Title of article
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists
Author/Authors
George A. Doherty، نويسنده , , Ginger X. Yang، نويسنده , , Edite Borges، نويسنده , , Linda L. Chang، نويسنده , , Malcolm MacCoss، نويسنده , , Sharon Tong، نويسنده , , Usha Kidambi، نويسنده , , Linda A. Egger، نويسنده , , Ermenegilda McCauley، نويسنده , , Gail Van Riper، نويسنده , , Richard A. Mumford، نويسنده , , John A. Schmidt، نويسنده , , William K. Hagmann، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
5
From page
1501
To page
1505
Abstract
A series of substituted tetrahydrofuroyl-1-phenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. Substitution of the α carbon of the tetrahydrofuran with aryl groups increased the specificity for VLA-4 versus α4β7 while amide substitution increased the potency of the series without increasing the specificity. Substitution of the β carbon of the tetrahydrofuran with keto or amino groups slightly improved the specificity for VLA-4 versus α4β7 but with a significant loss in binding affinity for VLA-4.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792247
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