1. Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. synthesis and SAR studies
- Author
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Angelo Carotti, Bernard Testa, Pierre-Alain Carrupt, Antonio Carrieri, Stefano Chimichi, Barbara Cosimelli, Andrea Carotti, Marco Boccalini, Carmela Gnerre, Carotti, A, Carrieri, A, Chimichi, S, Boccalini, M, Cosimelli, Barbara, Gnerre, C, CARRUPT P., A, and Testa, B.
- Subjects
Models, Molecular ,Monoamine Oxidase/drug effects ,Monoamine Oxidase Inhibitors ,Stereochemistry ,Monoamine oxidase ,Clinical Biochemistry ,Pharmaceutical Science ,Monoamine Oxidase Inhibitors/*chemical synthesis/chemistry/pharmacology ,Crystallography, X-Ray ,Biochemistry ,Geiparvarin ,Inhibitory Concentration 50 ,Structure-Activity Relationship ,chemistry.chemical_compound ,Coumarins ,Drug Discovery ,Organic chemistry ,Monoamine Oxidase ,Molecular Biology ,ddc:615 ,Coumarins/chemical synthesis/chemistry/*pharmacology ,Organic Chemistry ,Desmethyl ,Congener ,chemistry ,Molecular Medicine ,Monoamine oxidase B - 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.
- Published
- 2002
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