960062-75-3Relevant academic research and scientific papers
4-Aminothiazolyl analogs of GE2270 A: Design, synthesis and evaluation of imidazole analogs
Lamarche, Matthew J.,Leeds, Jennifer A.,Dzink-Fox, Joanne,Mullin, Steve,Patane, Michael A.,Rann, Elin M.,Tiamfook, Stacey
, p. 3210 - 3215 (2011/07/07)
Imidazole analogs of the antibiotic natural product GE2270 A (1) were designed, synthesized, and evaluated for Gram positive bacteria growth inhibition. A recently reported, copper-mediated synthesis was exploited to prepare 4-thiazolyl imidazole analogs
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: Identification of the cycloalkylcarboxylic acids
Lamarche, Matthew J.,Leeds, Jennifer A.,Amaral, Kerri,Brewer, Jason T.,Bushell, Simon M.,Dewhurst, Janetta M.,Dzink-Fox, Joanne,Gangl, Eric,Goldovitz, Julie,Jain, Akash,Mullin, Steve,Neckermann, Georg,Osborne, Colin,Palestrant, Deborah,Patane, Michael A.,Rann, Elin M.,Sachdeva, Meena,Shao, Jian,Tiamfook, Stacey,Whitehead, Lewis,Yu, Donghui
, p. 8099 - 8109 (2012/01/30)
4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for their activity against Gram positive bacterial infections. Optimization efforts focused on improving the physicochemical properties (e.g., aqueous solubility and chemical stability) of the 4-aminothiazolyl natural product template while improving the in vitro and in vivo antibacterial activity. Structure-activity relationships were defined, and the solubility and efficacy profiles were improved over those of previous analogues and 1. These studies identified novel, potent, soluble, and efficacious elongation factor-Tu inhibitors, which bear cycloalkylcarboxylic acid side chains, and culminated in the selection of development candidates amide 48 and urethane 58.
EFTU INHIBITORS OR AMINOTHIAZOLES AND THEIR USES
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Page/Page column 115-118, (2008/12/08)
The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
