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

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

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 pi-complex between topaquinone and the electron-rich aryl group of the inhibitor.

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