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N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists |
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| Authors: | Sidduri Achyutharao Tilley Jefferson W Hull Kenneth Lou Jian Ping Kaplan Gerry Sheffron Allen Chen Li Campbell Robert Guthrie Robert Huang Tai-Nan Huby Nicholas Rowan Karen Schwinge Virginia Renzetti Louis M |
| Affiliation: | Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. |
| 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. |
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