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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Coumarins / chemical synthesis
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Coumarins / chemistry
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Coumarins / pharmacology*
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Crystallography, X-Ray
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Inhibitory Concentration 50
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Models, Molecular
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Monoamine Oxidase / drug effects
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Monoamine Oxidase Inhibitors / chemical synthesis*
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Monoamine Oxidase Inhibitors / chemistry
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Monoamine Oxidase Inhibitors / pharmacology
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Structure-Activity Relationship
Substances
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Coumarins
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Monoamine Oxidase Inhibitors
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Monoamine Oxidase
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geiparvarin