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) |
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| Authors: | Foot Jonathan S Deodhar Mandar Turner Craig I Yin Ping van Dam Ellen M Silva Diego G Olivieri Aldo Holt Andrew McDonald Ian A |
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| Institution: | Pharmaxis Ltd., 20 Rodborough Road, Frenchs Forest, NSW 2086, Australia. jonathan.foot@pharmaxis.com.au |
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| Abstract: | 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. |
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