1328892-97-2Relevant academic research and scientific papers
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: A new scaffold for the selective inhibition of monoamine oxidase B
MacCioni, Elias,Alcaro, Stefano,Cirilli, Roberto,Vigo, Sara,Cardia, Maria Cristina,Sanna, Maria Luisa,Meleddu, Rita,Yanez, Matilde,Costa, Giosuè,Casu, Laura,Matyus, Peter,Distinto, Simona
, p. 6394 - 6398 (2011/11/06)
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles were designed, synthesized, and tested as inhibitors against human monoamine oxidase (MAO) A and B isoforms. Several compounds, obtained as racemates, were identified as selective MAO-B inhibitors. The enantiomers of some derivatives were separated by enantioselective HPLC and tested. The R-enantiomers always showed the highest activity. Docking study and molecular dynamic simulations demonstrated the putative binding mode. We conclude that these 1,3,4-oxadiazoles derivatives are promising reversible and selective MAO-B inhibitors.
