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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。
Twenty non-reported N ~ 2-aryl triazine acyl cephemics and N ~ 2-aryl triazine acyl-3-azacyclopentadienyl cephalosporin derivatives were synthesized and characterized by elemental analysis , IR and ~ 4H-NMR data. The chemical structures of these compounds were confirmed. The oil-water partition coefficients were determined and calculated by HPLC. The relationship between oil-water partition coefficient P and antibacterial activity was discussed. The minimum inhibitory concentration (MICμg / ml) of ten compounds against twenty Gram positive and negative bacteria, among them, the disodium salt JLP15,16,17,18, which corresponds to the compounds C_1, C_2, C_3, C_4 and C_5, 19 has a certain broad spectrum of characteristics, especially for penicillin-resistant strains and methicillin-resistant strains showed some activity.