Synthesis of novel 1,2,5-oxadiazoles and evaluation of action against Acinetobacter baumannii

Rebecca M. Christoff, Gerald L. Murray, Xenia P. Kostoulias, Anton Y. Peleg, Belinda M. Abbott

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6 Citations (Scopus)


With multidrug resistant bacteria on the rise, novel antibiotics are becoming highly sought after. In 2008, eleven compounds were identified by high throughput screening as inhibitors of BasE, a key enzyme of the non-ribosomal peptide synthetase pathway found in Acinetobacter baumannii. Herein, we describe the preparation of four structurally similar heterocyclic lead compounds from that study, including one 1,2,5-oxadiazole. A further library of 30 analogues containing the oxadiazole moiety was then generated. All compounds were screened against Acinetobacter baumannii and their minimum inhibitory concentration data is reported, with (E)-3-(2-hydroxyphenyl)-N-(4-methyl-1,2,5-oxadiazol-3-yl)acrylamide 32 found to have an MIC of 0.5 mM. This work provides the foundation for further investigation of 1,2,5-oxadizoles as novel inhibitors of A. baumannii.

Original languageEnglish
Pages (from-to)6267-6272
Number of pages6
JournalBioorganic & Medicinal Chemistry
Issue number24
Publication statusPublished - 15 Dec 2017


  • 1,2,5-Oxadiazoles
  • Acinetobacter baumannii
  • Antibiotic resistance
  • BasE inhibitors

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