1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: A Potent, Selective, and Orally Bioavailable Dipeptidyl Peptidase IV Inhibitor with Antihyperglycemic Properties

Autor:	Edwin Bernard Villhauer, Thomas Edward Hughes, John A Brinkman, Manisha Mone, Bonnie L Mangold, Mary E Russell, Goli B Naderi, Stephen Craig Weldon, Beth E. Dunning
Rok vydání:	2002
Předmět:	Male Pyrrolidines animal structures medicine.drug_class Dipeptidyl Peptidase 4 Administration Oral Biological Availability Carboxamide Chemical synthesis Dipeptidyl peptidase Rats Sprague-Dawley Structure-Activity Relationship Oral administration Nitriles Drug Discovery medicine Animals Humans Structure–activity relationship Protease Inhibitors Enzyme Inhibitors Hypolipidemic Agents chemistry.chemical_classification biology Glucose Tolerance Test Rats Bioavailability Macaca fascicularis Enzyme chemistry Biochemistry Enzyme inhibitor biology.protein Molecular Medicine Caco-2 Cells
Zdroj:	Journal of Medicinal Chemistry. 45:2362-2365
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm025522z
Popis:	Dipeptidyl peptidase IV (DPP-IV) inhibition has the potential to become a valuable therapy for type 2 diabetes. We report the first use of solid-phase synthesis in the discovery of a new DPP-IV inhibitor class and a solution-phase synthesis that is practical up to the multikilogram scale. One compound, NVP-DPP728 (2), is profiled as a potent, selective, and short-acting DPP-IV inhibitor that has excellent oral bioavailability and potent antihyperglycemic activity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1a23159d1dca769374d0d90eb53fdcb https://doi.org/10.1021/jm025522z Zobrazit plný text záznamu