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

Conn, C; Shimmon, R; Cordaro, F; Hargraves, TL; Ibrahim, P

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

Conn, C Shimmon, R

Cordaro, F Hargraves, TL

Ibrahim, P

Permalink

Publication Type:: Journal Article
Citation:: Bioorganic and Medicinal Chemistry Letters, 2001, 11 (19), pp. 2565 - 2568
Issue Date:: 2001-10-08

Closed Access

	Filename	Description	Size
	2004004617.pdf		306.45 kB	Adobe PDF	View/Open

Copyright Clearance Process

Recently Added
In Progress
Closed Access

This item is closed access and not available.

Full metadata record

Field	Value	Language
dc.contributor.author	Conn, C	en_US
dc.contributor.author	Shimmon, R https://orcid.org/0000-0002-8763-991X	en_US
dc.contributor.author	Cordaro, F	en_US
dc.contributor.author	Hargraves, TL https://orcid.org/0000-0002-5182-9092	en_US
dc.contributor.author	Ibrahim, P	en_US
dc.date.issued	2001-10-08	en_US
dc.identifier.citation	Bioorganic and Medicinal Chemistry Letters, 2001, 11 (19), pp. 2565 - 2568	en_US
dc.identifier.issn	0960-894X	en_US
dc.identifier.uri	http://hdl.handle.net/10453/3210
dc.description.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 π-complex between topaquinone and the electron-rich aryl group of the inhibitor. © 2001 Elsevier Science Ltd. All rights reserved.	en_US
dc.relation.ispartof	Bioorganic and Medicinal Chemistry Letters	en_US
dc.relation.isbasedon	10.1016/S0960-894X(01)00506-6	en_US
dc.subject.classification	Medicinal & Biomolecular Chemistry	en_US
dc.subject.mesh	Pargyline	en_US
dc.subject.mesh	Amine Oxidase (Copper-Containing)	en_US
dc.subject.mesh	Enzyme Inhibitors	en_US
dc.subject.mesh	Molecular Conformation	en_US
dc.subject.mesh	Structure-Activity Relationship	en_US
dc.title	Combinatorial synthesis of SSAO inhibitors using sonogashira coupling: SAR of aryl propargylic amines	en_US
dc.type	Journal Article
utslib.citation.volume	19	en_US
utslib.citation.volume	11	en_US
utslib.for	0304 Medicinal and Biomolecular Chemistry	en_US
utslib.for	0305 Organic Chemistry	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Business
pubs.organisational-group	/University of Technology Sydney/Faculty of Science
pubs.organisational-group	/University of Technology Sydney/Faculty of Science/School of Chemistry and Forensic Science
pubs.organisational-group	/University of Technology Sydney/Strength - CCET - Centre for Clean Energy Technology
pubs.organisational-group	/University of Technology Sydney/Strength - CHERE - Centre for Health Economics Research and Evaluation
utslib.copyright.status	closed_access
pubs.issue	19	en_US
pubs.publication-status	Published	en_US
pubs.volume	11	en_US

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 π-complex between topaquinone and the electron-rich aryl group of the inhibitor. © 2001 Elsevier Science Ltd. All rights reserved.

Please use this identifier to cite or link to this item:

http://hdl.handle.net/10453/3210