高效液相色谱法测定双哌嗪双季铵盐药物的分配系数及对构效关系的考察

The Determination of Partition Coefficient of Dipiperazine Diquaternary Ammonium Derivatives by High Performance Liquid Chromatography and the Investigation on Its Structure-Activity Relationship

采用高效液相色谱法测定了１０种新合成的双哌嗪双季铵盐药物的油－水分配系数，并对其毒性及生物活性进行了测试。讨论了分配系数、毒性、活性及分子结构间的关系，找出了２个理想的先导药物。

In the present work, the partition coefficients of ten dipiperazine diquaternary ammonium derivatives 2Br Ⅱ]were determined by high performance liquid chromatography,and their toxicities and antitumor activites were tested. The results indicated that,(1) the greater the n and R in compound Ⅱ, the high toxicity and partition coefficient were; quaternary ammonium ion plays an important part in the adjustment of oil-water partition coefficient: these can guide us looking for compounds with better characteristics, (2)Ⅱ 3 (n=6, R=Me) and Ⅱ5 (n=6, R=Et), with middle partition coefficients, possess higher activities aganist carcinoma S37. From the way of synthesis, their activity and toxicity, Ⅱ 3 and Ⅱ5 are considered to be preferential compounds.