Elsevier, Bioorganic and Medicinal Chemistry Letters, 24(12), p. 3551-3555
DOI: 10.1016/s0960-894x(02)00798-9
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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.