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

Published inBioorganic & medicinal chemistry letters, vol. 12, no. 24, p. 3551-3555
Publication date2002
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.

Keywords
  • Coumarins/chemical synthesis/chemistry/*pharmacology
  • Crystallography, X-Ray
  • Inhibitory Concentration 50
  • Models, Molecular
  • Monoamine Oxidase/drug effects
  • Monoamine Oxidase Inhibitors/*chemical synthesis/chemistry/pharmacology
  • Structure-Activity Relationship
Affiliation Not a UNIGE publication
Citation (ISO format)
CAROTTI, Angelo et al. Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies. In: Bioorganic & medicinal chemistry letters, 2002, vol. 12, n° 24, p. 3551–3555. doi: 10.1016/s0960-894x(02)00798-9
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ISSN of the journal0960-894X
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