3-O-烷基格兰地新同系物的合成及抗菌活性研究

Synthesis and Evaluation Antimicrobial Activity of 3-O-alkygroenlandicine Homolog

通过在格兰地新3位引入不同的烷基合成了3个新的化合物,对目标产物利用质谱(MS)和核磁共振谱(NMR)进行结构表征,通过倍半稀释法进行了其进行了抗菌活性评价,进行初步的构效关系研究。衍生物抗菌活性明显提高,其中3-O-月桂基格兰地新对金黄色葡萄球菌的MIC为15.62μg/m L和对枯草杆菌MIC为15.62μg/m L。引入不同长度的碳链可以改善格兰地新的亲脂性有助于提高格兰地新的抗菌活性,其中3-O-月桂基格兰地新的抗菌活性最好。

By introducing different alky at the C-3 position of groenlandicine,a series of groenlandicine homolog were synthesized and identified by MS,1 H NMR and13 C NMR. Antimicrobial activity was evaluated by two-fold serial dilution test in vitro to study the preliminary structure-activity relationships. The antimicrobial of the new derivatives increased obviously,3-O-decynyl groenlandicine showed good antimicrobial with MIC value of 15. 62 μg/m L against S.aureus and 15. 62 μg/m L against B. subtilis respectively. Introducing different alky at the C-3 position of groenlandicine could improve their antibacterial activities due to the enhanced hydrophilicity. 3-O-decynyl groenlandicine showed the greatest antimicrobial activities.