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
de 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.
Recherche sur Google
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Phénéthylamines
/
Pipéridines
/
Glycoprotéines
/
Inhibiteurs de la dipeptidyl-peptidase IV
/
Inhibiteurs de l'adénosine désaminase
Limites:
Animals
/
Humans
Langue:
En
Journal:
J Med Chem
Sujet du journal:
QUIMICA
Année:
2007
Type de document:
Article
Pays d'affiliation:
États-Unis d'Amérique