A Comprehensive Review on Discovery, Development, the Chemistry of Quinolones, and Their Antimicrobial Resistance.

IF 3.3 4区医学 Q3 CHEMISTRY, MEDICINAL

Current topics in medicinal chemistry Pub Date : 2025-08-05 DOI:10.2174/0115680266355989250730072511

Gayatri S Patil, Kiran N Gaikwad, Shailendra S Suryawanshi, Parixit Bhandurge

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Abstract

Quinolones, discovered in the 1970s, have played a critical role in revolutionizing the treatment of bacterial infections due to their broad-spectrum antimicrobial activity. Over the decades, these compounds have been extensively studied, resulting in the development of numerous new derivatives. This review explores the history and development of quinolones, focusing on their Structure-Activity Relationship (SAR), mechanisms of action, and the challenges posed by antimicrobial resistance. The key resistance mechanisms include mutations in DNA gyrase and topoisomerase IV, which reduce drug binding, plasma-mediated mechanisms, and chromosomal changes that decrease drug uptake or retention. These mechanisms highlight the need for innovative approaches to design quinolones to overcome these resistance pathways. This review also provides an understanding of the SAR of quinolones and, by integrating historical advancements and current challenges, it provides a foundation for the development of next-generation quinolone derivatives with improved efficacy and minimized resistance.

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喹诺酮类药物的发现、发展、化学性质及其耐药性综述。

喹诺酮类药物发现于20世纪70年代，由于其广谱抗菌活性，在彻底改变细菌感染的治疗方面发挥了关键作用。在过去的几十年里，人们对这些化合物进行了广泛的研究，从而开发了许多新的衍生物。本文综述了喹诺酮类药物的历史和发展，重点介绍了它们的构效关系（SAR）、作用机制以及耐药性带来的挑战。关键的耐药机制包括DNA旋切酶和拓扑异构酶IV的突变，这些突变会减少药物结合，血浆介导的机制，以及减少药物摄取或保留的染色体改变。这些机制强调需要创新方法来设计喹诺酮类药物以克服这些耐药途径。本综述还提供了对喹诺酮类药物的SAR的理解，并通过整合历史进展和当前挑战，为开发具有更高疗效和最小耐药性的下一代喹诺酮类衍生物提供了基础。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current topics in medicinal chemistry 医学-医药化学

CiteScore

6.40

自引率

2.90%

发文量

186

审稿时长

3-8 weeks

期刊介绍： Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.