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Updated: Jun 3, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Novel 3-chlorooxazolidin-2-ones as antimicrobial agents
Timothy P Shiau1, Eric D Turtle, Charles Francavilla
1Novabay Pharmaceuticals, 5980 Horton St. Suite 550, Emeryville, CA 94608, USA.
Abstract:
Antimicrobial resistance against many known therapeutics is on the rise. We examined derivatives of 3-chlorooxazolidin-2-one 1a (X=H) as antibacterial and antifungal agents. The key findings were that the activity and apparent in vitro cytotoxicity could be controlled by the substitution of charged solubilizers at the 4- and 5- positions. These changes both significantly increase the antifungal potency and decrease cytotoxicity. Particularly effective were trialkylammonium groups which led to 400- to 600-fold increases in the antifungal therapeutic index when compared to their unsubstituted counterparts.
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