NOVEL DUAL-BINDING CATION-Π INHIBITORS OF ACHE: DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION

R.S. Rathore

Centre for Biological Sciences (Bioinformatics), School of Earth, Biological and Environmental Sciences, Central University of South Bihar, Patna 800 014, India

Abstract

The characteristic dual binding of Acetylcholinesterase (AChE) inhibitors and discovery of predominant cation-π interactions responsible for high affinity has led to the design of new potent inhibitors for AChE. We report new scaffolds as AChE inhibitors, which tightly bind to enzyme, via hydrophobic interactions flanked by cation-π interactions. These compounds indicate activity in nano molar ranges in bioassays. MTT cytotoxic assays performed on prevalent neuronal cell lines (SK-N-SH) suggest no toxicity up to 0.6 µM. These new scaffolds for AChE serves as an alternate solution for ongoing symptomatic treatment for Alzhemier disorder.

Keywords: Inhibitors, toxicity, symptomatic, assays.