Paper Title
Synthesis and Characterization of a New Series of Thiazolylhydrazine Derivatives Containing Dimethylaminoethyl Moiety as Potential CHE Inhibitor
Abstract
Alzheimer’s disease (AD) is the most common of the degenerative brain diseases. Recent studies have shown that numerous thiazolylhydrazine derivatives exhibit cholinesterase (ChE) inhibitory activity in the micromolar concentration range. In addition, the dimethylaminoethyl residue gives the structure similarity to acetylcholine. Thus, in this study five new thiazolylhydrazine containing dimethylaminoethyl derivatives were designed and synthesized to able to have good inhibition profile as cholinesterase inhibitors. The structures of synthesized compounds were confirmed spectroscopic methods (1H NMR and 13C NMR). The ChE inhibitor activity of final compounds was performed. According to enzyme inhibition assay, compound 3e showed promising inhibition potency against AChE enzyme with IC50 values of 0.2058±0.007 µM.
Keywords - Alzhmeir, Cholinesterase, Dimethylaminoethyl, Thiazolylhydrazine.