Natural and synthetic xanthones as monoamine oxidase inhibitors: Biological assay and 3D-QSAR

• Tipo: Artigo em Revista Científica Internacional
• Data: 2001

Autores

Gnerre, C (Autor) Outra; Thull, U (Autor) Outra; Gaillard, P (Autor) Outra; Carrupt, PA (Autor) Outra; Testa, B (Autor) Outra; Fernandes, E (Autor) FFUP; Silva, F (Autor) Outra; Pinto, M (Autor) Outra; Pinto, MMM (Autor) FFUP; Wolfender, JL (Autor) Outra; Hostettmann, K (Autor) Outra; Cruciani, G (Autor) Outra

Revista

Título: Helvetica Chimica Acta

Vol. 84

Páginas: 552-570

ISSN: 0018-019X

Editora: Wiley-Blackwell

Indexação

ISI Web of Knowledge - 61 Citações

Scopus - 67 Citações

Classificação Científica

FOS: Ciências exactas e naturais > Química

Outras Informações

ID Authenticus: P-000-X5H

DOI: 10.1002/1522-2675(20010321)84:3<552::aid-hlca552>3.0.co;2-x

Abstract (EN): Fifty-nine xanthones (= 9H-xanthen-9-ones) of natural or synthetic origin were investigated for their inhibitory activity toward monoamine-oxidase A (MAO-A) and MAO-B. The compounds demonstrated reversible. time-independent activities, with selectivity toward MAO-A. The most active inhibitor had an IC50 of 40 nM. Electron absorption spectroscopy revealed the formation of a 1:1 charge-transfer complex between lumiflavine and xanthones. 3D-QSAR Studies according to the CoMFA/GOLPE procedure provided information on the relationship between steric and electrostatic fields and MAO-A inhibition. The ALMOND procedure yielded additional topographical information on structural factors favoring activity.

Idioma: Inglês

Tipo (Avaliação Docente): Científica