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ANTIBACTERIAL OPTIMIZATION OF 4-AMINOTHIAZOLYL ANALOGUES OF THE NATURAL PRODUCT GE2270 A: IDENTIFICATION OF THE CYCLOALKYLCARBOXYLIC ACIDS.
MedLine Citation:
PMID:  21999529     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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 that of previous analogs and GE2270 A. These studies identified novel, potent, soluble, and efficacious elongation factor-Tu inhibitors, which bear cycloalkyl-carboxylic acid sidechains, and culminated in the selection of development candidates amide 48 and urethane 58.
Authors:
Matthew J Lamarche; Jennifer Leeds; Kerri Amaral; Jason Brewer; Simon Bushell; Janetta Dewhurst; Joanne Dzink-Fox; Eric Gangl; Julie Goldovitz; Akash Jain; Steve Mullin; Georg Neckermann; Colin Osborn; Deborah Palestrant; Michael Patane; Elin Rann; Meena Sachdeva; Jian Shao; Stacey Tiamfook; Lewis Whitehead; Donghui Yu
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-10-14
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  -     Publication Date:  2011 Oct 
Date Detail:
Created Date:  2011-10-17     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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