Substituted dipiperidine alcohols as potent CCR2 antagonists

Autor:	James Brackley, Monica Singer, Cuifen Hou, Michael P. Wachter, Druie Cavender, Michele Matheis, Mingde Xia, Meng Pan, Scott R. Pollack, Demong Duane E
Rok vydání:	2008
Předmět:	Receptors CCR2 medicine.drug_class Stereochemistry Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Carboxamide Stereoisomerism Primary alcohol Biochemistry Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Piperidines Drug Discovery medicine Humans Structure–activity relationship Binding site Molecular Biology Binding Sites Molecular Structure Bicyclic molecule Organic Chemistry In vitro chemistry Alcohols Urea Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:3562-3564
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.05.010
Popis:	The synthesis and biological evaluation of a series of substituted dipiperidine alcohols are described. Structure-activity relationship studies led to the discovery of potent CCR2 antagonists displaying IC(50) values in the nanomolar or subnanomolar range. The cinnamoyl compounds had higher binding affinities than the corresponding urea analogs.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e084a0c77db0c8f8366185d0b2ba1c3 https://doi.org/10.1016/j.bmcl.2008.05.010 Zobrazit plný text záznamu Full Text from ScienceDirect