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Constraining the amide bond in N-Sulfonylated dipeptide VLA-4 antagonists

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

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(5), pp.1688-1691 [Peer Reviewed Journal]

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Title:
Constraining the amide bond in N-Sulfonylated dipeptide VLA-4 antagonists
Author: Chang, Linda L ; Yang, Ginger X ; Mccauley, Ermengilda ; Mumford, Richard A ; Schmidt, John A ; Hagmann, William K
Description: 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, , VLA-4 IC = 237 nM.
Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(5), pp.1688-1691
Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2008.01.045
Subjects: Vla-4 ; Peptide Bond Mimetic ; Bicyclic Vla-4 Antagonists ; Imidazole Vla-4 Antagonists ; Medicine ; Chemistry ; Anatomy & Physiology
Language: English

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