217452-76-1Relevant articles and documents
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists
Kopka, Ihor E,Young, David N,Lin, Linus S,Mumford, Richard A,Magriotis, Plato A,MacCoss, Malcolm,Mills, Sander G,Riper, Gail Van,McCauley, Ermengilda,Egger, Linda E,Kidambi, Usha,Schmidt, John A,Lyons, Kathryn,Stearns, Ralph,Vincent, Stella,Colletti, Adria,Wang, Zhen,Tong, Sharon,Wang, Junying,Zheng, Song,Owens, Karen,Levorse, Dorothy,Hagmann, William K
, p. 637 - 640 (2002)
A series of substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl- and α-methyl-L-prolyl-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. The compounds showed excellent potency with a wide variety of neutral, polar, electron withdrawing or donating groups on the phenylalanine ring (IC50～1 nM). Heteroaryl ring substitution for phenylalanine was also well tolerated. Pharmacokinetic studies in rat were performed on a representative set of compounds in both series.
