Synthesis and structure–activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists

Autor:	Kingsley H. Nelson, Lynne E. Ozgur, Laura L. Rokosz, Adriane E. Schilling, Taveras Arthur G, Wei Wang, Kaiser Bernd, Ge Li, Chao Jianping, Tara M. Stauffer, J. Robert Merritt, Baldwin John J, Michael P. Dwyer
Rok vydání:	2006
Předmět:	medicine.drug_class Stereochemistry Clinical Biochemistry Administration Oral Biological Availability Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Receptors Interleukin-8B Structure-Activity Relationship Drug Discovery medicine Humans Structure–activity relationship Molecular Biology Ene reaction Chemotype Chemistry Organic Chemistry Chemotaxis Bioavailability Microsomes Liver Microsome Molecular Medicine Caco-2 Cells Cyclobutanes
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:4107-4110
ISSN:	0960-894X
Popis:	A novel series of 3,4-diaminocyclobut-3-ene-1,2-diones was prepared and found to show potent inhibitory activity of CXCR2 binding and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Microsome stability and Caco2 studies were subsequently used to show that compounds of this chemotype are predicted to have good oral bioavailability and are thus suitable for pharmaceutical development.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0652277caad793e3c206100797dfcfa4 https://doi.org/10.1016/j.bmcl.2006.04.082 Zobrazit plný text záznamu Full Text from ScienceDirect