α-Substituted hydroxamic acids as novel bacterial deformylase inhibitor-based antibacterial agents

…, S Lopez, G Neckermann, C Wu, C Hackbarth…

文献索引：Jain; Sundram; Lopez; Neckermann; Wu; Hackbarth; Chen; Wang; Ryder; Weidmann; Patel; Trias; White; Yuan Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 23 p. 4223 - 4228

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被引用次数: 45

摘要

We report the synthesis and biological activity of analogues of VRC3375 (N-hydroxy-3-R- butyl-3-[(2-S-(tert-butoxycarbonyl)-pyrrolidin-1-ylcarbonyl] propionamide), an orally active peptide deformylase inhibitor. This study explores the structure–activity relationship of various chelator groups, alpha substituents, P2′ and P3′ substituents in order to achieve optimal antibacterial activity with minimal toxicity liability.