Nitroimidazoles: Part XIX. Structure-activity relationships

Abstract

A variety of nitroimidazoles, mostly 1,2-disubstituted-5-nitroderivatives were examined for in vitro activity against E. histolytica and in early hepatic infection of infected golden hamsters. Many preparations carried a functionalised N atom at position 2. In vivo activity was found widely among 1-alkyl-5-nitroimidazoles carrying a substituted imidazolidinone (1) or imidazole (2). Out of these derivatives, l-methyl-sulphonyl-3-(1-methyl-5-nitro-2-imidazolyl)-2-irnidazolidinone(la;C 10213-Go) was found to be the best and to be superior to marketed nitroimidazoles against hepatic and caecal infections of E. histolytica ip the golden hamster and T. foetus infections in mice, and has been developed as a drug for treatment of amoebiasis, giardiasis and trichomoniasis.