Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists

Autor:	Marc L. Reitman, Ann E. Weber, Douglas J. MacNeil, Alison M. Strack, Liping Wang, Drew T. Weingarth, Jie Pan, Susan J. Lee, Scott D. Edmondson, Su Qian, James Hubert
Rok vydání:	2011
Předmět:	Agonist Pyrimidine Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Inhibitory Concentration 50 Mice Structure-Activity Relationship chemistry.chemical_compound Heterocyclic Compounds Drug Discovery medicine Animals Humans Structure–activity relationship Receptor Molecular Biology Cells Cultured Cholecystokinin Molecular Structure Bicyclic molecule Chemistry Organic Chemistry Amides Receptor Cholecystokinin A Pyrimidines Molecular Medicine Protein Binding
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:2911-2915
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2011.03.069
Popis:	A series of six-membered heterocycle carboxamides were synthesized and evaluated as cholecystokinin 1 receptor (CCK1R) agonists. A pyrimidine core proved to be the best heterocycle, and SAR studies resulted in the discovery of analog 5, a potent and structurally diverse CCK1R agonist.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e404299f5f1bca8802c531b821e538c https://doi.org/10.1016/j.bmcl.2011.03.069 Zobrazit plný text záznamu Full Text from ScienceDirect