Design, synthesis of chiral thiourea derivatives from enantiosaph amines and determination of cholinesterase enzyme inhibition activities

In this thesis study, sixteen new chiral thiourea derivatives were synthesized using the general synthesis method for thioureas. In our study, based on benzyl isothiocyanate, new chiral thiourea derivatives were synthesized from its reaction with different chiral amines [1-16] and characterization and activity studies were performed. In addition to different substituents, the characteristic properties and biological activities of the R and S enantiomers of the same substituents were studied. The structures of all products were illuminated by FT-IR, 1H NMR, 13C NMR and elemental analysis methods. The anticholinesterase inhibition activity of the synthesized compounds [1-16] was tested against AChE and BChE. In the synthesis series, it was found that compound 4 (IC50: 6.35±1.89 µM) was the most active against AChE, while compound 12 (IC50: 1.46±1.99 µM) was the most active against BChE. Compounds 3 and 4 showed better activity in all tests against both enzymes.