Design, Synthesis, Characterization and antibacterial activity of new 1,2,3-triazole linked nucleosides

Abstract

Sixteen new 1-aryl-1,2,3-triazole linked nucleosides (7a-7i, 8a-8 g) were designed and synthesized by using Copper (I)-catalysed Huisgen-Sharpless-Meldal 1,3-dipolar cycloaddition reaction of propargylated nucleoside with substituted fluoro aryl azides in good yields. All compounds (7a-7i, 8a-8 g) were characterized by analysis their 1H NMR, 13C NMR, 2D-NMR and mass spectral data. Compounds were screened in vitro for their antibacterial activity against Xanthomonas citri pv. malvacearum, Ralstonia solanacearum, Bacillus siamensis and Pseudomonas aeruginosa. All the synthesized compounds exhibited antibacterial potential against four bacterial strains in the range of 0.318 mm to 3.596 mm. On the basis of zone of inhibition, potential of compounds against bacteria was assessed by determining the MIC value of three compounds. The results indicated that three compounds 7f, 7 g and 8f were found effective even at minimal concentration of 2 µg/ml. Therefore development of such type of new antibacterial agents is the need of time in order to overcome the problem of resistance and modification may lead to the development of new antibacterial agents.

Keywords

• 1,2,3-triazole
• Nucleosides
• 1,3-dipolar cycloaddition
• Antibacterial-activity