Published: 28 December 2019 in Molecules
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Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials that is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules

ACS Style

Jean Jacques Vanden Eynde; Arduino A. Mangoni; Jarkko Rautio; Jérôme Leprince; Yasu-Taka Azuma; Alfonso T. García-Sosa; Christopher Hulme; Josef Jampilek; Rafik Karaman; Wei Li; Paula A. C. Gomes; Dimitra Hadjipavlou-Litina; Raffaele Capasso; Athina Geronikaki; Laura Cerchia; Jean-Marc Sabatier; Rino Ragno; Tiziano Tuccinardi; Andrea Trabocchi; Jean-Yves Winum; F. Javier Luque; Katalin Prokai-Tatrai; Mariana Spetea; Michael Gütschow; Ivan Kosalec; Catherine Guillou; M. Helena Vasconcelos; George Kokotos; Giulio Rastelli; Maria Emília Sousa; Clementina Manera; Sandra Gemma; Stefano Mangani; Carlo Siciliano; Stefania Galdiero; Hong Liu; Peter J. H. Scott; Cristóbal De Los Ríos; Luigi A. Agrofoglio; Simona Collina; Rita C. Guedes; Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–6. Molecules 2019, 25, 119 .

AMA Style

Jean Jacques Vanden Eynde, Arduino A. Mangoni, Jarkko Rautio, Jérôme Leprince, Yasu-Taka Azuma, Alfonso T. García-Sosa, Christopher Hulme, Josef Jampilek, Rafik Karaman, Wei Li, Paula A. C. Gomes, Dimitra Hadjipavlou-Litina, Raffaele Capasso, Athina Geronikaki, Laura Cerchia, Jean-Marc Sabatier, Rino Ragno, Tiziano Tuccinardi, Andrea Trabocchi, Jean-Yves Winum, F. Javier Luque, Katalin Prokai-Tatrai, Mariana Spetea, Michael Gütschow, Ivan Kosalec, Catherine Guillou, M. Helena Vasconcelos, George Kokotos, Giulio Rastelli, Maria Emília Sousa, Clementina Manera, Sandra Gemma, Stefano Mangani, Carlo Siciliano, Stefania Galdiero, Hong Liu, Peter J. H. Scott, Cristóbal De Los Ríos, Luigi A. Agrofoglio, Simona Collina, Rita C. Guedes, Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–6. Molecules. 2019; 25 (1):119.

Chicago/Turabian Style

Jean Jacques Vanden Eynde; Arduino A. Mangoni; Jarkko Rautio; Jérôme Leprince; Yasu-Taka Azuma; Alfonso T. García-Sosa; Christopher Hulme; Josef Jampilek; Rafik Karaman; Wei Li; Paula A. C. Gomes; Dimitra Hadjipavlou-Litina; Raffaele Capasso; Athina Geronikaki; Laura Cerchia; Jean-Marc Sabatier; Rino Ragno; Tiziano Tuccinardi; Andrea Trabocchi; Jean-Yves Winum; F. Javier Luque; Katalin Prokai-Tatrai; Mariana Spetea; Michael Gütschow; Ivan Kosalec; Catherine Guillou; M. Helena Vasconcelos; George Kokotos; Giulio Rastelli; Maria Emília Sousa; Clementina Manera; Sandra Gemma; Stefano Mangani; Carlo Siciliano; Stefania Galdiero; Hong Liu; Peter J. H. Scott; Cristóbal De Los Ríos; Luigi A. Agrofoglio; Simona Collina; Rita C. Guedes; Diego Muñoz-Torrero. 2019. "Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–6." Molecules 25, no. 1: 119.

Journal article
Published: 28 December 2019 in Annals of Agricultural Sciences
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The effluent of secondary treatment process at Al-Quds University wastewater treatment plant was tertiary treated using an Epuvalisation technique in which geranium plants (Pelargonium hortorum) was employed as a treatment vehicle. The Epuvalisation system was installed in a greenhouse in which germanium was planted hydroponically in a closed-loop mode using secondary treated wastewater (TWW) and fresh water (FW) as a control. The water quality analysis results before and after the growing season of TWW showed a reduction of 23% and 41%, for BOD and COD, respectively. The electrical conductivity (EC) and total dissolved solids (TDS) for TWW demonstrated a reduction of 52% and 53%, respectively. Similar trend was observed for FW in which the reduction in EC and TDS were 48% and 49%, respectively. Furthermore, the percent reduction of the concentration of suspended solids, phosphate ions (PO4−3), chloride ion (Cl−), total nitrogen (TN), and potassium ion (K+) in TWW were found to be 95%, 89%, 60% 98% and 59%, respectively. Plant growth parameters (plant height, fresh and dry weight, number of branches and flowers number) of geranium revealed no significant difference between irrigation with TWW and FW. The chemical plant analysis of roots, leaves, stems and flowers revealed no significant difference between hydroponic plantation in TWW and in FW. From these results it is safe to conclude that the Epuvalisation technique is a promising technique for advanced wastewater treatment using ornamental plants such as geranium due to its simplicity, low cost and easy use.

ACS Style

Mohannad Qurie; Sabreen Daghra; Mustafa Khamis; Amer Kanan; Zaher Barghouthi; Abdallah Alimari; Rafik Karaman. Application of the epuvalisation technology for the tertiary treatment of secondary treated effluents using geranium plants. Annals of Agricultural Sciences 2019, 64, 237 -243.

AMA Style

Mohannad Qurie, Sabreen Daghra, Mustafa Khamis, Amer Kanan, Zaher Barghouthi, Abdallah Alimari, Rafik Karaman. Application of the epuvalisation technology for the tertiary treatment of secondary treated effluents using geranium plants. Annals of Agricultural Sciences. 2019; 64 (2):237-243.

Chicago/Turabian Style

Mohannad Qurie; Sabreen Daghra; Mustafa Khamis; Amer Kanan; Zaher Barghouthi; Abdallah Alimari; Rafik Karaman. 2019. "Application of the epuvalisation technology for the tertiary treatment of secondary treated effluents using geranium plants." Annals of Agricultural Sciences 64, no. 2: 237-243.

Review
Published: 11 November 2019 in Toxins
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The growing incidence of microorganisms that resist antimicrobials is a constant concern for the scientific community, while the development of new antimicrobials from new chemical entities has become more and more expensive, time-consuming, and exacerbated by emerging drug-resistant strains. In this regard, many scientists are conducting research on plants aiming to discover possible antimicrobial compounds. The secondary metabolites contained in plants are a source of chemical entities having pharmacological activities and intended to be used for the treatment of different diseases. These chemical entities have the potential to be used as an effective antioxidant, antimutagenic, anticarcinogenic and antimicrobial agents. Among these pharmacologically active entities are the alkaloids which are classified into a number of classes, including pyrrolizidines, pyrrolidines, quinolizidines, indoles, tropanes, piperidines, purines, imidazoles, and isoquinolines. Alkaloids that have antioxidant properties are capable of preventing a variety of degenerative diseases through capturing free radicals, or through binding to catalysts involved indifferent oxidation processes occurring within the human body. Furthermore, these entities are capable of inhibiting the activity of bacteria, fungi, protozoan and etc. The unique properties of these secondary metabolites are the main reason for their utilization by the pharmaceutical companies for the treatment of different diseases. Generally, these alkaloids are extracted from plants, animals and fungi. Penicillin is the most famous natural drug discovery deriving from fungus. Similarly, marines have been used as a source for thousands of bioactive marine natural products. In this review, we cover the medical use of natural alkaloids isolated from a variety of plants and utilized by humans as antibacterial, antiviral, antifungal and anticancer agents. An example for such alkaloids is berberine, an isoquinoline alkaloid, found in roots and stem-bark of Berberis asculin P. Renault plant and used to kill a variety of microorganisms.

ACS Style

Amin Thawabtah; Salma Juma; Mariam Bader; Donia Karaman; Laura Scrano; Sabino A. Bufo; Rafik Karaman. The Biological Activity of Natural Alkaloids against Herbivores, Cancerous Cells and Pathogens. Toxins 2019, 11, 656 .

AMA Style

Amin Thawabtah, Salma Juma, Mariam Bader, Donia Karaman, Laura Scrano, Sabino A. Bufo, Rafik Karaman. The Biological Activity of Natural Alkaloids against Herbivores, Cancerous Cells and Pathogens. Toxins. 2019; 11 (11):656.

Chicago/Turabian Style

Amin Thawabtah; Salma Juma; Mariam Bader; Donia Karaman; Laura Scrano; Sabino A. Bufo; Rafik Karaman. 2019. "The Biological Activity of Natural Alkaloids against Herbivores, Cancerous Cells and Pathogens." Toxins 11, no. 11: 656.

Editorial
Published: 30 June 2019 in Molecules
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Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules

ACS Style

Arduino A. Mangoni; Jean Jacques Vanden Eynde; Josef Jampilek; Dimitra Hadjipavlou-Litina; Hong Liu; Jóhannes Reynisson; Maria Emília Sousa; Paula A. C. Gomes; Katalin Prokai-Tatrai; Tiziano Tuccinardi; Jean-Marc Sabatier; F. Javier Luque; Jarkko Rautio; Rafik Karaman; M. Helena Vasconcelos; Sandra Gemma; Stefania Galdiero; Christopher Hulme; Simona Collina; Michael Gütschow; George Kokotos; Carlo Siciliano; Raffaele Capasso; Luigi A. Agrofoglio; Rino Ragno; Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–5. Molecules 2019, 24, 2415 .

AMA Style

Arduino A. Mangoni, Jean Jacques Vanden Eynde, Josef Jampilek, Dimitra Hadjipavlou-Litina, Hong Liu, Jóhannes Reynisson, Maria Emília Sousa, Paula A. C. Gomes, Katalin Prokai-Tatrai, Tiziano Tuccinardi, Jean-Marc Sabatier, F. Javier Luque, Jarkko Rautio, Rafik Karaman, M. Helena Vasconcelos, Sandra Gemma, Stefania Galdiero, Christopher Hulme, Simona Collina, Michael Gütschow, George Kokotos, Carlo Siciliano, Raffaele Capasso, Luigi A. Agrofoglio, Rino Ragno, Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–5. Molecules. 2019; 24 (13):2415.

Chicago/Turabian Style

Arduino A. Mangoni; Jean Jacques Vanden Eynde; Josef Jampilek; Dimitra Hadjipavlou-Litina; Hong Liu; Jóhannes Reynisson; Maria Emília Sousa; Paula A. C. Gomes; Katalin Prokai-Tatrai; Tiziano Tuccinardi; Jean-Marc Sabatier; F. Javier Luque; Jarkko Rautio; Rafik Karaman; M. Helena Vasconcelos; Sandra Gemma; Stefania Galdiero; Christopher Hulme; Simona Collina; Michael Gütschow; George Kokotos; Carlo Siciliano; Raffaele Capasso; Luigi A. Agrofoglio; Rino Ragno; Diego Muñoz-Torrero. 2019. "Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–5." Molecules 24, no. 13: 2415.

Journal article
Published: 01 May 2019 in Net Journal of Agricultural Science
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Mohannad Qurie; Sabreen Daghra; Mustafa Khamis; Amer Kanan; Zaher Barghouthi; Abdallah Alimari; Sameh Nussiebah; Rafik Karaman. Rosemary (Rosmarinus officinalis) plants irrigation with secondary treated effluents using Epuvalisation technology. Net Journal of Agricultural Science 2019, 7, 69 -77.

AMA Style

Mohannad Qurie, Sabreen Daghra, Mustafa Khamis, Amer Kanan, Zaher Barghouthi, Abdallah Alimari, Sameh Nussiebah, Rafik Karaman. Rosemary (Rosmarinus officinalis) plants irrigation with secondary treated effluents using Epuvalisation technology. Net Journal of Agricultural Science. 2019; 7 (2):69-77.

Chicago/Turabian Style

Mohannad Qurie; Sabreen Daghra; Mustafa Khamis; Amer Kanan; Zaher Barghouthi; Abdallah Alimari; Sameh Nussiebah; Rafik Karaman. 2019. "Rosemary (Rosmarinus officinalis) plants irrigation with secondary treated effluents using Epuvalisation technology." Net Journal of Agricultural Science 7, no. 2: 69-77.

Editorial
Published: 31 December 2018 in Molecules
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Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of Editorials, which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal Molecules.

ACS Style

Arduino A Mangoni; Catherine Guillou; Jean Jacques Vanden Eynde; Christopher Hulme; Josef Jampilek; Wei Li; Katalin Prokai-Tatrai; Jarkko Rautio; Simona Collina; Tiziano Tuccinardi; Maria Emília Sousa; Jean-Marc Sabatier; Stefania Galdiero; Rafik Karaman; George Kokotos; Giangiacomo Torri; F. Javier Luque; M. Helena Vasconcelos; Dimitra Hadjipavlou-Litina; Carlo Siciliano; Michael Gütschow; Rino Ragno; Paula A. C. Gomes; Luigi A. Agrofoglio; Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–4. Molecules 2018, 24, 130 .

AMA Style

Arduino A Mangoni, Catherine Guillou, Jean Jacques Vanden Eynde, Christopher Hulme, Josef Jampilek, Wei Li, Katalin Prokai-Tatrai, Jarkko Rautio, Simona Collina, Tiziano Tuccinardi, Maria Emília Sousa, Jean-Marc Sabatier, Stefania Galdiero, Rafik Karaman, George Kokotos, Giangiacomo Torri, F. Javier Luque, M. Helena Vasconcelos, Dimitra Hadjipavlou-Litina, Carlo Siciliano, Michael Gütschow, Rino Ragno, Paula A. C. Gomes, Luigi A. Agrofoglio, Diego Muñoz-Torrero. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–4. Molecules. 2018; 24 (1):130.

Chicago/Turabian Style

Arduino A Mangoni; Catherine Guillou; Jean Jacques Vanden Eynde; Christopher Hulme; Josef Jampilek; Wei Li; Katalin Prokai-Tatrai; Jarkko Rautio; Simona Collina; Tiziano Tuccinardi; Maria Emília Sousa; Jean-Marc Sabatier; Stefania Galdiero; Rafik Karaman; George Kokotos; Giangiacomo Torri; F. Javier Luque; M. Helena Vasconcelos; Dimitra Hadjipavlou-Litina; Carlo Siciliano; Michael Gütschow; Rino Ragno; Paula A. C. Gomes; Luigi A. Agrofoglio; Diego Muñoz-Torrero. 2018. "Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–4." Molecules 24, no. 1: 130.

Editorial
Published: 04 December 2018 in Expert Opinion on Drug Delivery
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Anas Najjar; Rafik Karaman. The prodrug approach in the era of drug design. Expert Opinion on Drug Delivery 2018, 16, 1 -5.

AMA Style

Anas Najjar, Rafik Karaman. The prodrug approach in the era of drug design. Expert Opinion on Drug Delivery. 2018; 16 (1):1-5.

Chicago/Turabian Style

Anas Najjar; Rafik Karaman. 2018. "The prodrug approach in the era of drug design." Expert Opinion on Drug Delivery 16, no. 1: 1-5.

Research article
Published: 01 October 2018 in Chemical Biology & Drug Design
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A respected number of drugs suffer from bitter taste which results in patient incompliance. With the aim of solving the bitterness of guaifenesin, dimethyl maleate, maleate, glutarate, succinate and dimethyl succinate prodrugs were designed and synthesized. Molecular orbital methods were utilized for the design of the ester prodrugs. The density functional theory (DFT) calculations revealed that the hydrolysis efficiency of the synthesized prodrugs is significantly sensitive to the pattern of substitution on C=C bond and distance between the nucleophile and the electrophile. The hydrolysis of the prodrugs was largely affected by the pH of the medium. The experimental t1/2for the hydrolysis of guaifenesin dimaleate ester prodrugs in 1N HCl was the least and for guaifenesin dimethyl succinate was the highest. Functional heterologous expression of TAS2R14, a broadly tuned bitter taste receptor responding to guaifenesin, and experiments using these prodrugs revealed that, while some of the prodrugs still activated the receptor similarly or even stronger than the parent substance, succinate derivatization resulted in the complete loss of receptor responses. The predicted binding modes of guaifenesin and its prodrugs to the TAS2R14 homology model suggest that the decreased activity of the succinate derivatives may be caused by a clash with Phe247. This article is protected by copyright. All rights reserved.

ACS Style

Amin Thawabtah; Filomena Lelario; Laura Scrano; Sabino A. Bufo; Stefanie Nowak; Maik Behrens; Antonella Di Pizio; Masha Y. Niv; Rafik Karaman. Bitterless guaifenesin prodrugs-design, synthesis, characterization, in vitro kinetics, and bitterness studies. Chemical Biology & Drug Design 2018, 93, 262 -271.

AMA Style

Amin Thawabtah, Filomena Lelario, Laura Scrano, Sabino A. Bufo, Stefanie Nowak, Maik Behrens, Antonella Di Pizio, Masha Y. Niv, Rafik Karaman. Bitterless guaifenesin prodrugs-design, synthesis, characterization, in vitro kinetics, and bitterness studies. Chemical Biology & Drug Design. 2018; 93 (3):262-271.

Chicago/Turabian Style

Amin Thawabtah; Filomena Lelario; Laura Scrano; Sabino A. Bufo; Stefanie Nowak; Maik Behrens; Antonella Di Pizio; Masha Y. Niv; Rafik Karaman. 2018. "Bitterless guaifenesin prodrugs-design, synthesis, characterization, in vitro kinetics, and bitterness studies." Chemical Biology & Drug Design 93, no. 3: 262-271.

Journal article
Published: 16 August 2018 in Environmental Science and Pollution Research
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This study examines the photocatalytic activity of titanium dioxide (TiO2) semiconductor supported on borosilicate tubes (cut-off 290 nm) towards removal of a mix of persistent organic pollutants (POPs) from water. For this purpose, two widely used analgesic and anti-inflammatory drugs (NSAIDs), ibuprofen (IBU) and mefenamic acid, along with MCPA sodium monohydrate, which is a common herbicide frequently used in the agricultural activities, were selected as a case study. Borosilicate tubes were coated with titanium oxide through two different approaches: sol-gel dip-coating and a hybrid nanoparticle dip-coating and plasma-enhanced chemical vapour deposition (PECVD) process. The photochemical reactor that hosts the titania-coated tubes was designed to permit continuous throughput of liquid feed stream. The photodegradation experiments were performed in laboratory conditions under artificial irradiation simulating solar light. The efficiency of direct photolysis and heterogeneous photocatalysis (TiO2) was investigated, and the performance of each coating method was evaluated. Kinetic studies for each experiment were accomplished, the overall results showed poor efficiency and insufficient removal for NSAIDs through direct photolysis, whereas applying heterogeneous photacatalysis with TiO2 coated on borosilicate tubes was found to accelerate their degradation rate with complete decomposition. Concomitantly, kinetic experimental results showed a critical difference of performance for the two coating methods used; in particular, the degradation rates of pollutants by the sol-gel-coated tubes were much faster than the degradation by the nanoparticle/PECVD-coated tubes. Using TiO2 supported on borosilicate tubes appears to be a promising alternative to conventional TiO2 suspension and avoid post-separation stages. The results achieved in this study can be used to optimise large-scale applications, and expanding the study to cover a wide range of pollutants will lead to achieve more representative results.

ACS Style

Samer Khalaf; Jawad H. Shoqeir; Laura Scrano; Rafik Karaman; Sabino A. Bufo. Photodegradation using TiO2-activated borosilicate tubes. Environmental Science and Pollution Research 2018, 26, 19025 -19034.

AMA Style

Samer Khalaf, Jawad H. Shoqeir, Laura Scrano, Rafik Karaman, Sabino A. Bufo. Photodegradation using TiO2-activated borosilicate tubes. Environmental Science and Pollution Research. 2018; 26 (19):19025-19034.

Chicago/Turabian Style

Samer Khalaf; Jawad H. Shoqeir; Laura Scrano; Rafik Karaman; Sabino A. Bufo. 2018. "Photodegradation using TiO2-activated borosilicate tubes." Environmental Science and Pollution Research 26, no. 19: 19025-19034.

Research article chemistry
Published: 03 July 2018 in Arabian Journal for Science and Engineering
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In this study, the removal of selected pharmaceuticals including ibuprofen, diclofenac sodium, indomethacin, chlorpheniramine maleate, and paracetamol from water using natural Jordanian zeolite was studied. The influence of pH, contact time, adsorbent dosage, and initial pharmaceutical concentration on the adsorption process was investigated using batch and column methods. The optimal pH for the removal of all selected pharmaceuticals was found to be 2 except for diclofenac sodium where the optimal pH was 6. The optimum adsorption time was found to be 80 min. The percentage removal increased as the initial concentration of the pharmaceuticals increased from 10.0 to 50.0 mg/L except for indomethacin where the removal decreased as the initial concentration increased. After optimization, the highest removal was found to be 88.3, 30.1, 59.0, 85.8, and 12.7% for ibuprofen, diclofenac sodium, indomethacin, chlorpheniraminemaleate, and paracetamol, respectively. Langmuir and Freundlich isotherm models were used to evaluate the adsorption efficiencies of the investigated pharmaceuticals. The results demonstrated that Langmuir isotherm fits the experimental data for diclofenac sodium, indomethacin and paracetamol with adsorption capacity \((Q_{\mathrm{max}})\) of 4.8, 26.6, and 55.6 mg/g, respectively, whereas Freundlich isotherm fits the experimental data for both ibuprofen and chlorpheniramine maleate. Continues flow experiment was performed on ibuprofen under constant influent concentration and fixed flow rate. Equal eluted fractions of 100 mL were collected and analyzed for ibuprofen content. The results indicated that percentage removal of ibuprofen on zeolite was found to be the highest after fraction 9 with 78% removal.

ACS Style

Fuad Al-Rimawi; Mahran Daana; Mustafa Khamis; Rafik Karaman; Hani Khoury; Mohannad Qurie. Removal of Selected Pharmaceuticals from Aqueous Solutions Using Natural Jordanian Zeolite. Arabian Journal for Science and Engineering 2018, 44, 209 -215.

AMA Style

Fuad Al-Rimawi, Mahran Daana, Mustafa Khamis, Rafik Karaman, Hani Khoury, Mohannad Qurie. Removal of Selected Pharmaceuticals from Aqueous Solutions Using Natural Jordanian Zeolite. Arabian Journal for Science and Engineering. 2018; 44 (1):209-215.

Chicago/Turabian Style

Fuad Al-Rimawi; Mahran Daana; Mustafa Khamis; Rafik Karaman; Hani Khoury; Mohannad Qurie. 2018. "Removal of Selected Pharmaceuticals from Aqueous Solutions Using Natural Jordanian Zeolite." Arabian Journal for Science and Engineering 44, no. 1: 209-215.

Editorial
Published: 30 June 2018 in Molecules
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Arduino A. Mangoni; Tiziano Tuccinardi; Simona Collina; Jean Jacques Vanden Eynde; Diego Muñoz-Torrero; Rafik Karaman; Carlo Siciliano; Maria Emília Sousa; Katalin Prokai-Tatrai; Jarkko Rautio; Catherine Guillou; Michael Gütschow; Stefania Galdiero; Hong Liu; Luigi A. Agrofoglio; Jean-Marc Sabatier; Christopher Hulme; George Kokotos; Qidong You; Paula A. C. Gomes. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-3. Molecules 2018, 23, 1596 .

AMA Style

Arduino A. Mangoni, Tiziano Tuccinardi, Simona Collina, Jean Jacques Vanden Eynde, Diego Muñoz-Torrero, Rafik Karaman, Carlo Siciliano, Maria Emília Sousa, Katalin Prokai-Tatrai, Jarkko Rautio, Catherine Guillou, Michael Gütschow, Stefania Galdiero, Hong Liu, Luigi A. Agrofoglio, Jean-Marc Sabatier, Christopher Hulme, George Kokotos, Qidong You, Paula A. C. Gomes. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-3. Molecules. 2018; 23 (7):1596.

Chicago/Turabian Style

Arduino A. Mangoni; Tiziano Tuccinardi; Simona Collina; Jean Jacques Vanden Eynde; Diego Muñoz-Torrero; Rafik Karaman; Carlo Siciliano; Maria Emília Sousa; Katalin Prokai-Tatrai; Jarkko Rautio; Catherine Guillou; Michael Gütschow; Stefania Galdiero; Hong Liu; Luigi A. Agrofoglio; Jean-Marc Sabatier; Christopher Hulme; George Kokotos; Qidong You; Paula A. C. Gomes. 2018. "Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-3." Molecules 23, no. 7: 1596.