PMID: 6411009Feb 1, 1983Paper

The activity of fexinidazole (HOE 239) against experimental infections with Trypanosoma cruzi, trichomonads and Entamoeba histolytica

Annals of Tropical Medicine and Parasitology
W Raether, H Seidenath

Abstract

A new 5-nitroimidazole compound, 1-methyl-2-(4-methylthiophenoxymethyl)-5-nitroimidazole: fexinidazole, HOE 239, was found to be highly active against experimental infections with Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis and Entamoeba histolytica. It was slightly superior to benznidazole and nifurtimox in suppressing parasitaemia in mice infected with T. cruzi. It also eradicated the parasites from infected mice after a prolonged treatment period. The order of activity of some standard 5-nitroimidazoles obtained on the basis of several mouse or hamster infections with trichomonads and E. histolytica, respectively, was: fexinidazole greater than tinidazole and ornidazole greater than metronidazole greater than nitrimidazine (nimorazole), except that ornidazole had an amoebicidal effect close to that of fexinidazole. The principal metabolites, the sulphoxide and the sulphone were as active as the parent compound against T. cruzi, trichomonads and E. histolytica infections in mice and hamsters, respectively. The general tolerability of fexinidazole in rodents, rabbits and dogs is good and there is a wide range between the effective and maximum tolerated dose. Some side effects, such as anaemia and reduction ...Continue Reading

References

Aug 1, 1978·Annals of Tropical Medicine and Parasitology·W E GutteridgeB Cover
Jan 1, 1980·Transactions of the Royal Society of Tropical Medicine and Hygiene·E BeveridgeM M Waldron

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Citations

Nov 8, 2012·PLoS Neglected Tropical Diseases·Maria Terezinha BahiaIsabela Ribeiro
May 27, 2014·Expert Opinion on Investigational Drugs·Maria Terezinha BahiaVanessa Carla Furtado Mosqueira
Sep 17, 2010·Current Opinion in Infectious Diseases·Michael P Barrett
Dec 19, 2018·Pharmaceutical Research·Helen W HernandezSean Ekins
Feb 6, 2020·Tropical Medicine and Infectious Disease·Philippe NeauLuc Kuykens
Apr 11, 2014·Expert Review of Clinical Pharmacology·Juan M Bustamante, Rick L Tarleton
Nov 21, 2014·Expert Opinion on Investigational Drugs·Shyam Sundar, Jaya Chakravarty
Feb 13, 2020·Parasitology·Claudio A PereiraEdward Valera-Vera
Apr 28, 2018·Current Medicinal Chemistry·Stephen Patterson, Alan H Fairlamb
Dec 4, 2019·European Journal of Medicinal Chemistry·Francisco do Vale Chaves E MelloIsrael Felzenszwalb
Dec 25, 2017·Trends in Parasitology·Michael P Pollastri
Apr 10, 2021·Journal of Experimental Pharmacology·Ana Lia MazzetiVanessa Carla Furtado Mosqueira
Jun 8, 2021·RSC Medicinal Chemistry·Ronald W BrownChristopher J T Hyland

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