Synthesis And Biological Activity Screening Of Nitazoxanide And Its Derivatives

Heterozygous drugs, which connect two different mechanisms of action of drugs via a covalent bond to form a stable, can have the dual role of the drug. The past ten years, researchers had begun to carry out a lot of their research work. The research on heterozygous drugs were very complex, with the unremitting efforts of scientists, hybrid drug research and development work has made significant progress, the world has developed a lot of these drugs and entered the stage of clinical trials.Nitazoxanide is first successfully synthesized by Jean-Francois Rossignol and Raymond Cavier team from France. It has a wide range of anti-parasitic actions, and it also possesses some other effects such as anti-bacteria, anti-virus, etc. Nitazoxanide which possesses a wide range of resistance is commonly used in the field of medicine.Artemisinin was first discovered by Tu Youyou team from China Academy of Chinese Medical Sciences. Artesunate as a water-soluble derivative of artemisinin also has a highly effective anti-malarial action. With the increase of resistance to antimalarial drugs in plasmodium, artemisinin and its derivatives becomes more and more attractive in the global medical circle.Nitazoxanide is a lead compound for screening the compound structures of Nitazoxanide and artesunate by computer simulation methods. With nitazoxanide as a basic molecule, we obtained artesunate- nitazoxanide hybrid molecule by esterification and obtained Artesunate-glycine-nitazoxanide hybrid molecule by esterification and amidation. The structure of the two novel compounds were identified by the application of 1H-NMR, 13C-NMR, MS, IR and UV. And the two novel compound shows a good bactericidal activity tested by the bacteriostatic circle experiment of golden staphylococcus and a good Antiparasitic activity tested by the zoopery of mouse.