结核分枝杆菌烯酰乙酰还原酶 (InhA) 抑制剂的开发:微型综述。

IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Mini reviews in medicinal chemistry Pub Date : 2024-09-19 DOI:10.2174/0113895575309785240902102421
Navin Kumar Tailor, Geeta Deswal, Kumar Guarve, Ajmer Singh Grewal
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引用次数: 0

摘要

这篇综述文章深入探讨了乙酰酰基载体蛋白还原酶(InhA;ENR)的关键作用,它是依赖 NADH 的酰基载体蛋白还原酶家族中的一种重要酶,强调了它在脂肪酸合成中的重要作用,更具体地说,是在霉菌酸的生物合成中的重要作用。本文献综述的主要目的是阐明以抑制 InhA 为目标的各种支架及其发展过程,从而破坏霉菌酸的生物合成。我们系统地探讨了硫脲、哌嗪、噻二唑、三唑、喹唑啉、苯甲酰胺、罗丹宁、苯并恶唑和吡啶等各种支架作为 InhA 抑制剂的潜力。值得注意的是,噻二唑和三唑衍生物在纳摩尔浓度范围内显示出良好的 IC50 值。该综述对 InhA 的结构、结构-活性关系提供了全面的见解,并详细概述了作为 InhA 有效抑制剂的不同支架。
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Development of Mycobacterium tuberculosis Enoyl Acyl Reductase (InhA) Inhibitors: A Mini-Review.

This review article delves into the critical role of Enoyl acyl carrier protein Reductase (InhA; ENR), a vital enzyme in the NADH-dependent acyl carrier protein reductase family, emphasizing its significance in fatty acid synthesis and, more specifically, the biosynthesis of mycolic acid. The primary objective of this literature review is to elucidate diverse scaffolds and their developmental progression targeting InhA inhibition, thereby disrupting mycolic acid biosynthesis. Various scaffolds, including thiourea, piperazine, thiadiazole, triazole, quinazoline, benzamide, rhodanine, benzoxazole, and pyridine, have been systematically explored for their potential as InhA inhibitors. Noteworthy findings highlight thiadiazole and triazole derivatives, demonstrating promising IC50 values within the nanomolar concentration range. The review offers comprehensive insights into InhA's structure, structure-activity relationships, and a detailed overview of distinct scaffolds as effective inhibitors of InhA.

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来源期刊
CiteScore
7.80
自引率
0.00%
发文量
231
审稿时长
6 months
期刊介绍: The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. Mini-Reviews in Medicinal Chemistry covers all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
期刊最新文献
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