Synthesis and structure–activity relationships of second-generation hydroxamate botulinum neurotoxin a protease inhibitors

K Čapková, Y Yoneda, TJ Dickerson…

Index: Capkova, Katerina; Yoneda, Yoshiyuki; Dickerson, Tobin J.; Janda, Kim D. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 23 p. 6463 - 6466

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Citation Number: 38

Abstract

Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently identified potent lead structure, 2, 4-dichlorocinnamic acid hydroxamate, herein we report on the structure–activity relationship of a series of hydroxamate BoNT/A inhibitors. Among them, 2-bromo-4-chlorocinnamic acid hydroxamate, 2-methyl-4-chlorocinnamic acid hydroxamate, and 2-trifluoromethyl-4-chlorocinnamic acid hydroxamate displayed comparable inhibitory ...