Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, PR China.
Bioorg Med Chem. 2013 Jul 15;21(14):4158-69. doi: 10.1016/j.bmc.2013.05.007. Epub 2013 May 16.
A series of novel hybrids of metronidazole and berberine as new type of antimicrobial agents were synthesized and characterized by (1)H NMR, (13)C 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.
一系列新型甲硝唑和小檗碱的杂合体作为新型抗菌剂被合成并通过 (1)H NMR、(13)C NMR、IR、MS 和 HRMS 图谱进行了表征。生物活性测定表明，大多数制备的化合物表现出有效的抗菌和抗真菌活性，一些化合物对耐甲氧西林金黄色葡萄球菌的活性与参考药物诺氟沙星、氯霉素和小檗碱相当或更高。还评估了人血清白蛋白 (HSA) 向高活性化合物 5g 的转运行为，并表明咪唑衍生物 5g 与 HSA 的结合是自发的，静电相互作用在 HSA 向 5g 的转运中起着重要作用。计算参数表明，化合物 5g 可以有效地被 HSA 储存和携带。
