Bioorganic and Medicinal Chemistry Letters p. 4223 - 4228 (2003)
Update date:2022-07-30
Topics:
Jain
Sundram
Lopez
Neckermann
Wu
Hackbarth
Chen
Wang
Ryder
Weidmann
Patel
Trias
White
Yuan
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.
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