Zafar_2019_Pak.J.Pharm.Sci_32_1155

Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vitro cholinesterases (AChE, BChE) inhibitory activity. All compounds showed potent activity with IC50 values between 0.21+/-0.003 to 147.14+/-0.12muM for AChE and among them five compounds showed potent activity with IC50 values 17.16+/-0.02 to 231.6+/-0.12muM for BChE when compared with standard Eserine (IC50 = 0.85+/-0.0001 muM (AChE) & 0.04+/-0.0001muM (BChE). The most potent compound 11 can be considered as potential lead compound showed an inhibition of 95.35+/-0.11 and IC50= 0.21+/-0.003 while compound 7 showed an inhibition of 83.45+/-0.13 and IC50= 17.16+/-0.02. It is concluded from structural activity relationship that the presence of nitro group at C-2 and C-4 position of dihydropyridine ring increase the acetyl cholinesterase and butyrylcholinesterase activities of these compounds while presence of -Br and -Cl also enhances the activities.