Nitrogen-Containing Heterocycles in Antibacterial Drug Discovery: Recent Advances and Structure-Activity Relationships.

IF 2.5 4区 医学 Q3 CHEMISTRY, MEDICINAL
Xiaoqing Zhu, Ping Zhang, Xueyu Wang, Meiran Jiao, Hui Sun, Bin Cui
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引用次数: 0

Abstract

Antibiotic resistance has become a major global public health challenge, creating an urgent need for the development of new antimicrobial agents. This article reviews the latest research on nitrogen-heterocyclic antimicrobial agents, including pyrazole, imidazole, triazole, thiazole, indole, and quinolone. The article analyzes synthetic strategies, antibacterial activities, and structure-activity relationships for various derivatives. Eight key antibacterial scaffolds, namely compounds 21aa, 30a, 40, 63S, 91, 105, 123, and 127a, were identified as exhibiting outstanding performance. Future research should focus on evaluating the in vivo pharmacodynamics, pharmacokinetics, clinical translation challenges, and safety of these key antibacterial scaffolds, thereby promoting the clinical translation of nitrogen-heterocyclic antibacterial candidate drugs.

含氮杂环类抗菌药物的发现:最新进展及构效关系。
抗生素耐药性已成为一项重大的全球公共卫生挑战,迫切需要开发新的抗微生物药物。本文综述了吡唑、咪唑、三唑、噻唑、吲哚和喹诺酮类氮杂环类抗菌药物的最新研究进展。本文分析了各种衍生物的合成策略、抗菌活性和构效关系。8个关键抗菌支架,即化合物21aa、30a、40、63S、91、105、123和127a表现优异。未来的研究应重点评价这些关键抗菌支架的体内药效学、药代动力学、临床翻译挑战和安全性,从而促进氮杂环抗菌候选药物的临床翻译。
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
Medicinal Chemistry
Medicinal Chemistry 医学-医药化学
CiteScore
4.30
自引率
4.30%
发文量
109
审稿时长
12 months
期刊介绍: Aims & Scope Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.
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