Synthesis And Biological Evaluation Of 2-Aminothiazole Derivatives

2-Aminothiazole derivatives are important intermediates for the synthesis of many anti-bacterial drug, anti-inflammatory drug, anti-tumor drug, anti-viral drugs and active natural products, which exist in a large number of bioactive natural products. The structure of a variety of marketed drugs containing 2-amino-thiazole ring, such as famotidine, cefdinir, meloxicam and the like. In addition, 2-aminothiazole derivatives are also important fine chemical raw materials and chemical intermediates, and play a significant role in the fields of perfumes, dyes and pesticides.This thesis used two different routes to concisely and efficiently synthesize fifty types of 2-amino-thiazole derivatives through the key reactions of Hantszch thiazole synthesis, Suzuki coupling, etc., and evaluated their antibacterial and anti-tumor activities. The results showed that most of the 2-amino-thiazole derivatives have a good inhibitory effect on A549 human lung cancer cells and non-small cell rat adrenal pheochromocytoma cells PC-12, especially the compound vii-14,vii-21,vii-25,vii-27,vii-29 and vii-43, etc. And their activities were better than the control drug BI6727. The structure-activity relationship of the compounds were summarized in this thesis in order to further optimize the structure and evaluate other pharmacological activity.