Abstract
The SAR of 1-sulfonyl-cyclopentyl carboxylic acid amides, ligands for the VLA-4 integrin, was investigated. This effort resulted in the identification of N-(3-phenylsulfonyl-3-piperidinoyl)-( l)-4-(2′,6′-dimethoxyphenyl)phenylalanine 52 as a potent, selective VLA-4 antagonist (IC 50=90 pM). Expansion of the SAR demonstrated that this structural unit can be used to identify a diverse series of sub-nanomolar antagonists.
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