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Extra resources for Bioreduction in the Activation of Drugs. Proceedings of the Second Biochemical Pharmacology Symposium, Oxford, UK, 25–26 July 1985

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REDUCTIVE ACTIVATION OF 5-NITROIMIDAZOLES The action of metronidazole and related 5-nitroimidazole derivatives on microorganisms is characterized by selective killing of anaerobic prokaryotes and eukaryotes. Inhibitory concentrations for facultative anaerobes and aerobes are at least two orders of magnitude higher than those for anaerobes. Mutagenicity is often observed in microorganisms that are not highly susceptible to 5-nitroimidazoles. In vitro studies with Trichomonas vaginalis, against which metronidazole was developed, show that 5-nitroimidazoles exert a high antitrichomonad activity under both anaerobic and aerobic conditions [7].

Moreover, the dicysteinylamino adduct of ronidazole, identified from microsomal incubations with excess, exogenous cysteine, is exactly the product expected from the stepwise nucleophilic attack of II and IVa by cysteine. During protein alkylation, however, IVa would be immobilized by the protein, R'SH, and, consequently, water might be a more reasonable alternative nucleophile yielding the putative 4-cysteinyl-aminoimidazole, Va. The Michael-like acceptor IVb, which results from the initial attack of II by water, could undergo nucleophilic addition with protein thiols to yield the protein-bound imidazolinone, Vb, while reactions with water would yield various hydrolysis products.

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