2. Academic Validation
  3. Structure-Activity Relationship for the Oxadiazole Class of Antibacterials

Structure-Activity Relationship for the Oxadiazole Class of Antibacterials

  • ACS Med Chem Lett. 2019 Oct 3;11(3):322-326. doi: 10.1021/acsmedchemlett.9b00379.
Marc A Boudreau 1,  Derong Ding 1,  Jayda E Meisel 1,  Jeshina Janardhanan 1,  Edward Spink 1,  Zhihong Peng 1,  Yuanyuan Qian 1,  Takao Yamaguchi 1,  Sebastian A Testero 1,  Peter I O'Daniel 1,  Erika Leemans 1,  Elena Lastochkin 1,  Wei Song 1,  Valerie A Schroeder 2,  William R Wolter 2,  Mark A Suckow 2,  Shahriar Mobashery 1,  Mayland Chang 1
Affiliations

Affiliations

  • 1 Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana 46556, United States.
  • 2 Freimann Life Sciences Center and Department of Biological Sciences, University of Notre Dame, Notre Dame, Indiana 46556, United States.
PMID: 32184964 DOI: 10.1021/acsmedchemlett.9b00379
Abstract

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.

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