Synthesis and investigation of 4-aminotetrahydrokinoline derivatives on inhibition effects of acetylcholinesterase enzyme

In this thesis, 4-aminotetrahydroquinoline derivatives were synthesized by using the Povarov reaction method. Characterization of synthesized molecules was done in 1H, 13C NMR, IR, and LC-MS-MS. In the next step, the inhibition effect of these molecules on the acetylcholinesterase enzyme was investigated. 9-Amino-1,2,3,4-tetrahydroacridine hydrochloride hydrate (Tacrin) was used as a standard inhibitor. As a result of the study, IC50 values of 8 different 4-amino-tetrahydro quinoline derivatives, known (4) and synthesized for the first time (4), were calculated. It was found that obtained values were between the 0.22 µM and 0.36 µM. The average KI constant was calculated by drawing Lineweaverburk graphs for the molecules and it was seen that the obtained data ranged from 0.50 µM to 1.13 µM. In the last step of the study, the IC50 value of the Tacrine molecule was calculated 0.770 µM, and the KI value was calculated 0.880 µM. Besides, Vmax and KM values for DTNB and AChI substrates were respectively calculated 0.106 EÜ / ml, 0.096 EÜ / ml and 1.637 µM, 1.021 µM. When the data were evaluated, it was observed that all of the studied organic molecules had an inhibitory effect similar to the standard inhibitor.