1141402-00-7Relevant academic research and scientific papers
Botulinum neurotoxin serotype A inhibitors: Small-molecule mercaptoacetamide analogs
Moe, Scott T.,Thompson, Andrew B.,Smith, Genessa M.,Fredenburg, Ross A.,Stein, Ross L.,Jacobson, Alan R.
experimental part, p. 3072 - 3079 (2009/09/25)
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.
