Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595097 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A series of 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles (3a-k and 4a-u) were designed, synthesized, and evaluated for their inhibitory efficacy towards the two hMAO isoforms. Most of the derivatives were found to be potent and selective hMAO-B inhibitors. In particular, derivative 3g showed greater hMAO-B affinity than selective inhibitor selegiline coupled with high selectivity index (SIÂ =Â 145). The most selective hMAO-B inhibitor was the 3-methyl analogue 3f with an SI higher than 909.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rossella Fioravanti, Nicoletta Desideri, Mariangela Biava, Luca Proietti Monaco, Laura Grammatica, Matilde Yáñez,