Synthesis And Biological Activity Of Triazole Derivatives Containing Piperazine

Cancer is one of the most dangerous diseases that endanger human beings. And it is one of the main fields of new drug research to seek for a new anti-tumor drug,which has higher activity and lower toxicity. This article profits from the anti-tumor medicine Taxus structure modification of ideas,which have been open to the public patent anti-tumor medicine Diphenyltriazol, and preliminary testing of biological activity. After three steps of the modification, got three better anti-tumor activity of compounds.This dissertation includes the following aspects such as:1. Triazole compounds on the history and current situation, pharmacological activity, QSAR and the use of the study were reviewed. Take the triazole class compound Diphenyltriazol as the object of study. In view of the Diphenyltriazol fat soluble oversized characteristic. I had determined the balance distribution coefficient for structure finishing's goal, with a view to obtaining better anti-tumor activity of compounds.2. Select 4-amino-5-substitute for the even triazole-3-mercaptan and piperazine synthesized from a series of piperazine double triazole compounds were replaced, after anti-tumor cell activity in vitro screening, found the activities of compounds in this series were poor, poor solubility.3. Reduces in the member the proportion of Hydrophobic groups, synthesized a series of single-triazole compounds, underwent in vitro antitumour cell activeness screening, discovered that this series compound solubility was good, but activeness was still bad.4. Took on some of the compounds two series of caused Schiff-bases, a preliminary test of biological activity, the activity was better. The results show that, by design, synthesis of compounds with potential development prospects.5. It was showed in this thesis that 40 compounds have been prepared, including 35 not reported in the literature.