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Antibacterial Optimization of 4-Aminothiazolyl Analogues of the Natural Product GE2270 A: Identification of the Cycloalkylcarboxylic Acids

Lamarche, Matthew and Leeds, Jennifer and Neckermann, Georg and Osborne, Colin and Palestrant, Deborah and Patane, Michael and Raimondi, Alejandra and Rann, Elin and Sachdeva, Meena and Shao, Jian and Tiamfook, Stacey and Whitehead, Lewis and Brewer, Jason and Yu, Donghui and Amaral, Kerri and Goldovitz, Julie and Bushell, Simon and Deng, Gejing and Dewhurst, Janetta and Dzink-Fox, Joann and Gangl, Eric and Jain, Akash and Mullin, Steve (2011) Antibacterial Optimization of 4-Aminothiazolyl Analogues of the Natural Product GE2270 A: Identification of the Cycloalkylcarboxylic Acids. Journal of Medicinal Chemistry, 54 (23). pp. 8099-8109. ISSN 0022-2623

Abstract

4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A were designed, synthesized, and optimized for the treatment of Gram positive bacterial infections which culminated in the identification of development candidates 1 and 2. In support of development candidate selection, amide 1 and urethane 2 were profiled for antibacterial activity, mechanism of action, antibacterial, selectivity, solubility, formulability, in pharmacokinetic studies, and in the mouse sepsis and thigh animal models of infection. In addition, 1 and 2 were compared to marketed antibiotics used to treat Gram positive bacterial infections.

Item Type: Article
Additional Information: Accoridn to the publication plan, this manuscript will be submitted back to back with "ANTIBACTERIAL LEAD OPTIMIZATION OF 4-AMINOTHIAZOLYL ANALOGUES OF GE2270 A: THE CYCLOALKYLCARBOXYLIC ACIDS"
Keywords: GE2270 A, Curtius, elongation factor Tu, antibiotic, drug discovery, lead optimization.
Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/4555

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