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Synthesis of Stable Aminoacyl‐tRNA Analogues Containing Triazole as a Bioisoster of Esters
Authors:Maryline Chemama  Matthieu Fonvielle Dr.  Michel Arthur Dr.  Jean‐Marc Valéry Prof.  Mélanie Etheve‐Quelquejeu Dr.
Affiliation:1. UMR 7613, Synthèse, Structure et Fonction de Molécules Bioactives, Université Pierre et Marie Curie, 4 place Jussieu, case 179, 75?252 Paris Cedex (France), Fax: (+33)?01?44?27?55?13;2. Centre de Recherche des Cordeliers, LRMA, Equipe 12, INSERM, U872, 75006 Paris (France);3. Université Pierre et Marie Curie, Paris 6, UMR S 872, 75006 Paris (France);4. Université Paris Descartes, UMR S 872, 75006 Paris (France)
Abstract:Stable analogues : An effective synthetic route involving cycloaddition between alkynes and azidonucleosides to afford a new class of stable aminoacyl‐tRNA analogues such as depicted is presented. Biological evaluation showed that theses new compounds act as potent inhibitors of FemXWv aminoacyl transferase, a novel drug target.
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Keywords:aminoacyl‐tRNA  click chemistry  dinucleotides  inhibitors  triazoles
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