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Bioorg Med Chem ; 27(21): 115097, 2019 11 01.
Article in English | MEDLINE | ID: mdl-31540826

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.


Subject(s)
Anti-Bacterial Agents/pharmacology , Oxadiazoles/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/toxicity , Cell Line, Tumor , Cell Survival/drug effects , Drug Design , Drug Synergism , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Humans , Microbial Sensitivity Tests , Oxadiazoles/chemical synthesis , Oxadiazoles/toxicity
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