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合成了14种未见文献报道的N~2 -芳基三嗪酰基氨苄青霉素,其中有9种化合物对葡萄球菌有较好活性(MIC=1～5μg/ml);有 8种化合物对绿脓杆菌稍有活性(MIC=50～100μg/ml)。利用HPLC法测定了这14种化合物的油水分配系数。并用已知logp六种芳胺做对照考察logk＇与logp的关系。用logk＇代替logp对这14种化合物的logk＇与其对葡萄球菌和绿脓杆菌的抑菌活性1/C之间的关系进行了探讨。结果表明,这些化合物的logk＇与其对葡萄球菌抑菌活性1/C的关系基本上呈抛物线形式,即当logk＇增大时抑菌活性也随之增强,但logk＇增大至一定值时抑菌活性反而降低; logk＇与绿脓杆菌活性的关系基本上呈下斜线形式,即化合物的logk＇逐渐增大时其活性大为降低。
Fourteen kinds of N ~ 2 - aryl triazine acyl ampicillin were synthesized. Among them, 9 kinds of compounds showed good activity against Staphylococcus aureus (MIC = 1 ~ 5μg / ml) Bacilli is slightly active (MIC = 50-100 μg / ml). The oil-water partition coefficients of these 14 compounds were determined by HPLC. Six known aromatic amines were used as controls to investigate the relationship between logk ’and logp. The relationship between logk ’of these 14 compounds and their antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa, 1 / C, was investigated using logk’ instead of logp. The results showed that the relationship between logk ’of these compounds and their antibacterial activity against Staphylococcus aureus 1 / C was basically a parabola, that is, when the logk’ was increased, the antibacterial activity was also enhanced. However, when the logk ’was increased to a certain value But the antibacterial activity decreased. The relationship between logk ’and Pseudomonas aeruginosa activity was basically in the form of a downward sloping line, that is, the activity of logk’ was greatly decreased when the logk ’of the compound increased gradually.