Structural modifications of thiazolidinediones at 3^rd and 5^th position have exhibited significant biological activities. In view of the facts, and based on in silico studies carried out on thiazolidine-2,4-diones as HIV-1- RT inhibitors, a novel series of 2,4-thiazolidinedione analogs have been designed and synthesized. Title compounds were prepared by the reported method. Conformations of the structures were assigned on the basis of results of different spectral data. The assay of HIV-1 RT was done as reported by Silprasit et al. Antimicrobial activity was determined by two fold serial dilution method. Docking study was performed for the highest active compounds by using Glide 5.0. The newly synthesized compounds were evaluated for their HIV-1 RT inhibitory activity. Among the synthesized compounds, compound 24 showed significant HIV-1 RT inhibitory activity with 73% of inhibition with an IC₅₀ value of 1.31 μM. Compound 10 showed highest activity against all the bacterial strains. A molecular modeling study was carried out in order to investigate the possible interactions of the highest active compounds 24, 10 and 4 with the non nucleoside inhibitory binding pocket(NNIBP) of RT, active site of GlcN-6-P synthase and cytochrome P450 14-α-sterol demethylase from Candida albicans (Candida P450DM) as the target receptors respectively using the Extra Precision (XP) mode of Glide software. A series of novel substituted 2-(5-benzylidene-2,4-dioxothiazolidin-3-yl)-N-(phenyl)propanamides (4–31) have been synthesized and evaluated for their HIV-1 RT inhibitory activity, antibacterial and antifungal activities. Some of the compounds have shown significant activity. Molecular docking studies showed very good interaction.

Synthesis, antibacterial and potential anti-HIV activity of some novel imidazole analogs: A series of 1-(2-methyl-4-nitro-imidazol-1-yl)-3-arylaminopropan-2-ones (2a-e), 2-methyl-5-nitro-1-{2-[arylmethoxy] ethyl}-1H-imidazoles (5a-d), and N-(3-hydroxyphenyl)-2-(substituted imidazol-1-yl)alkanamides (8a-e) were synthesized with the aim to develop novel imidazole analogs with broad-spectrum chemotherapeutic properties. Title compounds were evaluated for their anti-HIV and antibacterial activities.

All human cells contain the universal autocoid adenosine, which interacts with four types of G protein-coupled receptors (GPCRs), namely A₁, A_2A, A_2B, and A₃ adenosine receptors (ARs). Among these receptors, A_2A and A_2B ARs activate adenylate cyclase, while A₁ and A₃ ARs suppress the adenylate cyclase activity. Adenosine-receptor interactions play a crucial role in cancer biology by modulating the immune microenvironment, which tumors exploit to create immunosuppression that promotes their growth and metastasis. When the A_2A AR is activated on natural killer (NK) cells and T cells, it reduces their ability to carry out cytotoxic functions. This activation also encourages the formation of immune-suppressing cell types, such as myeloid-derived suppressor cells (MDSCs) and regulatory T cells (Tregs), further weakening the immune response. Targeting adenosine receptors, particularly the A_2A subtype, represents a promising therapeutic strategy. By antagonizing these receptors, it may be possible to restore T cell function, helping the body to recognize and attack cancer cells more effectively. Despite recent advancements in the discovery of novel, targeted anticancer agents, these treatments have shown limited effectiveness against metastatic tumours, complicating cancer management. Moreover, developing adenosine receptor agonists or antagonists with high target selectivity and potency remains a significant challenge, as the widespread distribution of adenosine receptors throughout the body raises concerns about off-target effects and reduced therapeutic efficacy. In order to improve outcomes for patients with advanced cancer, researchers are actively investigating safer and more efficient chemotherapy substitutes. However, drugs that activate A₃ adenosine receptors and block A_2A receptors are being explored as a novel approach for cancer treatment. Monoclonal antibodies and small-molecule inhibitors targeting the CD39/CD73/A_2A AR axis are also being tested in clinical trials, both as standalone treatments and in combination with anti-PD-1/PD-L1 immunotherapies. This review primarily focuses on the signaling pathways and the therapeutic potential of various adenosine receptor agonists and antagonists across various cancer types, highlighting their ongoing evaluation in preclinical and clinical trials, both as monotherapies and in rational combination with immunotherapy, chemotherapy, or targeted therapies, potentially leading to the development of advanced treatments that could aid in tumor suppression.

In this study 26 novel benzimidazole compounds bearing alkyl chain as linker at N-1 position were synthesized and evaluated to investigate their possible anti-HIV and antimicrobial activities. Structures of the synthesized compounds were elucidated by spectral data. HIV-1 RT inhibitory activity was evaluated by using HIV-1 RT RNA-dependent DNA polymerase activity assay. Among these derivatives, compounds 43, 45, 50 and 51 were found to have reasonable HIV-1 RT inhibitory activity while the rest exhibited weak activity in comparison to the standard efavirenz. On the other hand, most of the test compounds were found to be significantly effective against gram positive bacteria (Staphylococcus aureus and Bacillus subtilis) and some gram-negative bacterial strains (Escherichia coli, Salmonella typhi, Klebsiella pneumoniae and Pseudomonas aeruginosa), among which compounds 37, 43, 45, 50 and 51 surfaced out as the most effective antibacterials but less effective than the standard ciprofloxacin. Compounds 33, 41 and 47 also showed significant activity against almost all the bacterial strains while all other compounds showed moderate activity towards all the bacterial strains. In case of fungal strains like Candida albicans and Aspergillus niger, almost all the compounds were found to exhibit potency comparable or more than that of standard drug fluconazole except for the compounds 34, 39, 42, 47 and 48 which exhibited moderate to good activity against both the fungal strains. A structure activity relationship (SAR) as well as virtual ADME and toxicity prediction were carried out and a connection between activities, electronic, physicochemical properties and toxicity levels of the target compounds was determined.

In this paper, we present the drug loading and release works of ${\mathrm{L}\mathrm{a}}_{0.67}{\mathrm{S}\mathrm{r}}_{0.33}{\mathrm{M}\mathrm{n}\mathrm{O}}_3$ (LSMO) manganite nanoparticles (NPs). The LSMO NPs, grown using the sol–gel method, were embedded in an acrylic interpenetrating polymer network to make the sample applicable for biomedical purposes. The results of scanning electron microscopy showed that these NPs were well dispersed in the polymer. The grain size of these NPs lies in the range of 25–45 nm, as confirmed by transmission electron microscopy. The measurements of DC magnetization and hysteresis loops reveal that the basic magnetic behaviour of the LSMO NPs remained almost unaltered even after embedding in polymer, but with lower saturation value of magnetization. The drug loading and release studies of the grown sample were carried out using an antibiotic, ciprofloxacin. The minimum inhibitory effect of the sample loaded with this drug has exhibited high activity against different strains of bacteria, comparable to the pure ciprofloxacin.

Background: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are one of the key components in highly active anti-retroviral therapy because of their high specificity and less toxicity. NNRTIs inhibit reverse transcriptase enzyme by binding to the allosteric site, which is 10Å away from the active site. Rapid emergence of resistance is the major problem with all anti-HIV agents. Hence, there is continuous need to develop novel anti-HIV agents active against both drug sensitive and resistance strains. Results: All the 16 synthesized 2-(1,3-dioxo-3a,4-dihydro-1H-isoindol-2(3H,7H,7aH)-yl)-N-(substitutedphenyl) acetamide 4(a-p) analogs were characterized by Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy, mass spectroscopy, and elemental analysis. Lipinski rule of five parameters and molecular parameters like solubility, drug likeness, and drug score were derived for designed analogs using online servers like Molinspiration and Osiris property explorer. Synthesized compounds were evaluated for their HIV-1 reverse transcriptase inhibitor activity by HIV-1 RNA-dependent DNA polymerase activity assay at 2 and 20 μM concentrations. Conclusions: Among the 16 synthesized compounds, 4a, 4b, 4f, 4g, 4k, and 4l showed weak reverse transcriptase inhibitor activity at 20 μM concentration. For the designed compounds, there was no correlation observed between molecular modeling and in vitro studies.