Synthesis and bioactive evaluation of novel hybrids of metronidazole and berberine as new type of antimicrobial agents and their transportation behavior by human serum albumin |
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Authors: | Ling Zhang Juan-Juan Chang Shao-Lin Zhang Guri LV Damu Rong-Xia Geng Cheng-He Zhou |
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Institution: | Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, PR China |
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Abstract: | A series of novel hybrids of metronidazole and berberine as new type of antimicrobial agents were synthesized and characterized by 1H NMR, 13C NMR, IR, MS and HRMS spectra. Bioactive assay manifested that most of the prepared compounds exhibited effective antibacterial and antifungal activities and some showed comparable or superior potency against Methicillin-resistant Staphylococcus aureus to reference drugs Norfloxacin, Chloromycin and Berberine. The transportation behavior of human serum albumin (HSA) to the highly active compound 5g was evaluated and revealed that the association of imidazole derivative 5g with HSA was spontaneous and the electrostatic interactions played important roles in the transportation of HSA to 5g. The calculated parameters indicated that compound 5g could be effectively stored and carried by HSA. |
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Keywords: | Imidazole Metronidazole Berberine Antibacterial Antifungal Human serum albumin |
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