Arylsulfonamide pyrimidines as VLA-4 antagonists.

Bioorganic & Medicinal Chemistry Letters(2013)

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摘要
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.
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关键词
α4β1,VLA-4,Antagonist,Orally available,CIA model,EAE model
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