部分抗结核药物杂环核的 QSAR 研究和药物设计综述

R ROBIN JIYO, M VETRIVEL RAJAN, M. HARI SANKERJI
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引用次数: 0

摘要

这篇综述文章探讨了结核分枝杆菌耐药菌株这一紧迫问题,几十年来,由于抗生素在临床上的广泛和无节制使用,结核分枝杆菌出现了耐药菌株。为了应对这一挑战,人们开发了各种方法来合成新的抗结核化合物。其中,基于片段的药物发现(FBDD)方法已被证明是一种有效的策略。1,2-噻唑类化合物是在抗结核方面表现出巨大潜力的一类化合物。文章讨论了这些化合物的重要性及其作为未来抗结核药物的潜力。此外,文章还深入探讨了药物开发中采用的各种策略,强调了 FBDD 的相关性和有效性。分析方法在表征抗结核抗生素的特性方面起着至关重要的作用,文章重点介绍了液相色谱法和伏安法作为测定这些化合物的首选技术。抗结核抗生素的氧化还原特性使其适合使用电化学方法进行分析,其中伏安法尤其适用。此外,文章还强调了利用伏安法对不同剂型和人体体液中的各类抗生素进行定量分析的重要性。这种方法价格低廉,特别适合发展中国家,为监测和评估抗结核药物的存在提供了一种具有成本效益的方法。总之,这篇综述文章为当前应对结核病耐药性的策略提供了宝贵的见解,并强调了 1,2-二唑作为未来抗结核药物的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Review for QSAR studies and drug design of selected heterocyclic nucleus of antitubercular drugs
This review article explores the pressing issue of drug-resistant strains of Mycobacterium tuberculosis, which have emerged due to the widespread and uncontrolled use of antibiotics in clinical settings over several decades. In response to this challenge, various methods have been developed for synthesizing new antitubercular compounds. Among these, the fragment-based drug discovery (FBDD) approach has shown promise as an effective strategy. One class of compounds that has exhibited significant potential in combating tuberculosis is 1,2-diazoles. The article discusses the importance of these compounds and their potential as future antitubercular drugs. Additionally, it delves into the various strategies employed in drug development, emphasizing the relevance and efficacy of FBDD. Analytical methods play a crucial role in characterizing antitubercular antibiotics, and the article highlights liquid chromatography and voltammetry as preferred techniques for determining these compounds. The redox (oxidation/reduction) properties of antituberculars make them amenable to analysis using electrochemical methods, with voltammetry being particularly suitable. Furthermore, the article underscores the significance of utilizing voltammetry for quantifying different categories of antibiotics in both dosage forms and human body fluids. The affordability of this method makes it particularly advantageous for developing countries, providing a cost-effective approach to monitor and assess the presence of antitubercular drugs. Overall, the review article offers valuable insights into the current strategies for addressing drug resistance in tuberculosis and highlights the potential of 1,2-diazoles as future antitubercular agents.
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