Journal Name:
- Advance Research in Pharmaceuticals and Biologicals
Key Words:
| Author Name | University of Author |
|---|---|
Abstract (2. Language):
Rivastigmine is one of the important drug presently used to treat Alzheimer’s disease and it has short half life and
limited usage. That was the main reason for the synthesis of Rivastigmine related amino ethanones and acetamide
derivatives. 2-Chloro cycloamino ethanones and 2-chloro N-substituted acetamides were synthesized by adding
chloroacetylchloride dropwise to a mixture of cycloamine, dichloromethane and triethylamine and stirring for 1 hour at
0⁰c. These compounds were stirred at 60⁰c for 5 hours with a solution of m-hydroxy acetophenone in DMSO in presence
of potassium hydroxide to obtain 2-(3-acetyl)-phenoxy derivatives of 1-(cycloamino) ethanones and N-substituted
acetamides. The synthesized compounds were characeterized on the basis of physical and spectroscopic data.
Anticholinesterase inhibitory activity of these compounds was carried out by Ellman’s esterase assay and was found to
be active in 435 μM to 776 μM range. All the compounds were found to be drugable under Lipinski’s rule.
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FULL TEXT (PDF):
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400-402