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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
Testa, Bernard
Fernandes, Eduarda
Silva, Francisco
Pinto, Manuela
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Published in Helvetica Chimica Acta. 2001, vol. 84, no. 3, p. 552-570
Abstract 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
Stable URL http://archive-ouverte.unige.ch/unige:10582
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