Designing New 5-Nitroimidazoles: Towards Safer Anti-infectious Agents
Maxime D. Crozet, Thierry Terme and Patrice Vanelle
Affiliation: Aix-Marseille Univ, UMR CNRS 7273: Institut de Chimie Radicalaire, Equipe Pharmaco-Chimie Radicalaire (LPCR), Faculté de Pharmacie, 27 Boulevard Jean Moulin, CS 30064, 13385 Marseille cedex 5, France.
Keywords: Anti-infectious agents, Electron transfer reactions, 5-Nitroimidazole, Palladium-catalyzed reactions, VNS reaction.
5-Nitroimidazoles are drugs having both antiprotozoal and antibacterial activity, but show mutagenicity and
development of resistance particularly with metronidazole. For the development of new potentially safer derivatives, we
investigated new strategies of synthesis: such as Vicarious Nucleophilic Substitution of hydrogen (VNS), palladiumcatalyzed
cross-coupling reactions (Suzuki-Miyaura, Sonogashira…) and electron transfer reactions (Unimolecular Radical
Nucleophilic Substitution (SRN1), TDAE methodology) applied in 5-nitroimidazole series.
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