Inhibitory effects of novel benzamide derivatives towards acetylcholinesterase enzyme

Authors : Cem YAMALI, Halise İnci GÜL, Serkan LEVENT, Yeliz DEMİR

Pages : 429-434

Doi:10.18596/jotcsa.842465

View : 15 | Download : 13

Publication Date : 2021-05-31

Article Type : Research Paper

Abstract :Alzheimer`s disease is one of the diseases which is identified by progressive memory loss and cognitive deficits leading to a decline in the lifespan of the patients. The drugs used in the clinic show palliative properties and they are unable to modify disease progression. In this study, N-insert ignore into journalissuearticles values(4-insert ignore into journalissuearticles values(N-insert ignore into journalissuearticles values(diaminomethylene);sulfamoyl);phenyl);-2-insert ignore into journalissuearticles values(substituted-benzamido);benzamide derivatives were synthesized and evaluated towards acetylcholinesterase insert ignore into journalissuearticles values(AChE, E.C.3.1.1.7); enzyme which is the most studied enzyme regarding Alzheimer`s disease. The inhibition constants insert ignore into journalissuearticles values(Ki); of the compounds synthesized towards the AChE enzyme were in the range of 15.51 ± 1.88 - 41.24 ± 10.13 nM. The most effective compound with the lowest Ki = 15.51 ± 1.88 nM, 2-benzamido-N-insert ignore into journalissuearticles values(4-insert ignore into journalissuearticles values(N-insert ignore into journalissuearticles values(diaminomethylene);sulfamoyl);phenyl);benzamide 6, can be reported as a lead compound of this study. Bioactivity results obtained by this study may provide useful information on the development of novel and potent inhibitors targeting Alzheimer`s disease.
Keywords : Acetylcholinesterase, sulfaguanidine, Alzheimer`s disease