The reaction of unsaturated 4-arylidenoxazol-5(4 H )-ones with 2-(1 H -imidazol-4-yl)ethan-1-amine dihydrochloride was used to synthesize and describe the physicochemical characteristics of histamine N -acyl derivatives containing α,β-dehydroamino acids residues, as well as the corresponding 4-arylidenimidazol-5(4 H )-ones. Anticholinesterase and antiradical properties of the synthesized compounds were studied. It was revealed that the studied substances have anticholinesterase activity both acetylcholinesterase and butyrylcholinesterase and have almost no antiradical activity.