Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377123 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Linda L. Chang, Ginger X. Yang, Ermengilda McCauley, Richard A. Mumford, John A. Schmidt, William K. Hagmann,