Bioorg Med Chem Lett. 2002 Dec 16;12(24):3551-5.

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

Carotti A, Carrieri A, Chimichi S, Boccalini M, Cosimelli B, Gnerre C, Carotti A, Carrupt PA, Testa B.

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Dipartimento Farmaco Chimico, via Orabona 4, I-70125 Bari, Italy. carotti@farmchim.uniba.it

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.

PMID:: 12443774; [PubMed - indexed for MEDLINE]

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