Combinatorial Synthesis of SSAO Inhibitors Using Sonogashira Coupling: SAR of Aryl Propargylics Amines

Pergamon-Elsevier Science Ltd
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Journal Article
Bioorganic & Medicinal Letters, 2001, 11 pp. 2565 - 2568
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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 p-complex between topaquinone and the electron-rich aryl group of the inhibitor.
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