Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.
Bioorg Med Chem Lett
; 17(7): 1903-7, 2007 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-17291750
ABSTRACT
Following the discovery of N-acyl-1,4-diazepan-2-one as a novel pharmacophore for potent and selective DPP-4 inhibitors, optimization of this new lead with different substitution on the seven-membered ring resulted in several highly potent and selective, orally bioavailable, and efficacious DPP-4 inhibitors, such as 3R-methyl-1-cyclopropyl-1,4-diazepan-2-one derivative 9i (DPP-4 IC(50)=8.0 nM) and 3R,6R-dimethyl-1,4-diazepan-2-one derivative 14a (DPP-4 IC(50)=9.7 nM).
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Azepinas
/
Química Farmacêutica
/
Diabetes Mellitus Tipo 2
/
Inibidores Enzimáticos
/
Inibidores da Dipeptidil Peptidase IV
Limite:
Animals
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article