Arylsulfonamide pyrimidines as VLA-4 antagonists

Autor:	Jennifer S. Smith, Michael A. Pleiss, Caroline Garrido, Ying-Zi Xu, Frank Stappenbeck, Elizabeth Messersmith, Frederique Bard, Bhushan Samant, Linda Mutter, Semko Christopher M, Brent Welch, Brian P. Stupi, Chris Vandervert, Mark Dreyer, Zhenmei Liao, Mike Krimm, Brian Wipke, Ian Gallager, Ted Yednock, Michael S. Dappen, Andrei W. Konradi, Lilibeth Dofiles
Rok vydání:	2013
Předmět:	Models Molecular Multiple Sclerosis Stereochemistry Clinical Biochemistry Molecular Conformation Pharmaceutical Science Integrin alpha4beta1 Biochemistry Rats Sprague-Dawley Mice Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Cell Adhesion Animals Humans Structure–activity relationship Collagen Type II Molecular Biology Sulfonamides Dose-Response Relationship Drug Chemistry Organic Chemistry Antagonist VLA-4 Arthritis Experimental Asthma In vitro Fibronectins Rats Mice Inbred C57BL Sprague dawley Disease Models Animal Pyrimidines Propanoic acid Rats Inbred Lew Antirheumatic Agents Molecular Medicine Female Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 23:3070-3074
ISSN:	0960-894X
Popis:	A series of (S)-2-(2-(diethylamino)-5-(N-alkyl-N-sulfonamido)pyrimidin-4-ylamino)-3-(4-(carbamoyloxy)phenyl)propanoic acid is discovered as orally available VLA-4 antagonists. Representative compounds 11b and 11p showed efficacy in multiple in vivo animal models. The in vitro selectivity of 11p is also described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95f333c01a36b2c1dca73c9d1c52f995 https://doi.org/10.1016/j.bmcl.2013.03.010 Zobrazit plný text záznamu Full Text from ScienceDirect