Highly constrained bicyclic VLA-4 antagonists.

Linda L Chang,Quang Truong,George A Doss,Malcolm MacCoss,Kathryn Lyons,Ermengilda McCauley,Richard Mumford,Gail Forrest,Stella Vincent,John A Schmidt,William K Hagmann

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

VLA-4 antagonists containing a bicyclic β-amino acid were studied. Activity was found to be related to the P3-amino-carboxy dihedral angle in the bicycle. The best compound, 5m, had VLA-4 IC50 of 54nM and a 49% bioavailability in the rat at 2mpk.

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关键词

VLA-4 antagonists,Integrin,α4β1,Anti-inflammatory,Autoimmune,β-Amino acid,Conformational restriction,Bioavailable,Bicyclic

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