Literature DB >> 19329331

Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.

Scott T Moe1, Andrew B Thompson, Genessa M Smith, Ross A Fredenburg, Ross L Stein, Alan R Jacobson.   

Abstract

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.

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Year:  2009        PMID： 19329331      PMCID： PMC2677997          DOI： 10.1016/j.bmc.2009.03.013

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  25 in total

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8.  Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.

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9.  Design and synthesis of substrate-based inhibitors of botulinum neurotoxin type B metalloprotease.

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