Alpha-substituted hydroxamic acids as novel bacterial deformylase inhibitor-based antibacterial agents |
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| Authors: | Jain R Sundram A Lopez S Neckermann G Wu C Hackbarth C Chen D Wang W Ryder N S Weidmann B Patel D Trias J White R Yuan Z |
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| Institution: | Vicuron Pharmaceuticals (formerly Versicor Inc), 34790 Ardentech Court, Fremont, CA 94555, USA. |
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| Abstract: | 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, P(2)' and P(3)' substituents in order to achieve optimal antibacterial activity with minimal toxicity liability. |
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