Synthesis and Evaluation of New Tacrine Analogues as Anti-Alzheimer’s Agents (Research Article)

Author(s): Ranjithkumar Kadagandla and Baswaraju Macha

Abstract: A Series of new tacrine analogues were designed, synthesized, characterized by respective spectral data and evaluated for cholinesterase inhibitory activity to be useful in Alzheimer’s disease. Most of the synthesized compounds showed good in vitro inhibitory activities towards acetyl cholinesterase (AChE) and butyryl cholinesterase (BuChE) enzymes. Out of five compounds, synthesized, three (6a, 6b, 6c,) were evaluated for AChE and BuChE inhibitory activities,indicates that all the three compounds have exhibited almost similar potency against AChE with IC50 values between 0.31±0.02 and 0.37±0.04 μM, when compared to 0.23±0.01μM shown by the standard tacrine and 0.17μM exhibited by rivastigmine. Compound 6a and 6b with cyclopentano and cyclohexano fused tacrine analogs have shown almost equal potency to that of tacrine with IC50 values 0.34 and 0.31μM against AChE.

PAGES: 90-104  |  187 VIEWS  208 DOWNLOADS