Design and synthesis of chromone-based monoamine oxidase B inhibitors with improved drug-like properties

Autor:	Joana Reis, Carlos Fernandes, Hoda Salem, Marta Maia, Cláudia Tomé, Sofia Benfeito, José Teixeira, Paulo J. Oliveira, Eugenio Uriarte, Francesco Ortuso, Stefano Alcaro, Donatella Bagetta, Fernando Cagide, Fernanda Borges
Rok vydání:	2022
Předmět:	Pharmacology Structure-Activity Relationship Monoamine Oxidase Inhibitors Chromones Organic Chemistry Drug Discovery Dopamine Agents Humans Benzopyrans General Medicine Ferric Compounds Monoamine Oxidase
Zdroj:	European journal of medicinal chemistry. 239
ISSN:	1768-3254
Popis:	The absence of disease modifying drugs in Parkinson's disease therapy urges for new chemical entities acting on relevant PD-associated biological targets. As a result, developing selective and reversible inhibitors targeting MAO-B is still a desirable line of therapeutic research. Within this framework, a small library of chromone derivatives was synthesized and screened towards human monoamine oxidases. Structural modifications on the chromone 3-phenylcarboxamide resulted in potent MAO-B inhibitors with an improved drug-like profile, and for the first time we obtained potent and selective chromone 2-phenylcarboxamides acting in the low nanomolar range. Compounds 5-hydroxy-4-oxo-N-phenyl-4H-chromene-3-carboxamide (38) (IC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa085e4699884acd295c10b3f2e2df87 https://pubmed.ncbi.nlm.nih.gov/35772321 Zobrazit plný text záznamu Full Text from ScienceDirect