Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.
Bioorg Med Chem
; 17(8): 3072-9, 2009 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-19329331
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antitoxina Botulínica
/
Toxinas Botulínicas Tipo A
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article