Praziquantel analogs with activity against juvenile Schistosoma mansoni

…, Y Alnouti, J Huang, J Keiser, JL Vennerstrom

Index: Dong, Yuxiang; Chollet, Jacques; Vargas, Mireille; Mansour, Nuha R.; Bickle, Quentin; Alnouti, Yazen; Huang, Jiangeng; Keiser, Jennifer; Vennerstrom, Jonathan L. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 8 p. 2481 - 2484

Full Text: HTML

Citation Number: 40

Abstract

Six amide and four urea derivatives of praziquantel were synthesized and tested for antischistosomal activity against juvenile and adults stages of Schistosoma mansoni in infected mice. Only one of these had significant activity against adult worms, but, unlike praziquantel, six of these had low to modest activity against juvenile worms. A praziquantel ketone derivative had the best combination of activity against juveniles and adults, but it ...