Design, synthesis and insulin-sensitising effects of novel PTP1B inhibitors.
Bioorg Med Chem Lett
; 23(8): 2313-8, 2013 Apr 15.
Article
en En
| MEDLINE
| ID: mdl-23499238
ABSTRACT
Fifteen novel sulfathiazole-related compounds were designed as PTP1B inhibitors based on a previously reported allosteric inhibitor (1) of PTP1B. These compounds were synthesized and evaluated against human recombinant PTP1B. Six compounds (3, 4, 8 and 14-16) exhibited significant inhibitory activity against PTP1B. The most active compound (16) showed IC50 value of 3.2 µM and kinetic analysis indicated that it is a non-competitive inhibitor of PTP1B. Furthermore, compound 16 demonstrated excellent selectivity to PTP1B over other PTPs. It also displayed in vivo insulin sensitizing effect in the insulin resistant mice.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Sulfatiazoles
/
Inhibidores Enzimáticos
/
Proteína Tirosina Fosfatasa no Receptora Tipo 1
Límite:
Animals
/
Humans
Idioma:
En
Año:
2013
Tipo del documento:
Article