4-Aminothiazolyl analogs of GE2270 A: design, synthesis and evaluation of imidazole analogs |
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Authors: | LaMarche Matthew J Leeds Jennifer A Dzink-Fox JoAnne Mullin Steve Patane Michael A Rann Elin M Tiamfook Stacey |
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Affiliation: | a Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA b Infectious Disease Area, Novartis Institutes for Biomedical Research, Cambridge, MA 02139, USA |
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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 4-thiazolyl imidazole analogs of 1. 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 antibacterial template. |
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Keywords: | MIC, minimum inhibitory concentration G+, gram positive MRSA, methicillin resistant staphylococci VRE, vancomycin resistant enterococci S. aureus, Staphylococcus aureus E. faecalis, Enterrococcus faecalis E. faecium, Enterococcus faecium S. pyogenes, Streptococcus pyogenes EF-Tu, elongation factor Tu |
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