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

被引：0
作者：
Desai, Jigar [2 ]
Patel, Bhaumin
Panchal, Nandini
Gite, Archana
Darji, Brijesh
Viswanathan, Kasinath
Trivedi, Jinal
Vyas, Purvi
Pawar, Vishwanath
Giri, Poonam
Sachchidanand, S.
Sharma, Rajiv
Jain, Mukul
Iyer, Pravin
Kumar, Sanjay [1 ]
机构：
[1] Zydus Res Ctr, Sarkhej Bavla NH 8A Moraiya, Ahmadabad 382210, Gujarat, India
[2] Birla Inst Technol & Sci Pilani, K K Birla Goa Campus, Zuarinagar 403726, Goa, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2024年 / 111卷
基金：
美国国家卫生研究院;
关键词：
DNA gyrase; MIC; NBTI; Topoisomerase;
D O I：
10.1016/j.bmcl.2024.129911
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria. The N ovel B acterial T opoisomerase I nhibitors (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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页数：6
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