Title of article :
Constraining the amide bond in N-Sulfonylated dipeptide VLA-4 antagonists
Author/Authors :
Linda L. Chang، نويسنده , , Ginger X. Yang، نويسنده , , Ermengilda McCauley، نويسنده , , Richard A. Mumford، نويسنده , , John A. Schmidt، نويسنده , , William K. Hagmann، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Abstract :
The integrin VLA-4 is implicated in several inflammatory disease states. In search of non-peptidic antagonists of VLA-4, rotational constraints were imposed on the amide bond of prototypical N-sulfonylated dipeptide VLA-4 antagonists. By judicious structural modification of the side chains, trisubstituted imidazoles with moderate binding potencies were obtained, for example, 19, VLA-4 IC50 = 237 nM.
Keywords :
Peptide bond mimetic , Bicyclic VLA-4 antagonists , Imidazole VLA-4 antagonists , VLA-4
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
