| Literature DB >> 18242984 |
Linda L Chang1, Ginger X Yang, Ermengilda McCauley, Richard A Mumford, John A Schmidt, William K Hagmann.
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 IC(50)=237 nM.Entities:
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Year: 2008 PMID： 18242984 DOI： 10.1016/j.bmcl.2008.01.045
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823