| ANTIBACTERIAL OPTIMIZATION OF 4-AMINOTHIAZOLYL ANALOGUES OF THE NATURAL PRODUCT GE2270 A: IDENTIFICATION OF THE CYCLOALKYLCARBOXYLIC ACIDS. | |
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MedLine Citation:
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PMID: 21999529 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: JOURNAL ARTICLE Date: 2011-10-14 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: - ISSN: 1520-4804 ISO Abbreviation: - Publication Date: 2011 Oct |
Date Detail:
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Created Date: 2011-10-17 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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