Praziquantel analogs with activity against juvenile Schistosoma mansoni.
Yuxiang Dong;
Jacques Chollet;
Mireille Vargas;
Nuha R Mansour;
Quentin Bickle;
Yazen Alnouti;
Jiangeng Huang;
Jennifer Keiser;
Jonathan L Vennerstrom;
(2010)
Praziquantel analogs with activity against juvenile Schistosoma mansoni.
Bioorganic & medicinal chemistry letters, 20 (8).
pp. 2481-2484.
ISSN 0960-894X
DOI: 10.1016/j.bmcl.2010.03.001
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.
| Item Type | Article |
|---|---|
| Keywords | Praziquantel, Antischistosomal, Schistosoma mansoni, antischistosomal drugs, synthetic trioxolanes, in-vitro, derivatives, enantiomers, mechanisms, future, ring |
| ISI | 276291500018 |