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当前对苯并咪唑和咪唑衍生物的化学和抗结核潜力的深入了解。

Current Insights into the Chemistry and Antitubercular Potential of Benzimidazole and Imidazole Derivatives.

机构信息

Department of Pharmaceutical Sciences, Dr. Harisingh Gour University (A Central University), Sagar (MP), India.

Department of Chemistry, Dr. Harisingh Gour University (A Central University), Sagar (MP), India.

出版信息

Mini Rev Med Chem. 2021;21(5):643-657. doi: 10.2174/1389557520666201102094401.

DOI:10.2174/1389557520666201102094401
PMID:33138762
Abstract

Tuberculosis is a disease caused by Mycobacterium tuberculosis (Mtb), affecting millions of people worldwide. The emergence of drug resistance is a major problem in the successful treatment of tuberculosis. Due to the commencement of MDR-TB (multi-drug resistance) and XDR-TB (extensively drug resistance), there is a crucial need for the development of novel anti-tubercular agents with improved characteristics such as low toxicity, enhanced inhibitory activity and short duration of treatment. In this direction, various heterocyclic compounds have been synthesized and screened against Mycobacterium tuberculosis. Among them, benzimidazole and imidazole containing derivatives have been found to have potential anti-tubercular activity. The present review focuses on various imidazole and benzimidazole derivatives (from 2015-2019) with their structure-activity relationships in the treatment of tuberculosis.

摘要

结核病是由结核分枝杆菌(Mtb)引起的疾病,影响着全球数百万人。耐药性的出现是成功治疗结核病的主要问题。由于耐多药结核病(MDR-TB)和广泛耐药结核病(XDR-TB)的出现,迫切需要开发具有改善的特性的新型抗结核药物,例如低毒性、增强的抑制活性和较短的治疗时间。在这方面,已经合成了各种杂环化合物并对结核分枝杆菌进行了筛选。其中,发现含有苯并咪唑和咪唑的衍生物具有潜在的抗结核活性。本综述重点介绍了 2015 年至 2019 年期间具有结构-活性关系的各种咪唑和苯并咪唑衍生物在结核病治疗中的应用。

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