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Articles

Vol. 2 No. 2 (2011): April – June 2011

Acetylcholinesterase/butylcholinesterase Inhibitory Activities of Substituted Chromenone Derivatives

DOI
https://doi.org/10.37285/ijddd.2.2.1
Submitted
November 28, 2024
Published
2024-12-08

Abstract

3,6-Disubstituted-2H-2-chromenones 3a-l and 3,4,6-trisubstituted 2H-2-chromenones 3m & 3n were synthesized from 5-bromosalicylaldehyde 1 and 5-bromo-2-hydroxyacetophenone 5. Suzuki coupling of 5-bromosalicylaldehyde with various phenylboronic acids yielded 5-substituted salicylaldehydes 2b-l and these compounds were reacted with various β-ketoesters in presence of piperidine afforded substituted chromenone derivatives 3a-l in very good yields. The compounds 3m & 3n were prepared by Suzuki coupling of 2m. Synthesized compounds 3a-n were screened for in vitro AChE & BuChE activities and found that the compound 3n shown significant activity where as 3g, 3h, 3j, 3k & 3m compounds were shown moderate activity of AChE. The compound 3d shown potent activity, where as 3c & 3m shown moderate activity of BuChE and the results were compared with the standard drug Galanthamine.

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