Structure-Activity Relationship for the Oxadiazole Class of Antibacterials

Marc A. Boudreau, Derong Ding, Jayda E. Meisel, Jeshina Janardhanan, Edward Spink, Zhihong Peng, Yuanyuan Qian, Takao Yamaguchi, Sebastian A. Testero, Peter I. O'Daniel, Erika Leemans, Elena Lastochkin, Wei Song, Valerie A. Schroeder, William R. Wolter, Mark A. Suckow, Shahriar Mobashery, Mayland Chang

Research output: Contribution to journalArticlepeer-review

18 Scopus citations


A structure-activity relationship (SAR) for the oxadiazole class of antibacterials was evaluated by syntheses of 72 analogs and determination of the minimal-inhibitory concentrations (MICs) against the ESKAPE panel of bacteria. Selected compounds were further evaluated for in vitro toxicity, plasma protein binding, pharmacokinetics (PK), and a mouse model of methicillin-resistant Staphylococcus aureus (MRSA) infection. Oxadiazole 72c shows potent in vitro antibacterial activity, exhibits low clearance, a high volume of distribution, and 41% oral bioavailability, and shows efficacy in mouse models of MRSA infection.

Original languageEnglish
Pages (from-to)322-326
Number of pages5
JournalACS Medicinal Chemistry Letters
Issue number3
StatePublished - Mar 12 2020

Bibliographical note

Funding Information:
This work was supported by grants AI090818 (to MC and SM) and by AI104987 (to SM) from the National Institutes of Health. YQ is a Ruth L. Kirschstein National Research Service Award Fellow of the Chemistry-Biochemistry-Biology Interface Program at the University of Notre Dame, supported by training grant T32 GM075762 from the National Institutes of Health.

Publisher Copyright:
Copyright © 2019 American Chemical Society.


  • Antibacterials
  • oxadiazoles
  • penicillin-binding proteins
  • structure-activity relationship

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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