Designing New 5-Nitroimidazoles: Towards Safer Anti-infectious Agents
Maxime D. Crozet, Thierry Terme and Patrice Vanelle
5-Nitroimidazoles are drugs having both antiprotozoal and antibacterial activity, but show mutagenicity and development of resistance observed 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), palladium-catalyzed cross-coupling reactions (Suzuki-Miyaura, Sonogashira…) and electron transfer reactions (Unimolecular Radical Nucleophilic Substitution (SRN1), TDAE methodology) applied in 5-nitroimidazole series.
Anti-infectious agents, Electron transfer reactions, 5-Nitroimidazole, Palladium-catalyzed reactions, VNS reaction
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.