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Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists

Doherty, George A ; Yang, Ginger X ; Borges, Edite ; Chang, Linda L ; Maccoss, Malcolm ; Tong, Sharon ; Kidambi, Usha ; Egger, Linda A ; Mccauley, Ermenegilda ; Van Riper, Gail ; Mumford, Richard A ; Schmidt, John A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(11), pp.1501-1505 [Peer Reviewed Journal]

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  • Title:
    Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists
  • Author: Doherty, George A ; Yang, Ginger X ; Borges, Edite ; Chang, Linda L ; Maccoss, Malcolm ; Tong, Sharon ; Kidambi, Usha ; Egger, Linda A ; Mccauley, Ermenegilda ; Van Riper, Gail ; Mumford, Richard A ; Schmidt, John A ; Hagmann, William K
  • Description: 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 α 4β 7 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 α 4β 7 but with a significant loss in binding affinity for VLA-4. 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 α 4β 7 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...
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(11), pp.1501-1505
  • Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/S0960-894X(02)00211-1
  • Subjects: Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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