Synthesis and anthelminthic activity of alkyl-(5-acyl-1-H-benzimidazol-2-yl) carbamates.
A series of alkyl-(5-acyl-1-H-benzimidazol-2-yl)-carbamates were prepared and screened for anthelminthic activity. Some of them were found to be fully active at low, atoxic oral dose levels against gastro-intestinal nematodes. The activity against Symphacia muria and Strongyloides ratta is indicated. From these studies methyl (5-benzoyl-1-H-benzimidazol-2-yl) carbamate (mebendazole) and methyl [5-(4-flourobenzoyl)-1-H-benzimiazol-2 yl]carbamate flubendazole) were selected for detailed investigation.
D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000627:therapeutic use; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D008722:Methods; D010123:Oxyuriasis / Q000188:drug therapy; D010124:Oxyuroidea; D051381:Rats; D013322:Strongyloidiasis / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000871:Anthelmintics; D001562:Benzimidazoles