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Arylsulfonamide pyrimidines as VLA-4 antagonists.
Xu, Ying-Zi; Konradi, Andrei W; Bard, Frederique; Dappen, Michael; Dofiles, Lilibeth; Dreyer, Mark; Gallager, Ian; Garrido, Caroline; Krimm, Mike; Liao, Zhenmei; Messersmith, Elizabeth; Mutter, Linda; Pleiss, Michael A; Samant, Bhushan; Semko, Christopher M; Smith, Jennifer; Stappenbeck, Frank; Stupi, Brian; Vandervert, Chris; Welch, Brent; Wipke, Brian; Yednock, Ted.
Bioorg Med Chem Lett ; 23(10): 3070-4, 2013 May 15.
Article in English | MEDLINE | ID: mdl-23562062

ABSTRACT

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.


Subject(s)
Antirheumatic Agents/pharmacology , Integrin alpha4beta1/antagonists & inhibitors , Pyrimidines/pharmacology , Sulfonamides/pharmacology , Animals , Antirheumatic Agents/administration & dosage , Antirheumatic Agents/chemical synthesis , Arthritis, Experimental/drug therapy , Asthma/drug therapy , Cell Adhesion/drug effects , Collagen Type II/antagonists & inhibitors , Disease Models, Animal , Dose-Response Relationship, Drug , Female , Fibronectins/chemistry , Humans , Mice , Mice, Inbred C57BL , Models, Molecular , Molecular Conformation , Multiple Sclerosis/drug therapy , Pyrimidines/administration & dosage , Pyrimidines/chemical synthesis , Rats , Rats, Inbred Lew , Rats, Sprague-Dawley , Structure-Activity Relationship , Sulfonamides/administration & dosage , Sulfonamides/chemical synthesis
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