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Substituted N-(3,5-Dichlorobenzenesulfonyl)-l-prolyl-phenylalanine analogues as potent VLA-4 antagonists

Authors :
Plato A. Magriotis
John A. Schmidt
Stella H. Vincent
Junying Wang
Linus S. Lin
Dorothy Levorse
Sharon Tong
Zhen Wang
Linda E Egger
Ihor E. Kopka
Richard A. Mumford
Sander G. Mills
William K. Hagmann
Ralph A. Stearns
David N. Young
Malcolm MacCoss
Usha Kidambi
Ermengilda McCauley
Kathryn A. Lyons
Karen Owens
Gail Van Riper
Song Zheng
Adria Colletti
Source :
Bioorganic & Medicinal Chemistry Letters. 12:637-640
Publication Year :
2002
Publisher :
Elsevier BV, 2002.

Abstract

A series of substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl- and alpha-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 approximately 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.

Details

ISSN :
0960894X
Volume :
12
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....63055d86099dad6304a5f734a44d503d
Full Text :
https://doi.org/10.1016/s0960-894x(01)00821-6