Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists |
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| Authors: | Chang Linda L Yang Ginger X McCauley Ermengilda Mumford Richard A Schmidt John A Hagmann William K |
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| Institution: | Department of Medicinal Chemical Research, Merck Research Laboratories, Rahway, NJ, USA. linda_chang@merck.com |
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| 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. |
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