327618-72-4Relevant articles and documents
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists
Doherty, George A.,Yang, Ginger X.,Borges, Edite,Chang, Linda L.,MacCoss, Malcolm,Tong, Sharon,Kidambi, Usha,Egger, Linda A.,McCauley, Ermenegilda,Van Riper, Gail,Mumford, Richard A.,Schmidt, John A.,Hagmann, William K.
, p. 1501 - 1505 (2002)
A series of substituted tetrahydrofuroyl-1-phenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. Substitution of the α carbon of the tetrahydrofuran with aryl groups increased the specificity for VLA-4 versus α4β7 while amide substitution increased the potency of the series without increasing the specificity. Substitution of the β carbon of the tetrahydrofuran with keto or amino groups slightly improved the specificity for VLA-4 versus α4β7 but with a significant loss in binding affinity for VLA-4.
