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2007:
Capková Katerina; Yoneda Yoshiyuki; Dickerson Tobin J; Janda Kim D
Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.
Bioorganic & medicinal chemistry letters 2007;
17(
23):.
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 activity to that of the lead structure.
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