title: Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies.
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.
authors.affiliation: Dipartimento Farmaco Chimico, via Orabona 4, I-70125 Bari, Italy. carotti@farmchim.uniba.it
authors.forename: Angelo
authors.initials: A
authors.lastname: Carotti
authors.forename: Antonio
authors.initials: A
authors.lastname: Carrieri
authors.forename: Stefano
authors.initials: S
authors.lastname: Chimichi
authors.forename: Marco
authors.initials: M
authors.lastname: Boccalini
authors.forename: Barbara
authors.initials: B
authors.lastname: Cosimelli
authors.forename: Carmela
authors.initials: C
authors.lastname: Gnerre
authors.forename: Andrea
authors.initials: A
authors.lastname: Carotti
authors.forename: Pierre Alain
authors.initials: PA
authors.lastname: Carrupt
authors.forename: Bernard
authors.initials: B
authors.lastname: Testa
mesh_terms: D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D008995:Monoamine Oxidase / Q000187:drug effects; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D003374:Coumarins; D008996:Monoamine Oxidase Inhibitors; D008995:Monoamine Oxidase; C058446:geiparvarin