Efficacy of New 5-Nitroimidazoles against Metronidazole-Susceptible and -Resistant Giardia,Trichomonas, and Entamoebaspp

Autor: Upcroft, Jacqueline A., Campbell, Raymond W., Benakli, Kamel, Upcroft, Peter, Vanelle, Patrice
Zdroj: Antimicrobial Agents and Chemotherapy; January 1999, Vol. 43 Issue: 1 p73-76, 4p
Abstrakt: ABSTRACTThe efficacies of 12 5-nitroimidazole compounds and 1 previously described lactam-substituted nitroimidazole with antiparasitic activity, synthesized via SRN1 and subsequent reactions, were assayed against the protozoan parasites Giardia duodenalis, Trichomonas vaginalis, andEntamoeba histolytica. Two metronidazole-sensitive lines and two metronidazole-resistant lines of Giardiaand one line each of metronidazole-sensitive and -resistantTrichomonaswere tested. All except one of the compounds were as effective or more effective than metronidazole againstGiardiaand Trichomonas, but none was as effective overall as the previously described 2-lactam-substituted 5-nitroimidazole. None of the compounds was markedly more effective than metronidazole against Entamoeba. Significant cross-resistance between most of the drugs tested and metronidazole was evident among metronidazole-resistant lines of GiardiaandTrichomonas. However, some drugs were lethal to metronidazole-resistant Giardiaand had minimum lethal concentrations similar to that of metronidazole for drug-susceptible parasites. This study emphasizes the potential in developing new nitroimidazole drugs which are more effective than metronidazole and which may prove to be useful clinical alternatives to metronidazole.
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