化学
肉毒神经毒素
神经毒素
立体化学
蛋白酶
结构-活动关系
生物化学
酶抑制剂
三氟甲基
酶
抑制性突触后电位
体外
毒素
有机化学
神经科学
烷基
生物
作者
Kateřina Čapková,Yasuko Yoneda,Tobin J. Dickerson,Kim D. Janda
标识
DOI:10.1016/j.bmcl.2007.09.103
摘要
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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