(1H-Pyrrolo [2,3-B] Pyridine) 7-Azaindole as Cholinesterase/ Glycation Inhibitors

Abstract

As a part of our program to discover novel analoges of (1H-pyrrolo [2,3-b] pyridine) 7-azaindole having useful biological activities, a variety of 7-azaindole analogs 1-9 with variable substituents on phenyl ring of phenacyl moiety were synthesized and evaluated for their AChE, BChE and antiglycation Inhibitory potential. Compounds 2-5 were found to be AChE inhibitors with IC50 1.34 µM, 11.60 µM, 0.96 µM and 0.97 µM respectively, while compounds 2-5 were also found to be BChE inhibitors with IC50 1.25 µM,  3.93 µM, IC50 9.18µM and 10.20µM respectively. Compounds 2 (IC50 = 1.25±0.019uM) and 3 (IC50 = 3.93±0.36uM), showed potent BChE inhibitory potential than standard Galantamine (IC50 = 8.51±0.02uM). Besides this, compounds 2-9 were evaluated for glycation inhibition activity. Compound 5 (IC50 values 120.6+0.2uM) showed potent antiglycation potential than standard rutin (IC50=294.50+1.5uM). The size of the substituent, electron donating or  withdrawing effect of substituents as well as the position of substituent on phenyl effects the activity.