摘要
Decoquinate（1）, an old and inexpensive coccidiostat, exhibited potent antimalarial activity, however, its antischistosomal activity against Schistosoma japonicum has not yet been evaluated. Based on decoquinate, a series of decoquinate derivatives was designed, synthesized, evaluated as a new class of antischistosomal agents against S. japonicum adult worms in vitro. Among them, compound 15 killed 100% of adult S. japonicum in 72 h at the concentration of 10 mmol/L in vitro, exhibited stronger wormkilling activity than PZQ in vitro and could serve as a promising lead compound to develop new antischistosomal agents.
Decoquinate（1）, an old and inexpensive coccidiostat, exhibited potent antimalarial activity, however, its antischistosomal activity against Schistosoma japonicum has not yet been evaluated. Based on decoquinate, a series of decoquinate derivatives was designed, synthesized, evaluated as a new class of antischistosomal agents against S. japonicum adult worms in vitro. Among them, compound 15 killed 100% of adult S. japonicum in 72 h at the concentration of 10 mmol/L in vitro, exhibited stronger wormkilling activity than PZQ in vitro and could serve as a promising lead compound to develop new antischistosomal agents.
基金
supported by Laboratory Research Fund funded by Key Laboratory of National Health and Family Planning Commission on Parasitic Disease Control and Prevention,Jiangsu Provincial Key Laboratory on Parasite and Vector Control Technology,Parasitic Disease Prevention and Control Platform(No.WK014-002)
fund from the Department of Science and Technology of Jiangsu Province(No.BY2016022-37)
fund from the National Natural Science Foundation of China(Nos.21472069,30972581,8120316)
fund from the Natural Science Foundation of Jiangsu Province(Nos.BK2012544,BK20151120)
fund from the scientific research projects of Jiangsu Provincial Commission of Health and Family Planning(No.H201635)
fund from the scientific research projects of Wuxi City Commission of Health and Family Planning(No.Q201656)
fund from the Ministry of Education of China(No.JUSRP51516)
Jiangsu Science and Technology Department(No.BM2015024)
