头孢菌素类抗生素的合成研究

合成了未见文献报道的10种N~2-芳基三嗪酰基头孢氨苄和6种N~2-芳基三嗪酰基头孢羟氨苄,经元素分析、红外光谱、~1氢核磁共振光谱和质谱测定确定了它们的化学结构。用四种革蓝氏阳性细菌和阴性细菌初步测定了它们的最小抑菌浓度。用HPLC法测定了这16种化合物的油水分配系数,探讨了这些化合物的化学结构与其抗菌活性之间的关系。

SYNTHETIC STUDIES OF THE CEPHALOSPORIN ANTIBIOTICS

We have synthesized sixteen N~2-aryltriazine-carbonyl cephalosporin derivatives, which hitherto have not been reported in the literatures. The chemical structure of these compounds were determined by elementary analysis, IR,~1H-NMR, and Mass spectra. The Partition coefficient of these compounds were measured by means of the HPLC. The preliminary test of antibacterial activity against four species of bacteria in vitro showed that among the eight out of these new derivatives of cephalosporin have certain activity against Staphylococcus aureus. The relationship between partition coefficient and the antibacterial activity of these cephalosporin derivatives was also discussed.