Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors.
Bioorg Med Chem Lett
; 24(13): 2802-6, 2014 Jul 01.
Article
en En
| MEDLINE
| ID: mdl-24835199
ABSTRACT
Human acrosin is an attractive target for the discovery of novel male contraceptives. Isoxazole derivative ISO-1, a small-molecule weak human acrosin inhibitor, was used as the starting point for lead optimization. After two rounds of structure-based inhibitor design, a highly potent inhibitor B6 (IC50=1.44 µM) was successfully identified, which showed good selectivity over trypsin and represents one of the most active human acrosin inhibitors up to date.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Acrosina
/
Diseño de Fármacos
/
Isoxazoles
Límite:
Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2014
Tipo del documento:
Article
País de afiliación:
China