Screening the cholinesterase inhibitory potential of some (1E, 4E)-1.5- diphenylpenta-1.4-dien-3-one derivatives

Year 2019, Volume: 2 Issue: 1, 7 - 12, 11.09.2019

Açelya Mavideniz Amirhossein Fallah Foroogh Koshravi Farimah Ahdno Mehmet Arter Tuğba Erçetin Mustafa Fethi Sahin Hayrettin Ozan Gülcan

Abstract

α,β-unsaturated ketones are particularly important scaffolds to be
utilized in diverse organic reactions including the synthesis of many heterocyclics.
Regarding their reactivities as electrophiles, their nature to be utilized as
drug candidates are quite limited, although there are natural molecules with
diverse pharmacological activities whivh are known to have α,β-unsaturated
functionalization. Within this preliminary and random drug-screening based
medicinal chemistry study, some (1E,4E)-1,5-diphenylpenta-1,4-dien-3-one
derivatives were synthesized and their structures were identified employing
chromatographic and spectral methods. The potential of the compounds to inhibit
acetylcholinesterase and butyrylcholinesterase enzymes was measured employing
modified Ellman’s method. Although the compounds were not found to be potent
inhibitors in comparison to current drugs, their activity spectra and
selectivity properties displayed their availability to be utilized as important
scaffolds for further design of similar α,β-unsaturated systems.

Keywords

acetylcholinesterase, butyrylcholinesterase, α, β-, unsaturated ketones

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