The discovery and development of selective 3-fluoro-4-aryloxyallylamine inhibitors of the amine oxidase activity of semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1).

Jonathan S Foot, Mandar Deodhar, Craig I Turner, Ping Yin, Ellen M van Dam, Diego G Silva, Aldo Olivieri, Andrew Holt, Ian A McDonald

Pharmaxis Ltd., 20 Rodborough Road, Frenchs Forest, NSW 2086, Australia. jonathan.foot@pharmaxis.com.au

Bioorganic & medicinal chemistry letters 2012 Jun 15

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A new class of 3-fluoroallyl amine-based SSAO/VAP-1 inhibitors is reported. These compounds have excellent selectivity over diamine oxidase, MAO-A and MAO-B. Synthesis and SAR studies leading to compound 28 (PXS-4159A) are reported. The pharmacokinetic profile of 28 in the rat, together with activity in a murine model of lung inflammation are also disclosed. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Jonathan S Foot, Mandar Deodhar, Craig I Turner, Ping Yin, Ellen M van Dam, Diego G Silva, Aldo Olivieri, Andrew Holt, Ian A McDonald. The discovery and development of selective 3-fluoro-4-aryloxyallylamine inhibitors of the amine oxidase activity of semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1). Bioorganic & medicinal chemistry letters. 2012 Jun 15;22(12):3935-40