Yelekçi, KemalEvranos-Aksoz, BegumYabanoglu-Ciftci, SamiyeUcar, GulberkYelekçi, KemalErtan, Rahmiye2019-06-272019-06-272014470960-894X1464-34050960-894X1464-3405https://hdl.handle.net/20.500.12469/703https://doi.org/10.1016/j.bmcl.2014.06.015A novel series of 2-pyrazoline and hydrazone derivatives were synthesized and investigated for their human monoamine oxidase (hMAO) inhibitory activity. All compounds inhibited the hMAO isoforms (MAO-A or MAO-B) competitively and reversibly. With the exception of 5i which was a selective MAO-B inhibitor all derivatives inhibited hMAO-A potently and selectively. According to the experimental K-i values compounds 6e and 6h exhibited the highest inhibitory activity towards the hMAO-A whereas compound 5j which carries a bromine atom at R-4 of the A ring of the pyrazoline appeared to be the most selective MAO-A inhibitor. Tested compounds were docked computationally into the active site of the hMAO-A and hMAO-B isozymes. The computationally obtained results were in good agreement with the corresponding experimental values. (C) 2014 Elsevier Ltd. All rights reserved.eninfo:eu-repo/semantics/openAccess2-PyrazolineHydrazoneMAO inhibitorsMolecular dockingArticle327832841524WOS:00033922870001210.1016/j.bmcl.2014.06.0152-s2.0-84904036276N/AQ224986657