新型阳离子卟啉的设计合成与抗微生物活性.docVIP

新型阳离子卟啉的设计合成与抗微生物活性 于克贵2, 李东红1, 周成合（西南大学化学化工学院重庆 400715）摘 要:。方法 由缩合反应得到的四吡啶卟啉与一系列苄卤反应得到10个新型的阳离子卟啉化合物；采用琼脂双倍稀释法考查上述化合物对金葡菌、大肠杆菌、绿脓杆菌和白色念珠菌的光动力抑菌活性。结果 10个化合物对革兰氏阳性金葡球菌均表现出显著的光抑制作用，尤其是化合物3a、4a的MIC80分别为2 和0.5 μg/mL；对真菌白色念珠菌也有一定的抑菌活性；而对革兰氏阴性大肠杆菌的抑制作用较低，绿脓杆菌表现出对所有化合物的耐药性。阳离子卟啉的光抑菌活性随苯环上取代基吸电子能力的增强而降低。结论关键词Study on the synthesis and antimicrobial activity of novel cationic porphyrins YU Ke-gui2，LI Dong-hong 1( , ZHOU Cheng-he2, DIAO Jun-lin 1 (1. State Key Laboratory of Trauma, Burn and Combined Injury, the 2nd Department of Research Institute of Surgery, Dapin Hospital, Third Military Medical University, Chongqing, 400042, China；2. School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715, China) Abstract: Objective To investigate the photodynamic antimicrobial activities of cationic porphyrin derivatives and their metal compounds. Methods Tetrapyridyl-porphyrin obtained from condensation reaction reacted with a series of benzyl halides to get ten novel cationic porphyrin compounds; their photodynamic antimicrobial activities in vitro against S. aureus, E.coli, P.aeruginosa, and C.albicans were evaluated using twofold serial dilution technique. Results All these ten compounds displayed satisfactory photodynamic antibacterial activity against Cram positive bacteria S. aureus, especial compounds 3a, 4a with the value of MIC80 of 2 and 0.5 礸/mL respectively, aand moderate antifungal activity against C. albicans. Unfortunately, their photodynamic antibacterial activities against Cram negative bacteria E.coli were very weak, and P. aeruginasa was resistant to all compounds. The antimicrobial activity decreased with the increase of electron-withdrawing capability of the functional groups attached on the aromatic ring. Conclusion These preliminary results suggested that the remarkable antibacterial efficiency against S.aureus makes these substances promising microbial agents. Key words: cationic porphyrin; Synthesis; antimicrobial activity; Cram po