Synthesis and study of a series of 3-arylcoumarins as potent and selective monoamine oxidase B inhibitors

• Tipo: Artigo em Revista Científica Internacional
• Data: 2011

Autores

Matos, MJ (Autor) Outra; Terán, C (Autor) Outra; Pérez Castillo, Y (Autor) Outra; Uriarte, E (Autor) Outra; Santana, L (Autor) Outra; Viña, D (Autor) Outra

Revista

Título: Journal of Medicinal Chemistry

Vol. 54

Páginas: 7127-7137

ISSN: 0022-2623

Editora: American Chemical Society

Indexação

Scopus - 116 Citações

Outras Informações

ID Authenticus: P-00R-0MK

DOI: 10.1021/jm200716y

Abstract (EN): New series of 6-substituted-3-arylcoumarins displaying several alkyl, hydroxyl, halogen, and alkoxy groups in the two benzene rings have been designed, synthesized, and evaluated in vitro as human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibitors. Most of the studied compounds showed a high affinity and selectivity to the hMAO-B isoenzyme, with IC 50 values on nanomolar and picomolar range. Ten of the 22 described compounds displayed higher MAO-B inhibitory activity and selectivity than selegiline. Coumarin 7 is the most active compound of this series, being 64 times more active than selegiline and also showing the highest hMAO-B specificity. In addition, docking experiments were carried out on hMAO-A and h-MAO-B structures. This study provided new information about the enzyme-inhibitor interaction and the potential therapeutic application of this 3-arylcoumarin scaffold. © 2011 American Chemical Society.

Idioma: Inglês

Tipo (Avaliação Docente): Científica