Design and synthesis of novel selective monoamineoxidase-B inhibitor compounds and evaluation of effects in the treatment of parkinson's disease

pyridazinon-2-yl acetohydrazide starting materials were synthesized. The resulting substances were synthesized as a result of the reaction of 6-[4-morpholinopiperazin-1-yl]-3(2H)-pyridazinon-2-yl acetohydrazide with various benzaldehyde and acetophenone derivatives. Rf values, melting points, percentage yields and physical properties of the synthesized and purified compounds were determined. The structures of the compounds were elucidated by 1H-NMR, 13C-NMR and mass spectra. MAO inhibition activities of the compounds were determined by ELISA method at Bari Aldo Moro University. By comparing their effects with MAO-B inhibitor drugs such as selegiline used in the treatment of parkinson's, the passage of active compounds across the blood-brain barrier was investigated. Results: The MAO-A inhibitory effects of the compounds were quite low; compounds Y8, Y15 and Y16 showed no MAO-A inhibitory effects. The IC50 values of Y5 and Y11, which have a high percentage of MAO-B enzyme inhibition, are 0.704 ± 0.106 and 0.453 ± 0.035, respectively. Conclusion: Modifications and new drug designs to be made by determining the structure-activity relationships of the compounds synthesized within the scope of the thesis will shed light on further studies and provide access to the most active MAO inhibitors.