Yun-Lei Luo, Kishore Baathulaa, Vijaya Kumar Kannekanti
Jan 20, 2015
Citations
1
Influential Citations
45
Citations
Journal
Science China Chemistry
Abstract
A novel series of benzimidazole derived naphthalimide triazoles and some corresponding triazoliums have been successfully synthesized and characterized by 1H NMR, 13C NMR, 1H-1H COSY, IR and HRMS spectra. All the new compounds were screened for their antimicrobial activities in vitro by two-fold serial dilution. 2-Chlorobenzyl triazolium 8g and compound 9b with octyl group exhibited the best antibacterial activities among all the tested compounds, especially against S. aureus with inhibitory concentration of 2 μg/mL which was equipotent potency to Norfloxacin (MIC=2 μg/mL) and more active than Chloromycin (MIC=7 μg/mL). Triazoliums 8g and 8f bearing 3-fluorobenzyl moiety displayed the best antifungal activities (MIC=2−19 μg/mL) against all the tested fungal strains without being toxic to PC12 cell line within concentration of 128 μg/mL. Further investigations by fluorescence and UV-Vis spectroscopic methods revealed that the compound 8g could effectively intercalate into calf thymus DNA to form the 8g-DNA complex which could block DNA replication, exerting powerful antimicrobial activities.