N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.

Achyutharao Sidduri,Jefferson W Tilley, Kenneth Hull,Jian Ping Lou,Gerry Kaplan, Allen Sheffron,Li Chen,Robert Campbell,Robert Guthrie,Tai-Nan Huang,Nicholas Huby,Karen Rowan,Virginia Schwinge,Louis M Renzetti

Bioorganic & medicinal chemistry letters（2002）

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摘要

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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关键词

cheminform abstract,n-cycloalkanoyl-l-phenylalanine

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