Author/Authors :
Angelo Carotti، نويسنده , , Antonio Carrieri، نويسنده , , Stefano Chimichi، نويسنده , , Marco Boccalini، نويسنده , , Barbara Cosimelli، نويسنده , , Carmela Gnerre، نويسنده , , Andrea Carotti، نويسنده , , Pierre-Alain Carrupt، نويسنده , , Bernard Testa، نويسنده ,
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