Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.

Linda L Chang,Ginger X Yang,Ermengilda McCauley,Richard A Mumford,John A Schmidt,William K Hagmann

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要

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=237nM.

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关键词

VLA-4,Peptide bond mimetic,Bicyclic VLA-4 antagonists,Imidazole VLA-4 antagonists

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