2-Arylpyrimidines: Novel CRF-1 receptor antagonists

Autor:	Jayaraman Chandrasekhar, Raymond F. Horvath, Ping Ge, Stéphane De Lombaert, Hutchison Alan J, Kevin J. Hodgetts, Dario Doller, Robbin Brodbeck, James E. Krause, Diane Hoffman, Michael Gulianello, Yoon Taeyoung, John H. Kehne
Rok vydání:	2008
Předmět:	Pyrimidine Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Ether Receptors Corticotropin-Releasing Hormone Biochemistry Chemical synthesis Rats Sprague-Dawley Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Animals Humans Receptor Molecular Biology Binding Sites Molecular Structure Organic Chemistry Antagonist In vitro Rats Kinetics Pyrimidines Models Chemical Solubility chemistry Drug Design Lipophilicity Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:4486-4490
ISSN:	0960-894X
Popis:	The design, synthesis and structure-activity relationship studies of a novel series of CRF-1 receptor antagonists, the 2-arylpyrimidines, are described. The effects of substitution on the aromatic ring and the pyrimidine core on CRF-1 receptor binding were investigated. A number of compounds with K(i) values below 10 nM and lipophilicity in a minimally acceptable range for a CNS drug (cLogP5) were discovered.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e03715e3452d8f911694815b9df50eb https://doi.org/10.1016/j.bmcl.2008.07.063 Zobrazit plný text záznamu Full Text from ScienceDirect