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N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists
Achyutharao Sidduri1, Jefferson W Tilley, Kenneth Hull
1Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA.
Bioorganic & Medicinal Chemistry Letters
|August 6, 2002
Abstract:
A systematic structure-activity relationship investigation of the lead compound 1 resulted the identification of several N-[(substituted alkyl)cycloalkanoyl]-4-[((2,6-dichlorophenyl)carbonyl)amino]-L-phenylalanine derivatives as potent VCAM/VLA-4 antagonists. The data are consistent with a model of these compounds in which these alkanoylphenylalanines reside in a compact gauche (-) bioactive conformation.