In:
Journal of Chemical Research, SAGE Publications, Vol. 45, No. 5-6 ( 2021-05), p. 572-581
Abstract:
Four 2-phenylthiazole derivatives are synthesized, characterized, and evaluated as cholinesterase inhibitors. The structures of the 2-phenylthiazole derivatives are confirmed by 1 H and 13 C nuclear magnetic resonance spectroscopy, single-crystal X-ray diffraction studies, and Hirshfeld surfaces analysis. Hirshfeld surface analysis of the prepared compounds showed C–H···O intermolecular interactions. The cholinesterase inhibition activities of the synthesized compounds are tested by Ellman’s method. [2-(4-Benzyloxyphenyl)-thiazol-4-yl]-(3,5-dimethylpiperidin-1-yl)-methanone showed the best acetylcholinesterase inhibition activity with an IC 50 value of 8.86 µM and the best butyrylcholinesterase inhibition activity with an IC 50 value of 1.03 µM. A docking study demonstrates that the same compound interacts with the catalytic anionic site and peripheral anionic site of acetylcholinesterase and the catalytic anionic site of butyrylcholinesterase.
Type of Medium:
Online Resource
ISSN:
1747-5198
,
2047-6507
DOI:
10.1177/1747519820976543
Language:
English
Publisher:
SAGE Publications
Publication Date:
2021
detail.hit.zdb_id:
3010810-X