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目标β-环糊精6位取代基链适当的“长度”及其较强的疏水性能提高其“内洞”与客体药物分子形成复合(包合)物的能力,使其药物分子能够得到充分保护。依据这种性能,化学合成了β-环糊精衍生物6-辛基胺基-6-去氧-β-环糊精盐酸盐(1)。方法通过核磁共振氢谱(1H-NMR)实验,对化合物1与β-内酰胺类抗生素哌拉西林所组成的复合物进行了研究。研究结果表明,哌拉西林分子中的β-内酰胺内核被嵌入化合物1分子的内洞中,从而使哌拉西林分子得到保护。结果哌拉西林与化合物1合用前后对耐甲氧西林金葡菌(MRSA)等9种细菌的抗菌作用进行了测定。测定结果显示,哌拉西林与化合物1合用前后对耐甲氧西林金葡菌的体外最低抑菌浓度(MIC)分别为>128μg/mL及4.0~8.0μg/mL。结论研究结果表明化合物1对哌拉西林体外抗耐甲氧西林金葡菌具有较强的抗菌活性恢复和增效作用。
The proper “length” of the 6-substituent chain of target β-cyclodextrin and its strong hydrophobicity improve the ability of its “inner hole” to form a complex (inclusion) with the guest drug molecule so that its drug The molecules can be fully protected. Based on this property, β-cyclodextrin derivative 6-octylamino-6-deoxy-β-cyclodextrin hydrochloride (1) was chemically synthesized. Methods The complexes of compound 1 with β-lactam antibiotics piperacillin were studied by 1H-NMR. The results show that the piperacillin molecule β-lactam core is embedded in the inner hole of compound 1 molecule, so that the piperacillin molecule is protected. Results The antibacterial activity of nine strains of bacteria, MRSA, before and after piperacillin and compound 1 were tested. The results showed that the minimum inhibitory concentrations (MICs) of methicillin-resistant Staphylococcus aureus before and after combination of piperacillin and compound 1 were> 128μg / mL and 4.0 ~ 8.0μg / mL, respectively. Conclusion The results show that compound 1 has a strong antibacterial activity recovery and synergistic effect against piperacillin against methicillin-resistant Staphylococcus aureus.