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- Title
Natural and Synthetic Xanthones as Monoamine Oxidase Inhibitors: Biological Assay and 3D-QSAR.
- Authors
Gnerre, Carmela; Thull, Ulrike; Gaillard, Patrick; Carrupt, Pierre-Alain; Testa, Bernard; Fernandes, Eduarda; Silva, Francisco; Pinto, Manuela; Pinto, Madalena M. M.; Wolfender, Jean-Luc; Hostettmann, Kurt; Cruciani, Gabriele
- Abstract
Fifty-nine xanthones (=9 H-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 n M. 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.
- Publication
Helvetica Chimica Acta, 2001, Vol 84, Issue 3, p552
- ISSN
0018-019X
- Publication type
Article
- DOI
10.1002/1522-2675(20010321)84:3<552::AID-HLCA552>3.0.CO;2-X