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Inhibitors of pantothenate synthetase of Mycobacterium tuberculosis – a medicinal chemist perspective

机译：结核分枝杆菌泛酸合成酶的抑制剂 - 一种药用化学家的观点

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Tuberculosis (TB), one of the most prevalent infections, is on the rise today. Although there are drugs available in the market to combat this lethal disorder, there are several shortcomings with the current drug regimen, such as prolonged treatment period, drug resistance, high cost, etc. Hence, it is inevitable for the current researchers across the globe to embark on new strategies for TB drug discovery, which will yield highly active low cost drugs with a shorter treatment period. To achieve this, novel strategies need to be adopted to discover new drugs. Pantothenate Synthetase (PS) is one such striking drug target in Mycobacterium tuberculosis (MTB). It was observed that the pantothenate biosynthetic pathway is crucial for the pathogenicity of MTB. Pantothenate is absent in mammals and needs to be obtained from dietary sources. Hence, the pantothenate biosynthesis pathway is an impending target for emerging new therapeutics to treat TB. Worldwide, several approaches have been implemented by researchers in the quest for these inhibitors such as high-throughput screening, simulating the reaction intermediate pantoyl adenylate, use of vibrant combinatorial chemistry, hybridization approach, virtual screening of databases, inhibitors based on the crystal structure of MTB PS, etc. The present review recapitulates current developments in PS inhibitors, important analogues of numerous metabolic intermediates, and newly established inhibitors with innumerable chemical structures.
机译：结核病（TB）是最普遍的感染之一，是在今天的上升。虽然市场上有毒品可用于打击这种致命的障碍，但目前的药物方案有几种缺点，如长期治疗期，耐药性，高成本等，因此，目前全球的研究人员是不可避免的踏上Tb药物发现的新策略，这将产生高度活跃的低成本药物，治疗期更短。为实现这一目标，需要采用新的战略来发现新药。泛酸合成酶（PS）是结核分枝杆菌（MTB）中的一种这种尖尖药物靶标。观察到泛酸生物合成途径对于MTB的致病性至关重要。哺乳动物中不存在泛酸，需要从膳食来源获得。因此，泛酸生物合成途径是用于新兴治疗TB的新治疗方法的即将靶标。在全球范围内，研究人员在寻求这些抑制剂如高通量筛选，模拟反应中间食肉型腺苷酸，使用充满活力的组合化学，杂交方法，数据库虚拟筛选，基于晶体结构的抑制器的抑制剂MTB PS等。本综述概述了PS抑制剂的电流发展，许多代谢中间体的重要性类似物，以及具有无数化学结构的新建立的抑制剂。

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