发现基于氨基哌啶的具有广谱抗菌活性的新型强效拓扑异构酶抑制剂。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-07-26 DOI:10.1016/j.bmcl.2024.129911

Jigar Desai, Bhaumin Patel, Nandini Panchal, Archana Gite, Brijesh Darji, Kasinath Viswanathan, Jinal Trivedi, Purvi Vyas, Vishwanath Pawar, Poonam Giri, Sachchidanand S, Rajiv Sharma, Mukul Jain, Pravin Iyer, Sanjay Kumar

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引用次数: 0

摘要

抑制细菌 DNA 回旋酶和拓扑异构酶 IV 已成为治疗抗生素耐药细菌感染的一种有前途的策略。新型细菌拓扑异构酶抑制剂（NBTIs）与喹诺酮类药物的作用点不同，具有新的作用机制。这就避免了与喹诺酮类药物相关的由靶点介导的细菌耐药性。本文介绍了我们在体外鉴定强效广谱抗菌剂 4l 方面所做的努力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Discovery of aminopiperidine based potent & novel topoisomerase inhibitor with broad spectrum anti-bacterial activity

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Discovery of aminopiperidine based potent & novel topoisomerase inhibitor with broad spectrum anti-bacterial activity

Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria. The Novel Bacterial Topoisomerase Inhibitors (NBTIs) bind to a different site from that of the quinolones with novel mechanism of action. This evades the existing target-mediated bacterial resistance associated with quinolones. This article presents our efforts to identify in vitro potent and broad-spectrum antibacterial agent 4l.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.