高功能化氟化螺吡咯烷杂环衍生物的胆碱酯酶抑制活性

Cholinesterase inhibitory activity of highly functionalized fluorinated spiropyrrolidine heterocyclic hybrids.

作者信息

Kumar Raju Suresh, Almansour Abdulrahman I, Arumugam Natarajan, Kotresha D, Manohar Thota Sai, Venketesh S

机构信息

Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.

Department of Studies in Botany, Davangere University, Shivagangothri, Davangere 577007, Karnataka, India.

出版信息

Saudi J Biol Sci. 2021 Jan;28(1):754-761. doi: 10.1016/j.sjbs.2020.11.005. Epub 2020 Nov 11.

Two series of dimethoxyindanone imbedded novel fluorinated spiropyrrolidine heterocyclic hybrids were synthesized employing two different less explored azomethine ylides and were measured for their efficiency as inhibitors for Alzheimer's disease. Among the spiropyrrolidine heterocyclic hybrids, the indole based fluorinated compound with a methoxy substituent at the position of the aryl ring exhibited the utmost potent AChE and BChE inhibitory activities with an IC of 1.97 ± 0.19 µM and 7.08 ± 0.20 µM respectively. The plausible mechanism of inhibition on ChE receptors was unveiled via molecular docking studies.