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Article 2022 · 2 citations

SYNTHESIS AND ENZYME INHIBITORY PROPERTIES OF QUINOXALINE BRIDGED BIS(IMIDAZOLIUM) SALTS

Yigit, Murat, Demir, Yeliz, Arinc, Ali, Yigit, Beyhan, Koca, Murat, Ozdemir, Ismail, Gulcin, Ilhami

Abstract

In this study, a series of new salts containing quinoxaline and imidazole moieties were synthesized in good yield by the reaction of 2,3 -bis(bromomethyl)quinoxalines and 1-alkylimidazoles in N,N-dimethylformamide. These salts were characterized by elemental analysis, IR, H-1 NMR and C-13 NMR spectroscopy, which support the proposed structures. Furthermore, the enzyme inhibition activities of these compounds were investigated. They showed highly potent inhibition effect on acetylcholinesterase (AChE) and carbonic anhydrases (hCAs) (Ki values are in the range of 44.80 +/- 14.87 to 288.64 +/- 42.68 nM, 21.50 +/- 4.76 to 187.30 +/- 22.43 nM, and 5.81 +/- 0.71 to 164.52 +/- 26.0 nM for AChE, hCA I, and hCA II, respectively). Compound 3 showed the best inhibition effect for hCA I and compound 4 showed the best inhibition effect for hCA II and AChE.

Keywords
POTENT CARBONIC-ANHYDRASE ANTICHOLINERGIC ACTIVITIES ALPHA-GLYCOSIDASE CRYSTAL-STRUCTURE 1ST SYNTHESIS ACETYLCHOLINESTERASE DERIVATIVES BUTYRYLCHOLINESTERASE ANTIBACTERIAL BROMOPHENOLS
WoS Categories
Chemistry, Organic
Sustainable Development Goals
Citation
Journal
HETEROCYCLES
Year
2022
Volume
104
Issue
7
Pages
1268-1279
ISSN
0385-5414
eISSN
1881-0942
DOI
10.3987/COM-22-14668
WoS UID
WOS:000817759400006
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