Structure-based design, synthesis, and antimicrobial activity of indazole-derived SAH/MTA nucleosidase inhibitors.
J Med Chem
; 46(26): 5663-73, 2003 Dec 18.
Article
em En
| MEDLINE
| ID: mdl-14667220
ABSTRACT
The structure-based design, synthesis, and biological activity of a novel indazole-containing inhibitor series for S-adenosyl homocysteine/methylthioadenosine (SAH/MTA) nucleosidase are described. Use of 5-aminoindazole as the core scaffold provided a structure-guided series of low nanomolar inhibitors with broad-spectrum antimicrobial activity. The implementation of structure-based methodologies provided a 6000-fold increase in potency over a short timeline (several months) and an economy of synthesized compounds.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sulfonamidas
/
Indazóis
/
Antibacterianos
/
N-Glicosil Hidrolases
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article