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Synthesis and evaluation of 1,3,4-oxadiazole derivatives for development as broad-spectrum antibiotics

Abstract : The reality and intensity of antibiotic resistance in pathogenic bacteria calls for the rapid development of new antimicrobial drugs. In bacteria, trans-translation is the primary quality control mechanism for rescuing ribosomes arrested during translation. Because trans-translation is absent in eukaryotes but necessary to avoid ribosomal stalling and therefore essential for bacterial survival, it is a promising target either for novel antibiotics or for improving the activities of the protein synthesis inhibitors already in use. Oxadiazole derivatives display strong bactericidal activity against a large number of bacteria, but their effects on trans-translation were recently questioned. In this work, a series of new 1,3,4-oxadiazole derivatives and analogs were synthesized and assessed for their efficiency as antimicrobial agents against a wide range of gram-positive and gram-negative pathogenic strains. Despite the strong antimicrobial activity observed in these molecules, it turns out that they do not target trans-translation in vivo, but they definitely act on other cellular pathways.
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Cédric Tresse, Richard Radigue, Rafael Gomes von Borowski, Marion Thepaut, Hong Hanh Le, et al.. Synthesis and evaluation of 1,3,4-oxadiazole derivatives for development as broad-spectrum antibiotics. Bioorganic and Medicinal Chemistry, Elsevier, 2019, 27 (21), pp.115097. ⟨10.1016/j.bmc.2019.115097⟩. ⟨hal-02304766⟩

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