Synthesis and anthelmintic activity of 2,2'-disubstituted 5,5'-dibenzimidazolylsulfides and sulfones.
A number of substituted diphenylsulfides and sulfones (4-11) and 2,2'-disubstituted-5,5'-dibenzimidazolyl sulfides and sulphones (12-19) have been synthesized starting from 5-chloro-2-nitroacetanilide and (3) 4,4'-dichlorodiphenyl sulfone (9), respectively. Among the compounds tested against Ancylostoma ceylanicum in hamsters and Hymenolepis nana in rats and mice, 14, 15, 18 and 19 removed 100% of the worms at an oral dose of 25 mg/kg X 1 to 250 mg/kg X 3. Some of the compounds were tested for their blood schizontocidal activity against Plasmodium berghei in mice but none showed any activity up to an oral dose of 10 mg/kg given for 6 days.
D000723:Ancylostomatoidea / Q000187:drug effects; D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D002589:Cestoda / Q000187:drug effects; D006224:Cricetinae; D004353:Drug Evaluation, Preclinical; D005260:Female; D008297:Male; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D013440:Sulfides / Q000138:chemical synthesis / Q000494:pharmacology; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology
D000871:Anthelmintics; D001562:Benzimidazoles; D013440:Sulfides; D013450:Sulfones