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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 11 , Issue 5 , 2014

Page: [531 - 559] Pages: 29

DOI: 10.2174/1570180810666131122010615

Price: $65

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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