EXPERIMENTAL AND THEORETICAL-STUDIES OF ALBENDAZOLE, OXIBENDAZOLE, AND TIOXIDAZOLE

An investigation of the therapeutic effectiveness of albendazole (ABZ, methyl 5-[propylthio]benzimidazole-2-carbamate), oxibendazole (OBZ, methyl 5-[n-propoxy]benzimidazole-2-carbamate), and tioxidazole (TIOX, methyl 6-[n-propoxy]benzothiazole-2-carbamate) against Hymenolepis diminuta in experimentally infected rats is reported. All of the anthelmintics tested were effective therapeutically as a single oral dose against adult tapeworms, however, at different dose levels. The rank order of in vivo anthelmintic potency was ABZ > OBZ > TIOX. Molecular modeling revealed that drug efficacy depends on the orientation of the propyl group at position 5 on the heterocyclic ring system and on the magnitude of the molecular dipole moment.