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ID: ALA2380222
Journal: Bioorg Med Chem Lett
Title: Arylsulfonamide pyrimidines as VLA-4 antagonists.
Authors: Xu YZ, Konradi AW, Bard F, Dappen M, Dofiles L, Dreyer M, Gallager I, Garrido C, Krimm M, Liao Z, Messersmith E, Mutter L, Pleiss MA, Samant B, Semko CM, Smith J, Stappenbeck F, Stupi B, Vandervert C, Welch B, Wipke B, Yednock T.
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.
CiteXplore: 23562062