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Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies

Carotti, Angelo
Carrieri, A.
Chimichi, S.
Boccalini, M.
Cosimelli, B.
Gnerre, Carmela
Testa, Bernard
Published in Bioorganic & Medicinal Chemistry Letters. 2002, vol. 12, no. 24, p. 3551-3555
Abstract Natural geiparvarin 1 and a number of its analogues were prepared and tested as inhibitors of both monoamine oxidase isoforms, MAO-B and MAO-A. The desmethyl congener 6 of geiparvarin, proved potent and selective MAO-B inhibitor (pIC(50)=7.55 vs 4.62). X-ray crystallography and molecular modelling studies helped the understanding of the observed structure-activity relationships.
Keywords Coumarins/chemical synthesis/chemistry/*pharmacologyCrystallography, X-RayInhibitory Concentration 50Models, MolecularMonoamine Oxidase/drug effectsMonoamine Oxidase Inhibitors/*chemical synthesis/chemistry/pharmacologyStructure-Activity Relationship
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PMID: 12443774

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Deposited on : 2010-08-06

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