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Synthesis of 2-substituted 4-quinazolone-5-carboxylic acids as inhibitors of DNA-gyrase

✍ Scribed by Zhihua Sui; Van N. Nguyen; Jeff Fernandez; John F. Barrett; Kwasi A. Ohemeng

Publisher: Journal of Heterocyclic Chemistry
Year: 1997
Tongue: English
Weight: 266 KB
Volume: 34
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.5570340124

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✦ Synopsis

Abstract

A series of 4‐quinazolone‐5‐carboxylic acids were designed as bacterial DNA gyrase inhibitors. The syntheses of the target compounds were accomplished by reacting 3‐aminophthalimide with aroyl chlorides followed by rearrangement of the resulting 3‐acylaminophthalimides under basic conditions. The designed compounds showed moderate DNA gyrase inhibitory activity.

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