Synthesis and antidiabetic evaluation of benzimidazole‐tethered 1,2,3‐triazoles
| Autor: | C. P. Kaushik, Suman Punia, Devinder Kumar, Yogesh Deswal, Vikas Verma, Ashwani Kumar, Laxmi Deswal |
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| Rok vydání: | 2020 |
| Předmět: |
Benzimidazole
Magnetic Resonance Spectroscopy 1 2 3-Triazole 010405 organic chemistry Pharmaceutical Science Triazoles 01 natural sciences 0104 chemical sciences Molecular Docking Simulation Inhibitory Concentration 50 Structure-Activity Relationship 010404 medicinal & biomolecular chemistry chemistry.chemical_compound Binding conformation chemistry Docking (molecular) Spectroscopy Fourier Transform Infrared Drug Discovery Click chemistry Mass spectrum Hypoglycemic Agents Imidazole Benzimidazoles Azide Nuclear chemistry |
| Zdroj: | Archiv der Pharmazie. 353:2000090 |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.202000090 |
| Popis: | Some novel benzimidazole-tethered 1,2,3-triazole derivatives (4a-r) were synthesized by a click reaction between 2-substituted 1-(prop-2-yn-1-yl)-1H-benzo[d]imidazole and in situ azide. The structures of the synthesized compounds were confirmed by spectroscopic studies (one- and two-dimensional nuclear magnetic resonance, Fourier transform infrared, and high-resolution mass spectra). The synthesized compounds were evaluated for their antidiabetic activity. Compounds 4a-r exhibited a good-to-moderate α-amylase and α-glucosidase inhibitory activity, with IC50 values ranging from 0.0410 to 0.0916 µmol/ml and 0.0146 to 0.0732 µmol/ml, respectively. Compounds 4e, 4g, and 4n were found to be most active. Furthermore, the binding conformation of the most active compounds was ascertained by docking studies. |
| Databáze: | OpenAIRE |
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