Article detail · 2020
Novel amine-functionalized benzimidazolium salts: Synthesis, characterization, bioactivity, and molecular docking studies
- Year
- 2020
- Type
- article
Data source split
- YÖKSİS YÖKSİS article record
- YÖKSİS venue JOURNAL OF MOLECULAR STRUCTURE
- Catalog match (ISSN) Journal of Molecular Structure
- OpenAlex OpenAlex enrichment (abstract, citations, topics)
Abstract
OpenAlex · English
Sulfonamide derivatives exhibit a wide biological activity and can function as potential medical molecules in the development of a drug. Studies have reported that the compounds have an effect on many enzymes. In this study, the derivatives of amine sulfonamide (1i-11i) were prepared with reduced imine compounds (1-11) with NaBH4 in methanol. The synthesized compounds were fully characterized by spectral data and analytical. The effect of the synthesized derivatives on acetylcholinesterase (AChE), glutathione S-transferase (GST) and α-glycosidase (α-GLY) enzymes were determined. For the AChE and α-GLY, the most powerful inhibition was observed on 10 and 10i series with KI value in the range 2.26 ± 0.45–3.57 ± 0.97 and 95.73 ± 13.67–102.45 ± 11.72 µM, respectively. KI values of the series for GST were found in the range of 22.76 ± 1.23–49.29 ± 4.49. Finally, the compounds have a stronger inhibitor in lower concentrations by the attachment of functional electronegative groups such as two halogens (-Br and -CI), -OH to the benzene ring and -SO2NH2. The crystal structures of AChE, α-GLY, and GST in complex with selected derivatives 4 and 10 show the importance of the functional moieties in the binding modes within the receptors.Communicated by Ramaswamy H. Sarma
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109 citations
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247 publications in the local catalog that cite this work (OpenAlex reference match; not the full global list).
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