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

Author(s): Maxime D. Crozet, Thierry Terme, Patrice Vanelle.

Journal Name:Letters in Drug Design & Discovery

Volume 11 , Issue 5 , 2014

Abstract:

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.

Keywords: Anti-infectious agents, Electron transfer reactions, 5-Nitroimidazole, Palladium-catalyzed reactions, VNS reaction.

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Article Details

VOLUME: 11
ISSUE: 5
Year: 2014
Page: [531 - 559]
Pages: 29
DOI: 10.2174/1570180810666131122010615
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