Studies in enteric anthelmintics: activity profile of prodrug of a bisbenzimidazole [1].
The comparative anthelmintic activity of a possible prodrug, 2,2'-dicarbomethoxyamino-5,5'-dibenzimidazolyl methanol (2) with its parent compound 2,2'-dicarbomethoxyamino-5,5'-dibenzimidazolyl ketone (1) and the reference drug mebendazole (3a) is reported. At a dose of 25 mg/kg, compound 2 was 100% effective against Ancylostoma ceylanicum in hamsters. Compound 2 also exhibited a similar order of activity against Syphacia obvelata, Hymenolepis nana and H. diminuta at a dose of 100 mg/kg. The drug exhibited lethal effects against metamorphic forms of A. ceylanicum at a dose of 100 mg/kg. However the trichostrongylids, Nippostrongylus brasiliensis remained unaffected up to a dose of 250 mg/kg of 2. Both 1 and 3a exhibited inferior activity than 2 except against adult A. ceylanicum. The activity of 1 and 2 has been explained on the basis of their ability to resist systemic hydrolysis resulting in higher concentration of the active drug in biophase.
Khan
A M
AM
Parasitology Division, Central Drug Research Institute, Lucknow, India.
Gupta
S
S
Katiyar
J C
JC
Singh
S K
SK
Sharma
V L
VL
Sharma
S
S
Bhaduri
A P
AP
D000818:Animals; D000871:Anthelmintics / Q000627:therapeutic use*; D006224:Cricetinae; D006373:Helminthiasis / Q000188:drug therapy; D006376:Helminths / Q000302:isolation & purification; D008463:Mebendazole / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D051379:Mice; D011355:Prodrugs / Q000627:therapeutic use*; D051381:Rats
D000871:Anthelmintics; D011355:Prodrugs; D008463:Mebendazole