Combinatorial synthesis of SSAO inhibitors using sonogashira coupling: SAR of aryl propargylic amines

Publication Type:
Journal Article
Citation:
Bioorganic and Medicinal Chemistry Letters, 2001, 11 (19), pp. 2565 - 2568
Issue Date:
2001-10-08
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The structure-activity relationships for semicarbazide-sensitive amine oxidase (SSAO) inhibitors based on arylpropynylamines was investigated using solution-phase combinatorial Sonogashira coupling. The results suggest that binding to the active site occurs by coordination of the amine to the proximal copper(II) and formation of a π-complex between topaquinone and the electron-rich aryl group of the inhibitor. © 2001 Elsevier Science Ltd. All rights reserved.
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