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Synthèse d’analogues de nucléosides et d'hétérocycles visant l'inhibition des Mur ligases bactériennes

Abstract : Last decade, a growing problem of antibiotic resistance has become true worries for public health. Since the golden age of antibiotics, their development contributed to improve new marketing active compounds with large broad structural varieties, especially against mycobacteria, pneumococcal or staphylococcal strains. However, pathogenic bacterial infections, still an urgent public health concern because of bacterial resistance, remove the efficacy of employed antibiotics. Therefore, the development of new structural compounds for new antibiotics is a most potent pathway to improve their biological powerful against multi- and/or resistant bacterial strains. This manuscript describes new nucleosidic analogues obtained by diversity-oriented synthesis (DOS) approach. Thus, new synthetic methodology for carbocyclic nucleosides cyclopentanone moiety was investigated and carba-nucleoside from virtual screening was synthetized. Small library of heterocyclic compounds containing an indole structure was developed. Key reactions was used like 1,3-dipolar cycloaddition (CuAAC) allowing to develop a diversity-oriented synthesis approach (DOS). Furthermore, new methodology for pseudo-sugar of carbanucleoside synthesis use an allylic C-H activation cyclization palladium-catalyzed as C(sp3)-C(sp3) bond formation. These molecules have been shown to be active against Mur ligases from Mycobacterium tuberculosis.
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Submitted on : Friday, October 1, 2021 - 1:42:12 PM
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Vincent Hervin. Synthèse d’analogues de nucléosides et d'hétérocycles visant l'inhibition des Mur ligases bactériennes. Chimie organique. Université d'Orléans, 2020. Français. ⟨NNT : 2020ORLE3110⟩. ⟨tel-03361400⟩

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