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Peptide deformylase inhibitors with retro-amide scaffold: Synthesis and structure–activity relationships

SK Lee, KH Choi, SJ Lee, SW Suh, BM Kim…

文献索引:Lee, Seung Kyu; Choi, Kwang Hyun; Lee, Sang Jae; Suh, Se Won; Kim, B. Moon; Lee, Bong Jin Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 15 p. 4317 - 4319

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被引用次数: 12

摘要

Peptide deformylase (PDF) is a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins. Thus inhibition of PDF activity is considered to be one of the most effective antibiotic strategies. Reported herein are the synthesis and structure– activity relationship studies of retro-amide inhibitors based on actinonin, a naturally occurring PDF inhibitor. Analysis of the structure–activity relationships led to the discovery ...