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The incidence of cancer is increasing worldwide, affecting a vast majority of the human population. As new different anticancer agents are being developed now, the requirement is to deal somehow with them and evaluate their safety. Among them, pyridine based drugs are contributing a lot, as it is one of the imperative pharmacophores occurring synthetically as well as naturally in heterocyclic compounds, and having a wide range of therapeutic applications in the area of drug discovery, thereby offering many chances for further improvement in antitumor agents via acting onto numerous receptors of extreme prominence. Many pyridine derivatives have been 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 expansions of pyridine together with its molecular docking, structure-activity-relationship, availability in the market, and a summary of recently patented and published research works that shall jointly help the scientists to produce effective drugs with the desired pharmacological activity.
Pyridine is an imperative pharmacophore, a privileged scaffold and an exceptional heterocyclic system in the field of drug discovery which provides many opportunities in study/explore this moiety as an anticancer agent by acting on various receptors of utmost importance. Several pyridine derivatives are reported to inhibit tubulin polymerization, androgen receptors, human carbonic anhydrase, kinase, topoisomerase enzyme and many other targets for controlling and curing global health issue of cancer. Now a days in combination with other moieties researchers are focusing for development of pyridine new entities for the treatment of cancer. This review throws light on recent biological expansions of pyridine along with their structure activity relationships/molecular docking to deliver association between various synthesized newer derivatives and receptor sites.
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.
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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.
Among the large variety of nitrogen and oxygen-containing heterocycles, 1,3,4-oxadiazole, the scaffold, has attracted considerable attention owing to its ability to show an extensive range of pharmacological actions. According to literature investigations, prepared 1,3,4-oxadiazole and its derivative are pharmacologically significant and consist of a variety of activities, such as anticonvulsant, anticancer, antioxidant, anti-inflammatory, antibacterial, antidiabetic, etc. These heterocyclics are formed mainly by the cyclization reactions of various reactants under diverse reaction circumstances. Therefore, significant efforts of organic chemists have been directed towards the synthesis of new drug candidates containing 1,3,4-oxadiazole subunits connected to an established potential pharmacophore to improve the efficacy and potency. This article aims to highlight recent publications on the various synthesis techniques of 1,3,4-oxadiazole and related compounds over the previous ten years (2011–2021). The purpose of this review is to help researchers by summarizing several synthetic strategies for synthesizing oxadiazole.
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