Acetylcholinesterase inhibitory potencies of new pyrazoline derivatives

Abstract

Alzheimer's disease (AD) has no current cure and its mechanism is not fully known, but treatments for symptoms are available. Acetylcholinesterase (AChE) has been reported to be an applicable therapeutic target in patient with AD. Acetylcholinesterase inhibitors (AChEIs) are commonly used for it. For this purpose, novel series of pyrazoline based compounds [2-(3-(4-methoxyphenyl)-5-aryl-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazole, 1-9] were synthesized and AChE inhibitory potencies were reported here. The results indicated that compound 1 (Ki= 0.13±0.004 μM) possessed the highest AChE inhibitory effect in series, which is two times more potent than the reference compound Tacrin (Ki= 0.26±0.045 μM). So, pyrazoline derivative 1 can be considered as a lead inhibitor in designing new AChE inhibitors.