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Pak J Pharm Sci ; 32(3 (Supplementary)): 1155-1162, 2019 May.
Article in English | MEDLINE | ID: mdl-31303584

ABSTRACT

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±0.12µM for AChE and among them five compounds showed potent activity with IC50 values 17.16±0.02 to 231.6±0.12µM for BChE when compared with standard Eserine (IC50 = 0.85±0.0001 µM (AChE) & 0.04±0.0001µM (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.


Subject(s)
Cholinesterase Inhibitors/chemical synthesis , Cholinesterase Inhibitors/pharmacology , Dihydropyridines/chemistry , Acetylcholinesterase/metabolism , Butyrylcholinesterase/metabolism , Dihydropyridines/chemical synthesis , Dihydropyridines/pharmacology , Drug Evaluation, Preclinical , Magnetic Resonance Spectroscopy , Spectroscopy, Fourier Transform Infrared , Structure-Activity Relationship
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