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Studies on antiparasitic agents part 10. synthesis of 2 substituted 5 6 arylthiosulfonobenzimidazoles as potential anthelmintics



Studies on antiparasitic agents part 10. synthesis of 2 substituted 5 6 arylthiosulfonobenzimidazoles as potential anthelmintics



Indian Journal of Chemistry Section B Organic Chemistry Including Medicinal Chemistry 28(5): 397-402



2-Substituted 5(6)-arylthiobenzimidazoles (9, 10, 13-25) and 2-substitutedamino-5(6)-arylsulphonobenzimidazoles (11, 12, 26-28) have been synthesized starting from 2-amino-5(6)-phenylthiobenzimidazole (8) and evaluated for their anthelminitic activity against Ancylostoma ceylanicum, Nippostrongylus brasiliensis, Hymenolepis nana, Litomosoides carinii, Dipetalonema viteae and Brugia malayi in rodents. Compounds 8, 9, 20, 21, 23 and 24 causes 100% elimination of the hookworms. A. ceylanicum from hamsters at a single oral dose of 100-250 mg/kg. Compound 9 has also been found to be effective in killing 100% of the microfilariae and adult worms of L. carinii from cotton rats at an intraperitoneal dose of 30 mg/kg given for 5 days.

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