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首页> 外文期刊>Journal of Young Pharmacists >Synthesis, Characterization and Biological Evaluation of Novel 1, 4-Benzodiazepine Derivatives as Potent Anti-Tubercular Agents
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Synthesis, Characterization and Biological Evaluation of Novel 1, 4-Benzodiazepine Derivatives as Potent Anti-Tubercular Agents

机译：新型1,4-苯二氮杂卓类衍生物作为强效抗结核药的合成，表征和生物学评价

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Background: Benzodiazepines are interesting compounds due to their therapeutic properties. TB chemotherapy is highly regulated and Its research research is often considered non-remunerative. Hence, there remains a pressing requisite to discover novel, potent and safe anti-TB agents. Objective: One of the biggest problem of Tuberculosis is the lack of effective treatments. Bedaquiline (2013) and Delaminid (2014) are the only two agents approved for treating tuberculosis after Rifampicin (1963). This clearly shows the need for new lead molecules to fight against tuberculosis. Methodology: In the present work, a series of eighteen derivatives of 1, 4-Benzodiazepines were synthesized by condensation of o-phenylenediamines with 1, 3-diketone (Dimedone). Further these synthesized derivatives were analyzed by IR, NMR and MASS spectral studies and are screened for anti-tubercular and antimicrobial activity. Results: Among these, potent activity were observed for compounds 9, 10 (MIC 1.6 μg/mL) followed by 11(3.12 μg/mL), 04 (6.25 μg/mL) against M. tuberculosis H37Rv. We report here the synthesis, screening data and SAR studies of Benzodiazepines and its derivatives as Antitubercular agents. Conclusion: In conclusion, we synthesized eighteen 1, 4-Benzodiazepines derivatives with selective anti-tubercular activity.
机译：背景：苯二氮卓类药物由于其治疗特性而成为令人感兴趣的化合物。结核病的化疗受到严格管制，其研究通常被认为是无偿的。因此，发现新颖，有效和安全的抗结核病药物仍然迫切需要。目的：结核病的最大问题之一是缺乏有效的治疗方法。 Bedaquiline（2013）和Delaminid（2014）是继利福平（1963）之后被批准用于治疗结核病的仅有的两种药物。这清楚地表明需要新的先导分子来对抗结核病。方法：在目前的工作中，通过邻苯二胺与1，3-二酮（二甲酮）的缩合反应合成了18种1，4-苯二氮卓类衍生物。此外，通过IR，NMR和MASS光谱研究分析了这些合成的衍生物，并筛选了其抗结核和抗微生物活性。结果：在这些化合物中，观察到化合物9、10（MIC 1.6μg/ mL），接着是11（3.12μg/ mL），04（6.25μg/ mL）对结核分枝杆菌H37Rv的有效活性。我们在此报告苯二氮卓类药物及其衍生物作为抗结核药的合成，筛选数据和SAR研究。结论：总之，我们合成了18种具有选择性抗结核活性的1，4，4-苯二氮卓类衍生物。

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