1360468-64-9Relevant academic research and scientific papers
Novel amine-functionalized benzimidazolium salts: Synthesis, characterization, bioactivity, and molecular docking studies
Yi?it, Murat,Yi?it, Beyhan,Taslimi, Parham,?zdemir, ?smail,Karaman, Muhammet,Gul?in, ?lhami
, (2020)
A series of amine-tethered benzimidazolium salts were synthesized by the reactions between 1-(1-methyl-2-dimethylaminoethyl)benzimidazole and various alkyl halides. The characterization of the newly synthesized salts was done by spectroscopic methods. Also, 2e, 2f, and 2h have been docked into the catalytic active site hCA I, hCA II, AChE, BChE, and α-glycosidase enzymes. We have identified high binding affinity and explained inhibition mechanism of the compounds against the enzymes. These novel amine-functionalized benzimidazolium salts derivatives were good inhibitor compounds of the α-glycosidase, hCA I and II isoforms, and both cholinesterase enzymes with Ki values in the range of 0.63 ± 0.05–3.63 ± 0.83 nM for α-glycosidase, 8.42 ± 1.03–27.04 ± 3.74 nM for hCA I, 7.94 ± 0.74–21.82 ± 5.81 nM for hCA II, 136.38 ± 19.55–247.34 ± 34.06 nM for BChE, and 124.24 ± 13.94–283.55 ± 54.06 nM for AChE, respectively. Among the inhibitors, 2e, 2e, 2f, 2f, and 2h were obtained to be the excellent inhibitors with Ki values of 8.42 ± 1.03, 7.94 ± 0.74, 124.24 ± 13.94, 136.38 ± 19.55, and 0.63 ± 0.05 nM for hCA I, hCA II, AChE, BChE, α-glycosidase enzymes, respectively. The ability to model some metabolic enzymes receptors and theirs inhibitors in silico are important because they can save valuable resources and help to rationalize the mode of binding, and to design better inhibitors.
Synthesis and antimicrobial studies of 1-methyl-2-dimethylaminoethyl- substituted benzimidazolium salts and N-heterocyclic carbene-silver complexes
Yigit, Beyhan,Goek, Yetkn,Oezdemir, Ilknur,Guenal, Selami
experimental part, p. 371 - 379 (2012/05/31)
The synthesis and antimicrobial studies of 1-methyl-2-dimethylaminoethyl- substituted carbene precursors and silver complexes are reported. The carbene precursors (1a-d) have been prepared from 1-methyl-2-dimethylaminoethyl- substituted benzimidazole and various alkyl halides. The silver-NHC complexes (2a-d) were synthesized from the benzimidazolium salts and Ag2O in dichloromethane at room temperature. The new compounds were characterized by 1H NMR, 13C NMR, FT-IR, and elemental analyses. The new carbene precursors and Ag-complexes were tested for their invitro antimicrobial activity against a variety of Gram-positive and Gram-negative bacteria, as well as for their antifungal activities against Candida albicans and Candida tropicalis. Copyright
