Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Bioorg Med Chem Lett
; 20(3): 1109-13, 2010 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-20031405
ABSTRACT
Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin (8p), was chosen for clinical development. Its X-ray structure in complex with the enzyme and early efficacy data in animal models of type 2 diabetes are also presented.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinolizinas
/
Desenho de Fármacos
/
Diabetes Mellitus Tipo 2
/
Inibidores da Dipeptidil Peptidase IV
/
Hipoglicemiantes
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article