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

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

Index: 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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Citation Number: 12

Abstract

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 ...