STUDY ON DRUGS AGAINST HYDATIDOSIS:SYNTHESIS OF METABOLITES AND ANALOGUES OF ALBENDAZOLE
Li Huang
Abstract
Li Huang
Abstract
Twenty-five metabolites and analogues of albendazole were synthesized for screening drugs against Echinococcus granulosus cysts in mice and their biological activities were compared.The results of preliminary screening tests showed that compounds 4,5,7,8,11,13,and 20 exhibited better effects against hydatidosis in mice.Among them,albendazole sulfoxide(13)was more effective than the others including albendazole even administered at a half dose of the latter.Nevertheless,an other major metabolite,albendazole sulfone,possessed no effect.
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Twenty-five metabolites and analogues of albendazole were synthesized for screening drugs against Echinococcus granulosus cysts in mice and their biological activities were compared.The results of preliminary screening tests showed that compounds 4,5,7,8,11,13,and 20 exhibited better effects against hydatidosis in mice.Among them,albendazole sulfoxide(13)was more effective than the others including albendazole even administered at a half dose of the latter.Nevertheless,an other major metabolite,albendazole sulfone,possessed no effect.
Key concepts: Albendazole, Echinococcus granulosus, Chemistry, Metabolite, Pharmacology, Echinococcosis, Chromatography, Biochemistry