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

Details

Serval ID
serval:BIB_22837
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies.
Journal
Bioorganic & Medicinal Chemistry Letters
Author(s)
Carotti A., Carrieri A., Chimichi S., Boccalini M., Cosimelli B., Gnerre C., Carotti A., Carrupt P.A., Testa B.
ISSN
0960-894X
Publication state
Published
Issued date
2002
Volume
12
Number
24
Pages
3551-3555
Language
english
Notes
Publication types: Journal Article
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, Coumarins/chemistry, Crystallography, X-Ray, Inhibitory Concentration 50, Models, Molecular, Monoamine Oxidase/drug effects, Monoamine Oxidase Inhibitors/chemical synthesis, Monoamine Oxidase Inhibitors/chemistry, Structure-Activity Relationship
Pubmed
Create date
19/11/2007 9:47
Last modification date
20/08/2019 12:59
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