Literature DB >> 29963738

meta-Cyanobenzyl substituted benzimidazolium salts: Synthesis, characterization, crystal structure and carbonic anhydrase, α-glycosidase, butyrylcholinesterase, and acetylcholinesterase inhibitory properties.

Ferhat Türker1, Duygu Barut Celepci2, Aydın Aktaş1, Parham Taslimi3, Yetkin Gök1, Muhittin Aygün2, İlhami Gülçin3.   

Abstract

meta-Cyanobenzyl-substituted N-heterocyclic carbene (NHC) precursors were synthesized by the reaction of a series of N-(alkyl)benzimidazolium with 3-bromomethyl-benzonitrile. These benzimidazolium salts were characterized by using 1 H NMR, 13 C NMR, FTIR spectroscopy, and elemental analysis techniques. The molecular and crystal structures of 2f and 2g complexes were obtained by using the single-crystal X-ray diffraction method. The derivatives of these novel NHC precursors were effective inhibitors of α-glycosidase (AG), the cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with Ki values in the range of 1.01-2.12 nM for AG, 189.56-402.44 nM for hCA I, 112.50-277.37 nM for hCA II, 95.45-352.58 nM for AChE, and 132.91-571.18 nM for BChE. In the last years, inhibition of the CA enzyme has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances such as obesity, glaucoma, cancer, and epilepsy.
© 2018 Deutsche Pharmazeutische Gesellschaft.

Entities:  

Keywords:  N-heterocyclic carbene precursors; acetylcholinesterase; butyrylcholinesterase; carbonic anhydrase; enzyme inhibition; α-glycosidase

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Year:  2018        PMID: 29963738     DOI: 10.1002/ardp.201800029

Source DB:  PubMed          Journal:  Arch Pharm (Weinheim)        ISSN: 0365-6233            Impact factor:   3.751


  3 in total

1.  Screening of Carbonic Anhydrase, Acetylcholinesterase, Butyrylcholinesterase, and α-Glycosidase Enzyme Inhibition Effects and Antioxidant Activity of Coumestrol.

Authors:  Lokman Durmaz; Adem Erturk; Mehmet Akyüz; Leyla Polat Kose; Eda Mehtap Uc; Zeynebe Bingol; Ruya Saglamtas; Saleh Alwasel; İlhami Gulcin
Journal:  Molecules       Date:  2022-05-11       Impact factor: 4.927

2.  Antioxidant, Antidiabetic, Anticholinergic, and Antiglaucoma Effects of Magnofluorine.

Authors:  Lokman Durmaz; Hatice Kiziltas; Leyla Guven; Hasan Karagecili; Saleh Alwasel; İlhami Gulcin
Journal:  Molecules       Date:  2022-09-11       Impact factor: 4.927

3.  The palladium-based complexes bearing 1,3-dibenzylbenzimidazolium with morpholine, triphenylphosphine, and pyridine derivate ligands: synthesis, characterization, structure and enzyme inhibitions.

Authors:  Aydın Aktaş; Gül Yakalı; Yeliz Demir; İlhami Gülçin; Muhittin Aygün; Yetkin Gök
Journal:  Heliyon       Date:  2022-09-16
  3 in total

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