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4-AMINOTHIAZOLYL ANALOGS OF GE2270 A: DESIGN, SYNTHESIS AND EVALUATION OF IMIDAZOLE ANALOGS

Lamarche, Matthew and Leeds, Jennifer and Mullin, Steve and Patane, Michael and Rann, Elin and Dzink-Fox, Joann and Tiamfook, Stacey (2011) 4-AMINOTHIAZOLYL ANALOGS OF GE2270 A: DESIGN, SYNTHESIS AND EVALUATION OF IMIDAZOLE ANALOGS. Bioorganic Medicinal Chemistry Letters, 21 (11). pp. 3210-3215. ISSN 0960-894X

Abstract

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 the 4-thiazolyl imidazole analogs of GE2270 A. The synthesis described represents a structurally complex, natural product-based application of this recently reported synthetic methodology. In addition, the biological evaluation of the imidazole-based analogs further define the SAR of the 4-aminothiazolyl-based template.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: GE2270 A, Curtius, elongation factor Tu, antibiotic, imidazole, drug discovery
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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/3896

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