Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors
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- 作者：Jing Zhang ; Qingyi Yang ; Jan Antoinette C. Romero ; Jason Cross ; Bin Wang ; Katherine M. Poutsiaka ; Felix Epie ; Douglas Bevan ; Yuchuan Wu ; Terence Moy ; Anu Daniel ; Brian Chamberlain ; Nicole Carter ; Joseph Shotwell ; Anu Arya ; Vipul Kumar ; Jared Silverman ; Kien Nguyen ; Chester A. Metcalf ; III ; Dominic Ryan ; Blaise Lippa ; Roland E. Dolle
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2015
- 出版时间：October 8, 2015
- 年：2015
- 卷：6
- 期：10
- 页码：1080-1085
- 全文大小：442K
- ISSN：1948-5875
文摘
Antibacterials with a novel mechanism of action offer a great opportunity to combat widespread antimicrobial resistance. Bacterial DNA Gyrase is a clinically validated target. Through physiochemical property optimization of a pyrazolopyridone hit, a novel class of GyrB inhibitors were discovered. Guided by structure-based drug design, indazole derivatives with excellent enzymatic and antibacterial activity as well as great animal efficacy were discovered.