Synthesis of epoxypropyloxy chromones and allyl hydroxy chromones and in vitro-in vivo activity on protoscoleces of Echinococcus multilocularis (Cestoda).
Derivatives with epoxypropyloxy, allyloxy and allyl hydroxychromone structures were synthesized and tested against protoscoleces of Echinococcus multilocularis. Compounds IV-IX were tested in vitro and compound VII proved the most active of them with, at 0.1 mmol.L-1, 98% dead protoscoleces in open vesicles after 24 hours and 80% in closed vesicles within 96 hours. Compound VII was tested in vivo on Meriones unguiculatus infested by Echinococcus multilocularis, but was found to be rather inactive.
Faculté des Sciences Pharmaceutiques et Biologiques, Université de Lille II 3, France.
B
B
Haddad
G
G
Bethegnies
A
A
Marcincal-Lefebvre
T
T
Duriez
D
D
Afchain
P
P
Thuillier
D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D002867:Chromones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D004443:Echinococcosis / Q000188:drug therapy* / Q000469:parasitology; D004446:Echinococcus / Q000187:drug effects*; D004852:Epoxy Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D005260:Female; D005849:Gerbillinae; D007814:Larva / Q000187:drug effects; D008297:Male; D051379:Mice
D000871:Anthelmintics; D002867:Chromones; D004852:Epoxy Compounds