Inhibitory effects of novel benzamide derivatives towards acetylcholinesterase enzyme

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-(4-(N-(diaminomethylene)sulfamoyl)phenyl)-2-(substituted-benzamido)benzamide derivatives were synthesized and evaluated towards acetylcholinesterase (AChE, E.C.3.1.1.7) enzyme which is the most studied enzyme regarding Alzheimer's disease. The inhibition constants (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-(4-(N-(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

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