The incidence of cancer is increasing worldwide, affecting a vast majority of the human population, therefore, new different anticancer agents are being developed now and their safety still needs to be evaluated. Among them, pyridine based drugs are contributing a lot, as they are one of the imperative pharmacophores occurring synthetically as well as naturally in heterocyclic compounds, having a wide-range of therapeutic applications in the area of drug discovery that offers many chances for further improvement in antitumor agents via acting onto numerous receptors of extreme prominence. Many pyridine derivatives are reported to inhibit enzymes, receptors and many other targets for controlling and curing the global health issue of cancer. Nowadays in combination with other moieties, researchers are focusing on the development of pyridine-based new derivatives for cancer treatment. Therefore, this review sheds light on the recent therapeutic expansion of pyridine together with its molecular docking, structure-activity-relationship, availability in the market, a summary of recently patented and published research works that shall jointly help the scientists to produce effective drugs with the desired pharmacological activity.
Benzothiazole is a heterocyclic compound that contains a benzene ring fused with a five-member 1,3-thiazole ring. Several types of research have established its potential as an antimicrobial agent, anticancer agent, anti-epileptic agent, antiviral agent, etc. Nowadays, various effective drugs utilize the hybridization of two or more pharmacophores in a single-molecule for synergizing its pharmacological action or to interact with more than one target or to reduce the side effects associated with it. In this article, various strategies for the synthesis of different pharmacologically active hybrid compounds containing benzothiazole with different substituents are highlighted. Apart from presenting the synthesis strategies, the article also highlights various pharmacological actions and molecular interactions with different biological molecules of the potential drugs containing benzothiazole.
1 February 2022 in Mini-Reviews in Organic Chemistry
Background:: Diabetes mellitus refers to one of the leading cause of diseases that affect large populations of human and is characterized by a high glucose level in the blood (also known as hyperglycemia). Thiazolidinedione (TZD) is a five-member heterocyclic compound consisting of three carbons, nitrogen and sulfur. It is also known as glitazones, can be used as potent hypoglycemic agents and is also reduce many other cardiovascular risk factors including percutaneous coronary intervention, carotid and coronary atherosclerosis. As it plays a very important role in the field of medicinal chemistry or pharmaceutical sciences, novel medicine developed and many are on underdevelopment, these derivatives have thiazolidinedione as their primary nucleus.Objective:: This article has discussed the different synthetic procedures of thiazolidinediones that exhibited potential antidiabetic activity by the activation of PPAR-γ, by reducing the blood glucose levels and by different metabolic process incorporation.Conclusion:: Thiazolidinediones has effective profile as the future investigational drug and can be processed in drug discovery because of its efficient anti-diabetic potential.
16 September 2020 in International Journal of Applied Pharmaceutics
Objective: The research work unveils the use of nuclear magnetic resonance (NMR) technique for quantitative determination and method validation of obeticholic acid. As standard expository methodology for more up to date medications or formulations may not be available in pharmacopeias, hence it is fundamental need to create novel analytical procedures which should be precise and accurate. Methods: Proton (1H) and carbon (13C) NMR analysis were initially performed to confirm the preliminary authenticity of obeticholic acid API. Method validation was accomplished on the basis of standard guidelines for the parameters, in which tetramethylbenzene as an internal standard and deuterated dimethyl sulfoxide as a diluent were used to assess the obeticholic acid. Results: For the quantification of the drug, the proton nuclear magnetic resonance signals at 0.602 ppm and 6.86 ppm corresponding to the analyte proton of drug and internal standard respectively were used. The curve equation calculated from the regression method, the relative-standard-deviation and correlation-coefficient were found to be 0.743% and 0.9989 respectively, indicating good linearity. Consequently, the quantitative assay of the drug was found to be 99.91% in linearity with limit of detection and quantification values as 0.0773 mg and 0.2344 mg respectively, making successful the study of method validation for obeticholic acid. Conclusion: The advantage of the method was that no reference standard of analyte drug was required for quantification and method validation. The method is non-destructive and can be applied for quantification of drug in commercial pharmaceutical formulation products.
The two benzyl rings in the title quinoline derivative, C24H19NO3, are inclined to the quinoline ring mean plane by 74.09 and 89.43 (7)o, respectively, and to each other by 63.97 (10)o. The carboxylate group is twisted from the quinoline ring mean plane by 32.2 (2) . Bifurcated C-H, H...O hydrogen bonds connect molecules in the crystal, forming layers parallel to the ac plane. The two layers of the crystal are connected by C-H...\(\pi\) interactions, and C-H...O contact form an S(6) ring motif. The HOMO-LUMO energy gap was found to be 0.15223 a.u. and the Hirshfeld surface analysis exhibited that H H (46.6 %) intermolecular interaction played a key role in the Hirshfeld surface of the title compound.
25 April 2023 in International Journal of Research in Ayurveda and Pharmacy