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

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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 (pIC50=7.55 vs 4.62). X-ray crystallography and molecular modelling studies helped the understanding of the observed structure–activity relationships.

Natural geiparvarin 1 and a number of its analogues were prepared and tested as MAO inhibitors. The desmethyl congener 6, proved the most potent and selective MAO-B inhibitor: pIC50 (MAO-B)=7.55 versus pIC50 (MAO-A)=4.62.

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Acknowledgements

The Italian authors wish to thank MIUR (Rome, Italy) for financial support.

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