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A series of coumarin-derived azolyl ethanols including imidazolyl,triazolyl,tetrazolyl,benzotriazolyl,thiol-imidazolyl and thiol-triazolyl ones were conveniently synthesized and characterized by IR,~1H NMR,~(13)C NMR and high-resolution mass spectra(HRMS) spectra.Some of the prepared compounds showed appropriate logP_(ow) values and effective antibacterial and antifungal activities.Noticeably,compound 14 with bis-triazolyl ethanol group exhibited low minimal inhibitory concentration(MIC)value of 8 μg/mL against MRSA,which was comparable or even superior to reference drugs Norfloxacin(MIC=8μg/mL)and Chloramphenicol(MIC=16μg/mL).It could also effectively inhibit the growth of the tested fungal strains compared to Fluconazole.Further binding studies of coumarin 14 with calf thymus DNA were investigated by UV-Vis absorption and fluorescence spectroscopy.It was found that compound 14 could interact with calf thymus DNA by groove binding to form14-DNA complex via both hydrogen bonds and van der Waals force,which might be the factor to exert the powerful antimicrobial activity.
A series of coumarin-derived azolyl ethanols including imidazolyl, triazolyl, tetrazolyl, benzotriazolyl, thiol-imidazolyl and thiol-triazolyl ones were produced by IR, ~ 1H NMR, 13C NMR and high-resolution mass spectra ( HRMS) spectra. Some of the prepared compounds showed appropriate logP_ (ow) values and effective antibacterial and antifungal activities. Notably, compound 14 with low inhibitory concentration (MIC) value of 8 μg / mL against MRSA, which was comparable or even superior to reference drugs Norfloxacin (MIC = 8 μg / mL) and Chloramphenicol (MIC = 16 μg / mL) .It could also practically inhibit the growth of the tested fungal strain compared to Fluconazole. calf thymus DNA were investigated by UV-Vis absorption and fluorescence spectroscopy. It was found that compound 14 could interact with calf thymus DNA by groove binding to form 14-DNA complex via both hydrogen bonds and v an der Waals force, which might be the factor to exert the powerful antimicrobial activity.