Novel (coumarin-3-yl)carbamates as selective MAO-B inhibitors: Synthesis, in vitro and in vivo assays, theoretical evaluation of ADME properties and docking study

• Tipo: Artigo em Revista Científica Internacional
• Data: 2013

Autores

Matos, MJ (Autor) Outra; Vilar, S (Autor) Outra; Gonzalez Franco, RM (Autor) Outra; Uriarte, E (Autor) Outra; Santana, L (Autor) Outra; Friedman, C (Autor) Outra; Tatonetti, NP (Autor) Outra; Viña, D (Autor) Outra; Fontenla, JA (Autor) Outra

Revista

Título: European Journal of Medicinal Chemistry

Vol. 63

Páginas: 151-161

ISSN: 0223-5234

Editora: Elsevier

Indexação

Scopus - 35 Citações

Outras Informações

ID Authenticus: P-00R-0MW

DOI: 10.1016/j.ejmech.2013.02.009

Abstract (EN): A series of (coumarin-3-yl)carbamates was synthesized and evaluated in vitro as monoamine oxidase (MAO-A and MAO-B) inhibitors. Most of the new compounds selectively inhibited MAO-B isoenzyme with IC50 values in the micro or nanoMolar ranges. Since these compounds must achieve the brain cells, theoretical evaluation of ADME properties were also carried out. Compound 8 (benzyl(coumarin-3-yl)carbamate), which presented the most interesting in vitro MAO-B inhibitory profile (IC50 against MAO-B = 45 nM), was subjected to further studies. This in vitro MAO-B inhibitory activity is comparable with that of the selegiline, the reference compound (IC50 against MAO-B = 20 nM). Taking into account the in vitro results of compound 8, in vivo assays and docking calculations were also carried out for this derivative.

Idioma: Inglês

Tipo (Avaliação Docente): Científica