双、三及四（二氢咖啡酰）多胺共轭物作为抗耐万古霉素金黄色葡萄球菌抗菌剂的合成
Synthesis of bis, tris and tetra(dihydrocaffeoyl)polyamine conjugates as antibacterial agents against VRSA.
作者信息
Yingyongnarongkul Boon-ek, Apiratikul Nuttapon, Aroonrerk Nuntana, Suksamrarn Apichart
机构信息
Department of Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkapi, Bangkok, 10240, Thailand.
出版信息
Arch Pharm Res. 2008 Jun;31(6):698-704. doi: 10.1007/s12272-001-1215-4. Epub 2008 Jun 19.
Bis, tris and tetra(dihydrocaffeoyl)polyamine conjugates were synthesized using solid phase synthesis technique. These compounds were screened for antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) (11 strains) and vancomycin-resistant S. aureus (VRSA) (4 strains). Bis, tris and tetra(dihydrocaffeoyl)polyamine analogues showed antibacterial activity against VRSA which were better than the reference drugs, vancomycin. Tetra(dihydrocaffeoyl)polyamine conjugate exhibited the highest activity. These compounds showed no cytotoxicity against vero cells.
使用固相合成技术合成了双（二氢咖啡酰）多胺、三（二氢咖啡酰）多胺和四（二氢咖啡酰）多胺缀合物。对这些化合物针对耐甲氧西林金黄色葡萄球菌（MRSA）（11株）和耐万古霉素金黄色葡萄球菌（VRSA）（4株）的抗菌活性进行了筛选。双（二氢咖啡酰）多胺、三（二氢咖啡酰）多胺和四（二氢咖啡酰）多胺类似物对VRSA显示出抗菌活性，其活性优于参考药物万古霉素。四（二氢咖啡酰）多胺缀合物表现出最高活性。这些化合物对 vero 细胞无细胞毒性。
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