Article: article from journal or magazin.
Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies.
Bioorganic & Medicinal Chemistry Letters
Publication types: Journal Article
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.
Coumarins/chemical synthesis, Coumarins/chemistry, Crystallography, X-Ray, Inhibitory Concentration 50, Models, Molecular, Monoamine Oxidase/drug effects, Monoamine Oxidase Inhibitors/chemical synthesis, Monoamine Oxidase Inhibitors/chemistry, Structure-Activity Relationship
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