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 toxicity, plasma protein binding, pharmacokinetics (PK), and a mouse model of methicillin-resistant (MRSA) infection. Oxadiazole shows potent 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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7073871 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.9b00379 | DOI Listing |
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