微生物および生化学技術ジャーナル

概要

Synthesis and SAR Studies of New Oxadiazole-2-oxide Derivatives with Remarkable In Vitro Activity against Schistosoma japonicum

C 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 worms. Some new functional groups would be synthesized here may lead us to the new treatment of schistosomiasis. The synthesis and structure activity relationship (SAR) studies of oxadiazole-2-oxide analogues with activity against S. japonicum can help us to design some more new derivatives to find out better activity and potential candidate. Some of these compounds could be used to develop new anti-schistosomal drugs while the mechanism of these compounds still needs to found.