Tyrosine-like condensed derivatives as tyrosinase inhibitors

• Tipo: Artigo em Revista Científica Internacional
• Data: 2012

Autores

Matos, MJ (Autor) Outra; Santana, L (Autor) Outra; Uriarte, E (Autor) Outra; Serra, S (Autor) Outra; Corda, M (Autor) Outra; Fadda, MB (Autor) Outra; Era, B (Autor) Outra; Fais, A (Autor) Outra

Revista

Título: Journal of Pharmacy and Pharmacology

Vol. 64

Páginas: 742-746

ISSN: 0022-3573

Editora: Oxford University Press

Indexação

Scopus - 11 Citações

Outras Informações

ID Authenticus: P-00R-0MQ

DOI: 10.1111/j.2042-7158.2012.01467.x

Abstract (EN): Objectives We report the pharmacological evaluation of a new series of 3-aminocoumarins differently substituted with hydroxyl groups, which have been synthesized because they include in their structures the tyrosine fragment (tyrosine-like compounds), with the aim of discovering structural features necessary for tyrosinase inhibitory activity. Methods The synthesized compounds 4 and 7-9 were evaluated in vitro as mushroom tyrosinase inhibitors. Key findings Two of the described compounds showed lower IC50 (concentration giving 50% inhibition of tyrosinase activity) than umbelliferone, used as a reference compound. Conclusions Compound 7 (IC50 = 53 ¿m) was the best tyrosinase inhibitor of this small series, having an IC50 value 10-fold lower than umbelliferone. Compound 7 (3-amino-7-hydroxycoumarin) had amino and hydroxyl groups precisely mimicking the same positions that both groups occupy on the tyrosine molecule. © 2012 The Authors. JPP © 2012 Royal Pharmaceutical Society.

Idioma: Inglês

Tipo (Avaliação Docente): Científica