Author/Authors :
Clare E. Gutteridge، نويسنده , , Stephen E. de Laszlo، نويسنده , , Theodore M. Kamenecka، نويسنده , , Ermengilda McCauley، نويسنده , , Gail Van Riper، نويسنده , , Richard A. Mumford، نويسنده , , Usha Kidambi، نويسنده , , Linda A. Egger، نويسنده , , Sharon Tong، نويسنده , , William K. Hagmann، نويسنده ,
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)-( )-4-(2′,6′-dimethoxyphenyl)phenylalanine 52 as a potent, selective VLA-4 antagonist (IC50=90 pM). Expansion of the SAR demonstrated that this structural unit can be used to identify a diverse series of sub-nanomolar antagonists.
