Wen-Hua F
China
Research Article
Synthesis and SAR Studies of New Oxadiazole-2-oxide Derivatives with
Remarkable In Vitro Activity against Schistosoma japonicum
Author(s): C M A Gause M, Wen-Hua F, Li-Jun S, Chuan-Xin Y and Bainian FC M A Gause M, Wen-Hua F, Li-Jun S, Chuan-Xin Y and Bainian F
Schistosomiasis is the most neglected tropical disease in the world now where every day more and more people are being affected. The only approved drug Praziquantel (PZQ) that could not prevent re-infection but only effective against adult worms. Resistance of PZQ has been found in some areas, so an alternative drug would be needed as a substitute. Oxadiazole-2-oxide has been proven as potential anti schistosomal agents in which they kill both adult and juvenile worms. We synthesized 25 novel oxadiazole-2-oxide analogues and check their in vitro activity on adult Schistosoma japonicum. In here, all of them showed better in vitro activity than praziquantel and 1, 2, 5-oxadiazole- 2-oxide. Compounds 16, 17, 20, 23 and 24 showed excellent activity even in low concentration and short time period. There are no differences found while checking their in vitro activity against male and female.. View More»
DOI:
10.4172/1948-5948.1000339