In:
Journal of Chemical Research, SAGE Publications, Vol. 41, No. 1 ( 2017-01), p. 30-35
Abstract:
A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3-triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. Three different linkers were used to optimise the enzyme inhibitory effect. Out of the 20 compounds, 13 showed some AChE inhibition. The most potent compound, which showed 84% inhibition at 100 μM, contained a 1-(2-fluorobenzyl)-1,2,3-triazole linked to a benzimidazole group. A docking simulation study showed that the most active compound bound preferentially to the catalytic anionic subsite of the AChE enzyme.
Type of Medium:
Online Resource
ISSN:
1747-5198
,
2047-6507
DOI:
10.3184/174751917X14836231670980
Language:
English
Publisher:
SAGE Publications
Publication Date:
2017
detail.hit.zdb_id:
3010810-X
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