Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
J Med Chem
; 50(8): 1983-7, 2007 Apr 19.
Article
em En
| MEDLINE
| ID: mdl-17367123
ABSTRACT
Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent insulinotropic peptide, which are two important incretins for glucose homeostasis. Starting from a high-throughput screening hit, we were able to identify a series of piperidinone- and piperidine-constrained phenethylamines as novel DPP4 inhibitors. Optimized compounds are potent, selective, and have good pharmacokinetic profiles.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fenetilaminas
/
Piperidinas
/
Glicoproteínas
/
Inibidores da Dipeptidil Peptidase IV
/
Inibidores de Adenosina Desaminase
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article