(Central University of Punjab, 2018) Bala, Manu; Kumar, Vinod
MAO inhibitors have been explored as therapeutic agents for the treatment or management of PD. A series of 2,4,6-trisubstituted pyrimidine derivatives incorporating a propargyl moiety were synthesized and screened for their MAO inhibition potential using Amplex® Red assay. All the compounds showed good inhibitory activity for MAO-B. The structure-activity relationship profile has been developed with number of electron releasing and electron withdrawing substituents attached to the pyrimidine nucleus. MV7 was found to be the most potent MAO-B inhibitor with IC50 value of 0.44 ± 0.02 ?M. From molecular docking studies, it was found that compounds fit well in the active site of MAO-B isoform near FAD cofactor. Thus, the active compound MV7 obtained in this series can act as promising lead for the development of effective and potent MAO-B inhibitor for the treatment of Parkinson's disease.