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ANTIBACTERIAL LEAD OPTIMIZATION OF 4-AMINOTHIAZOLYL ANALOGUES OF GE2270 A: THE CYCLOALKYLCARBOXYLIC ACIDS

Lamarche, Matthew and Leeds, Jennifer and Brewer, Jason and Bushell, Simon and Dewhurst, Janetta and Jain, Akash and Mullin, Steve and Neckermann, Georg and Palestrant, Deborah and Patane, Michael and Rann, Elin and Sachdeva, Meena and Shao, Jian and Whitehead, Lewis and Tiamfook, Stacey and Yu, Donghui (2011) ANTIBACTERIAL LEAD OPTIMIZATION OF 4-AMINOTHIAZOLYL ANALOGUES OF GE2270 A: THE CYCLOALKYLCARBOXYLIC ACIDS. Journal of Medicinal Chemistry, 54 (7). pp. 2517-2521. ISSN 0022-2623

Abstract

4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for the treatment of Gram positive bacterial infections. Lead optimization efforts of the 4-aminothiazolyl natural product template focused on improving aqueous solubility while maintaining in vitro and in vivo antibacterial activity. Structure-activity relationships were defined, and the solubility and efficacy profiles were improved. These studies culminated in the identification of the cycloalkyl-carboxylic acid class of EF-Tu inhibitors, and development candidates amide 48 and urethane 58.

Item Type: Article
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Additional Information: archiving not formally supported by this publisher
Keywords: GE2270 A, Curtius, elongation factor Tu, antibiotic, drug discovery, lead optimization.
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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/4553

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