Synthesis and in vitro activity of alkylaminoalkyloxy chromones on protoscoleces of Echinococcus multilocularis (Cestoda).
Twelve derivatives with alkylaminoalkyloxy chromone structures were synthesized and tested upon protoscoleces of Echinococcus multilocularis metacestode kept alive in vitro. Assays were performed with protoscoleces attached to the germinal layer in open and in closed vesicles. Compounds IVb and IIIe at the concentration of 0.1 mmol.L-1 killed 50% of the protoscoleces in open vesicles in 48 hours and compound IVb killed 100% of the protoscoleces in open vesicles within 96 hours at the same concentration. In closed vesicles after four days compound IVb killed all protoscoleces, compounds IIIe and IVd half of them, whereas in the controls all protoscoleces were alive. Trifluoperazine (TFP) was the reference compound; none of the new compounds showed better activity than TFP.
Haddad
B
B
Laboratoire de Chimie Organique, Université de Lille II, France.
Marcincal-Lefebvre
A
A
Duriez
T
T
Afchain
D
D
D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000494:pharmacology; D002867:Chromones / Q000138:chemical synthesis* / Q000494:pharmacology; D004446:Echinococcus / Q000187:drug effects*; D005849:Gerbillinae; D006801:Humans; D007814:Larva; D014268:Trifluoperazine / Q000494:pharmacology
D000871:Anthelmintics; D002867:Chromones; D014268:Trifluoperazine