Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors |
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| Authors: | Shen Gang Zhu Jinge Simpson Anthony M Pei Dehua |
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| Institution: | Department of Chemistry, The Ohio State University, 100 West 18th Avenue, Columbus, OH 43210, USA. |
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| Abstract: | Macrocyclic peptidyl hydroxamates were designed, synthesized, and evaluated as peptide deformylase (PDF) inhibitors. The most potent compound exhibited tight, slow-binding inhibition of Escherichia coli PDF (K(I)(*)=4.4 nM) and had potent antibacterial activity against Gram-positive bacterium Bacillus subtilis (MIC=2-4 microg/mL). |
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