4-Aminothiazolyl Analogues of GE2270 A: Antibacterial Lead Finding

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• 作者：Matthew J. LaMarche ; Jennifer A. Leeds ; JoAnne Dzink-Fox ; Karl Gunderson ; Philipp Krastel ; Klaus Memmert ; Michael A. Patane ; Elin M. Rann ; Esther Schmitt ; Stacey Tiamfook ; Bing Wang
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：April 14, 2011
• 年：2011
• 卷：54
• 期：7
• 页码：2517-2521
• 全文大小：858K
• 年卷期：v.54,no.7(April 14, 2011)
• ISSN：1520-4804

文摘

4-Aminothiazolyl analogues of the antibacterial natural product GE2270 A (1) were designed, synthesized, and evaluated for Gram positive bacteria growth inhibition. The aminothiazole-based chemical template was evaluated for chemical stability, and its decomposition revealed a novel, structurally simplified, des-thiazole analogue of 1. Subsequent stabilization of the 4-aminothiazolyl functional motif was achieved and initial structure activity relationships defined.