Designing New 5-Nitroimidazoles: Towards Safer Anti-infectious Agents

作者：Crozet Maxime D; Terme Thierry; Vanelle Patrice^*

来源：Letters in Drug Design and Discovery, 2014, 11(5): 531-559.

• 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), palladium-catalyzed cross-coupling reactions (Suzuki-Miyaura, Sonogashira...) and electron transfer reactions (Unimolecular Radical Nucleophilic Substitution (SRN1), TDAE methodology) applied in 5-nitroimidazole series.

• 出版日期2014-6