Synthesis of some 2-phenoxyacetamide/3-phenoxypropanamide derivatives and evaluation of their biological activities

In the presented thesis 8 new compounds were synthesized, including 3 phenoxyacetamide derivatives, 2 phenoxypropanamide derivatives and 3 oxobutanamide derivatives. The structures of the sythesized compounds were confirmed by 1H-NMR, 13C-NMR, HRMS and elemental analysis. Following that, the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of compounds at 10 μM concentration were evaluated by in vitro Ellman's method and IC50 value of compounds which showed cholinesterase inhibition more than %50 was determined. In addition, the effects of all synthesized compounds on the levels of inflammatory markers such as IL-1β, IL-6, TNF-α and NO were investigated. Moreover cytotoxicity and metal chelation properties of all compounds were evaluated. Finally, molecular docking studies were carried out to determine binding modes of the most potent AChE inhibitor compound 8 (IC50 = 0.63 μM) and the most potent BChE inhibitor compound 1 (IC50 = 2.10 μM).