Praziquantel analogs with activity against juvenile Schistosoma mansoni |
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| Authors: | Yuxiang Dong Jacques Chollet Mireille Vargas Nuha R Mansour Quentin Bickle Yazen Alnouti Jiangeng Huang Jennifer Keiser Jonathan L Vennerstrom |
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| Institution: | 1. University of Nebraska Medical Center, College of Pharmacy, 986025 Nebraska Medical Center, Omaha, NE, USA;2. Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland;3. Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, United Kingdom |
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| 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 had no effect on the motility of adult S. mansoni in ex vivo culture. Cytochrome P450 metabolic stability data support the hypothesis that the major trans-cyclohexanol metabolite of praziquantel plays an important role in the antischistosomal activity of this drug. |
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