摘要/Abstract

基于查尔酮缩氨基胍衍生物的结构修饰，设计合成了一系列含联苯片段的缩氨基胍衍生物.目标化合物的结构通过¹H NMR、¹³C NMR和HRMS进行了确证，并评价了其抗菌活性.结果显示目标化合物对所选菌种显示出了较好的抑制活性，最低抑菌浓度值（MIC）大都在0.5～8 μg/mL.其中，2-（（4'-溴[1，1'-二苯]-4-基）亚甲基）肼-1-甲脒（3j）的抗菌活性最好，对所选菌株包括耐药菌均显示出强的抑菌活性，其中对金葡菌CMCC（B）26003、粪肠球菌CMCC 29212和多药耐药金葡菌ATCC 33591尤为敏感，最低抑菌浓度值达到0.5 μg/mL.此外，化合物3j表现低的细胞毒性，对正常人体细胞HEK 293T的IC₅₀值为60.90 μmol/L.该结果表明化合物3j具有较好的选择性，在抗菌药物研究领域具有研究价值.
关键词: 缩氨基胍, 联苯, 抗菌活性
A series of aminoguanidine derivatives containing a biphenyl moiety were designed, synthesized, and characterized by spectra methods using chalcone-aminoguanidine derivative as the lead compound. The antibacterial activity of the target compounds was evaluated. The results indicated that most of the target compounds showed potent inhibitory activity with the minimum inhibitory concentration values (MICs) in range of 0.5~8 μg/mL. Among of which, 2-((4'-bromo-[1,1'- biphenyl]-4-yl)methylene)hydrazine-1-carboximidamide (3j) exhibited broad-spectrum antibacterial activity, effective to all the chosen strains including two multidrug-resistant gram-positive strains, showed the most potent inhibitory against S. aureus CMCC(B) 26003, E. faecalis CMCC 29212 and multidrug-resistant S. aureus ATCC 33591 with a MIC value of 0.5 μg/mL. Moreover, low cytotoxicity of compound 3j (HEK 293T, IC₅₀=60.90 µmol/L) was found. These results suggested that the Compound 3j, with high safety, was potential and valuable in the research of novel antibacterial drugs.
Key words: aminoguanidine, biphenyl, antimicrobial activity


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