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)

Artigo Revisado por pares

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)

2012; Elsevier BV; Volume: 22; Issue: 12 Linguagem: Inglês

10.1016/j.bmcl.2012.04.111

ISSN

1464-3405

Autores

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

Tópico(s)

Biochemical Acid Research Studies

Resumo

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.

Ver no editor

Altmetric

PlumX

Entrar

Lembrar minha senha

Receber meu e-mail de confirmação

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)