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

  • Bioorg Med Chem Lett. 2002 Dec 16;12(24):3551-5. doi: 10.1016/s0960-894x(02)00798-9.
Angelo Carotti  1 ,  Antonio Carrieri ,  Stefano Chimichi ,  Marco Boccalini ,  Barbara Cosimelli ,  Carmela Gnerre ,  Andrea Carotti ,  Pierre Alain Carrupt ,  Bernard Testa
Affiliations
PMID: 12443774 DOI: 10.1016/s0960-894x(02)00798-9
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.

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