Synthesis and pharmacological evaluation of novel coumarin based triazolyl glycoconjugates as potential antibacterial and anti-proliferative agents

AbstractA library of novel coumarin-based triazolyl glycoconjugates is prepared and screened for in vitro antibacterial activity against Gram-positive (Bacillus megaterium) and Gram-negative bacteria (Escherichia coli)via disc diffusion technique in the current study. The biological assays revealed significant antibacterial potential of new synthetic coumarin triazolyl glycoconjugates, compound5d being the most active one with zones of inhibition (mm) of 34.33  ± 0.88 (10 μg/mL) and 36.66 ± 0.88 (20 μg/mL) againstE. coli and 17.66  ± 1.20 (10 μg/mL) and 20 ± 1.15 (20 μg/mL) againstB. megaterium. The activity was found comparable to the reference drugs chloramphenicol [36.33  ± 0.88 (10 μg/mL), 38.66 ± 0.88 (20 μg/mL) againstE. coli and 25  ± 0.57 (10 μg/mL), 25.33 ± 0.66 (20 μg/mL) againstB. megaterium] and ampicillin [32.33  ± 1.71 (10 μg/mL), 34.66 ± 2.40 (20 μg/mL) againstE. coli and 20.33  ± 1.85 (10 μg/mL), 23.66 ± 2.33 (20 μg/mL) againstB. megaterium]. The coumarin-based triazole analog5e also displayed selective but moderate antiproliferative activity (growth inhibition ~ 23%) against leukemia cell lines when screened against 60 cancer cell lines at National Cancer Institute, USA. The study leads to the identification of several novel coumarin based compounds with dual anti-proliferative and antibacterial activity profile.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research