5-nitro-furan Derivatives Research Synthesis And Anti-schistosomiasis

According to the report of July2007, schistosomiasis is epidemic in76developing countries, whichinfects2million people rural and suburban areas.110counties(city, area) of China,such as Hunan, Hubei,Jiangxi, Anhui, Jiangsu, Sichuan, Yunnan and other provinces haven’t yet controlled the prevalent ofschistosomiasis. As reported,chronic schistosomiasis patients are0.81million, terminal schistosomiasispatients are twenty-six thousand and the threatened are ninety-nine million and thirty thousand. In Jiangxiprovince, there are11counties(city, area) that haven’t controlled the epidemic of schistosomiasis. Morethan90%schistosomiasis epidemic areas distribute in the counties and cities surrounding Poyang Lake, andpeople threatened by the disease are forty-five million and eighteen thousand. Praziquantel is a highefficient and broad-spectrum antiparasitic drugs, especially remarkable insecticidal effect to Schistosoma,along with low toxicity. However, with the widely and lasting use of praziquantel, issues of resistance andtolerance to drug have become increasingly prominent, and arouses great attention. At present, research onanti-schistosomiasis drugs has become hot.This thesis mainly contains three parts:PartⅠ: ReviewsThis part introduces and briefly summarizes a few kinds of anti-schistosomiasis drugs.Part II: The synthesis and anti-schistosomiasis research of2-imino-5-nitrofuransWe use ethanol as solvent, in the reflux condition,5-nitrofuran formaldehyde and arylamines react to getthe target compounds. And then,those synthetic2-imino-5-nitrofurans are used to conductanti-schistosomiasis activity experiment.Part Ш: The synthesis and anti-schistosomiasis research of5-nitrofuran amidesIn the reaction condition of tetrahydrofuran as solvent, DCC as dehydrating agent and condensationagent, HOBt as catalytic agent,5-nitrofuran formic acid and arylamines react to get the target compounds.Those synthetic2-imino-5-nitrofurans are used to conduct anti-schistosomiasis activity experiment.