| Autor: |
Hu, X., Nguyen, K. T., Verlinde, C. L. M. J., Hol, W. G. J., Pei, D. |
| Zdroj: |
Journal of Medicinal Chemistry; August 2003, Vol. 46 Issue: 18 p3771-3774, 4p |
| Abstrakt: |
A macrocyclic, peptidomimetic inhibitor of peptide deformylase was designed by covalently cross-linking the P1 and P3 side chains. The macrocycle, which contains an N-formylhydroxylamine side chain as the metal-chelating group, was synthesized from a diene precursor via olefin metathesis using Grubbs's catalyst. The cyclic inhibitor showed potent inhibitory activity toward Escherichia coli deformylase (KI = 0.67 nM) and antibacterial activity against both Gram-positive and Gram-negative bacteria (MIC = 0.7−12 μg/mL). |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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