title: Combinatorial synthesis of SSAO inhibitors using sonogashira coupling: SAR of aryl propargylic amines.
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.
authors.affiliation: Department of Chemistry, Materials and Forensic Sciences, University of Technology, Sydney, PO Box 123, Broadway, NSW 2007, Australia. c.conn@uts.edu.au
authors.forename: C
authors.initials: C
authors.lastname: Conn
authors.forename: R
authors.initials: R
authors.lastname: Shimmon
authors.forename: F
authors.initials: F
authors.lastname: Cordaro
authors.forename: T L
authors.initials: TL
authors.lastname: Hargraves
authors.forename: P
authors.initials: P
authors.lastname: Ibrahim
mesh_terms: D006631:Amine Oxidase (Copper-Containing) / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008968:Molecular Conformation; D010293:Pargyline / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D010293:Pargyline; D006631:Amine Oxidase (Copper-Containing)