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)

Autor:	Andrew Holt, Jonathan S. Foot, Craig Ivan Turner, Aldo Olivieri, Ian A. McDonald, Diego Silva, Ellen M. van Dam, Mandar Deodhar, Ping Yin
Rok vydání:	2012
Předmět:	Models Molecular Amine oxidase Monoamine Oxidase Inhibitors Halogenation Clinical Biochemistry Anti-Inflammatory Agents Pharmaceutical Science Inflammation Biochemistry Mice Structure-Activity Relationship Drug Discovery medicine Structure–activity relationship Animals Humans Amines Molecular Biology Chemistry Drug discovery Organic Chemistry Pneumonia Rats Allyl Compounds Isoenzymes Molecular Medicine Amine gas treating Amine Oxidase (Copper-Containing) medicine.symptom Diamine oxidase Selectivity
Zdroj:	Bioorganicmedicinal chemistry letters. 22(12)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70da8507dc54027204a56780fa27cf5c https://pubmed.ncbi.nlm.nih.gov/22595173 Zobrazit plný text záznamu Full Text from ScienceDirect