Coumarin-based 1,4-disubstituted 1,2,3-triazole derivatives were synthesized using a highly efficient, ecofriendly protocol via a copper(I)-catalyzed click reaction between various substituted arylazides and terminal alkynes. The synthetic route was easy to access and gave excellent yields under microwave irradiation conditions compared to the conventional heating route. The structures of all the compounds were characterized by IR, 1 H NMR, 13 C NMR spectroscopy and mass spectrometry. All the synthesized compounds were screened for their in vitro antimicrobial, antioxidant and anti-inflammatory activities; among all compounds, 8a, 8j, 8k and 8l exhibited better results with respect to standard drugs.Furthermore, molecular docking studies have been carried out with PDB IDs 2VCX (anti-inflammatory), 3VXI (antioxidant), 4GEE (antimicrobial) and 2XFH (antifungal) using the Glide module of the Schrödinger suite. The final compounds 8d, 8e, 8h, and 8k showed the highest hydrogen bond interactions with His-88 and Val-191 proteins and with water in all the proteins.
The synthesized benzimidazoles compounds were prepared from the condensation reaction between o-Phenylenediamine and various carbonyl compounds, in the presence of ammonium chloride as a catalyst. Ammonium chloride is a commercial and environmentally benign catalyst. The yield of all benzimidazole derivatives was found to be in the range of 75 – 94%. The purity of the compounds was ascertained by melting point and TLC. The synthesized compounds were characterized by using IR,1H NMR, and MASS spectral data together with elemental analysis. The synthesized benzimidazole compounds were screened for acute and chronic anti-anxiety activity in Wistar rats by using an elevated plus maze model with standard Diazepam. The synthesized compounds ZB, ZE, ZF, ZG, and ZH showed potent anti-anxiety activity when compared to the standard Diazepam. The compound ZH exhibited a higher anti-anxiety activity when compared to other prepared benzimidazoles. The results were subjected to statistical analysis by using one-way ANOVA followed by the Tukey-Kramer test, to calculate the significance.
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