Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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

Author(s): 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.

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
Page: [531 - 559]
Pages: 29
DOI: 10.2174/1570180810666131122010615