Botulinum neurotoxin serotype A inhibitors: Small-molecule mercaptoacetamide analogs
Botulinum neurotoxin serotype A inhibitors: Small-molecule mercaptoacetamide analogs
复制标题
DOI：
10.1016/j.bmc.2009.03.013
复制
发表时间：
2009-04-15
影响因子：
3.5
通讯作者：
Jacobson, Alan R.
中科院分区：
文献类型：
--
作者：
Moe, Scott T.;Thompson, Andrew B.;Jacobson, Alan R.
Botulinum neurotoxin elicits its paralytic activity through a zinc-dependant metalloprotease that cleaves proteins involved in neurotransmitter release. Currently, no drugs are available to reverse the effects of botulinum intoxication. Herein we report the design of a novel series of mercaptoacetamide small-molecule inhibitors active against botulinum neurotoxin serotype A. These analogs show low micromolar inhibitory activity against the isolated enzyme. Structure-activity relationship studies for a series of mercaptoacetamide analogs of 5-amino-3-phenylpyrazole reveal components essential for potent inhibitory activity. (C) 2009 Elsevier Ltd. All rights reserved.
