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Macrocyclic inhibitors for peptide deformylase: a structure-activity relationship study of the ring size

X Hu, KT Nguyen, VC Jiang, D Lofland…

文献索引:Hu, Xubo; Nguyen, Kiet T.; Jiang, Vernon C.; Lofland, Denene; Moser, Heinz E.; Pei, Dehua Journal of Medicinal Chemistry, 2004 , vol. 47, # 20 p. 4941 - 4949

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被引用次数: 53

摘要

Peptide deformylase (PDF) catalyzes the removal of the N-terminal formyl group from newly synthesized polypeptides in eubacteria. Its essential role in bacterial cells but not in mammalian cells makes it an attractive target for antibacterial drug design. We have previously reported an N-formylhydroxylamine-based, metal-chelating macrocyclic PDF inhibitor, in which the P1'and P3'side chains are covalently joined. In this work, we have ...