Antiamoebic activity of 3,3'-fluro-4,4'-di-(pyrrolidine-2-ylidene amino)-diphenyl (liroldine), against experimentally infected intestinal and hepatic amoebiasis.
HL 707, Liroldine, a novel synthetic compound, was found effective against both extraintestinal and intestinal amoebiasis in animal models. Its activity against hepatic infection in golden hamsters is comparable with that of different derivatives of nitroimidazoles used for human treatment. Against intestinal amoebiasis in Wistar rats, the activity was superior to nitroimidazoles and chloroquine. Paramomycin was comparable and diloxanide furoate was marginally superior. The comparative in vitro and in vivo studies with standard marketed drugs and Liroldine indicate an excellent profile of the compound against experimental amoebiasis. LD50 of Liroldine determined in mice is 910 mg/kg x 1, po and 940 mg/kg x 1 ip).
Chatterjee
D K
DK
Department of Experimental Biology, Hoechst Marion Roussel Ltd., L.B.S. Marg, Mulund (West), Mumbai, India.
Iyer
S N
SN
Venugopalan
B
B
Raether
W
W
D000562:Amebiasis / Q000188:drug therapy*; D000563:Amebicides / Q000627:therapeutic use*; D000818:Animals; D001713:Biphenyl Compounds / Q000627:therapeutic use*; D006224:Cricetinae; D006801:Humans; D007411:Intestinal Diseases, Parasitic / Q000188:drug therapy*; D008109:Liver Diseases, Parasitic / Q000188:drug therapy*; D008647:Mesocricetus; D051379:Mice; D008826:Microbial Sensitivity Tests; D011759:Pyrrolidines / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar
D000563:Amebicides; D001713:Biphenyl Compounds; D011759:Pyrrolidines; C110499:liroldine