Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors

被引：31

作者：

Geng, Bolin ^{[1
]}

Comita-Prevoir, Janelle ^{[1
]}

Eyermann, Charles J. ^{[1
]}

Reck, Folkert ^{[1
]}

Fisher, Stewart ^{[1
]}

机构：

[1] AstraZeneca R&D Boston, Infect Innovat Med, Waltham, MA 02451 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 18期

关键词：

Antibacterials; 4-Amino-piperidines; DNA gyrase; Topoisomerase IV; Type IIa topoisomerases; ANTIBACTERIAL DISCOVERY; CHALLENGES; DRUGS; DNA;

D O I：

10.1016/j.bmcl.2011.06.126

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5432 / 5435

页数：4

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