1.
Bioorg Med Chem Lett
; 25(22): 5291-4, 2015 Nov 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26433449
RESUMO
The design and synthesis of two conformationally restricted oxazabicyclo octane derivatives as GRP119 agonists is described. Derivatives of scaffold C, with syn configuration, have the best overall profiles with respect to solubility and in vivo efficacy. Compound 25a was found to have extremely potent agonistic activity and was orally active in lowering blood glucose levels in a mouse oral glucose tolerance test at a dose of 0.1 mg/kg.