摘要
合成了二十个未见文献报道的N^2-芳基三嗪酰基头孢烯酸和N^2-芳基三嗪酰基-3-氮杂环硫甲基头孢菌素衍生物,经元素分析、IR和~4H-NMR等数据的测定,证实了它们的化学结构,运用HPLC法测定和计算了化合物的油水分配系数,初步探讨了油水分配系数P与抗菌活性之间的关系;测定了二十个化合物对二十种革兰氏阳性和阴性菌的最小抑菌浓度(MICμg/ml),其中化合物C_1、C_2、C_3、C_4、C_5所对应的二钠盐JLP15、16、17、18、19具有一定的广谱特征,特别是对青霉素耐药菌株和甲氧西林耐药菌株都显示了一定的活性。
We have synthesized twenty N2-aryltriazineearbonyl cephalosporin derivatives, which have not been reportedin the literatures. Their chemical strutures were determined by elementary analysis, 1H-NMR and IR. The partition coefficient of these compounds were measured by HPLC. The result of the initial test of the antibacterial activity against twenty species of bacteria in vitro showed that compounds JLP15, 16.17,18 and 19 have a rather broad activity agamst StaPhylococcus aureus and Pseudomor.as aeruginosa 42. The structural requirements which influenced antibacterial activity were aslo discussed.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
1991年第4期256-265,共10页
Chinese Journal of Antibiotics
关键词
头孢菌素
油水分配系数
抗菌活性
N2-arytriazine-carbonyl cephalosporin
HPLC
Partition coefficie-at
Antibacterial activity
