Rational design and synthesis of some substituted aminoethanones and acetamides as novel acetyl cholinesterase inhibitors

Chowdhary, PVR and Raveendran, N and Mehta, KC (2013) Rational design and synthesis of some substituted aminoethanones and acetamides as novel acetyl cholinesterase inhibitors. Advance Research in Pharmaceuticals and Biologicals, 3 (II). pp. 400-402. ISSN 2250-0774

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Abstract

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.

Item Type: Article
Uncontrolled Keywords: Anticholinesterase inhibition; Acetyl phenoxy aminoethanones; Acetyl phenoxy acetamides; Rivastigmine.
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Depositing User: KMC Manipal
Date Deposited: 21 Aug 2013 04:22
Last Modified: 21 Aug 2013 04:22
URI: http://eprints.manipal.edu/id/eprint/136829

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