1136833-01-6Relevant academic research and scientific papers
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials
Boudreau, Marc A.,Ding, Derong,Meisel, Jayda E.,Janardhanan, Jeshina,Spink, Edward,Peng, Zhihong,Qian, Yuanyuan,Yamaguchi, Takao,Testero, Sebastian A.,O'Daniel, Peter I.,Leemans, Erika,Lastochkin, Elena,Song, Wei,Schroeder, Valerie A.,Wolter, William R.,Suckow, Mark A.,Mobashery, Shahriar,Chang, Mayland
, p. 322 - 326 (2019/10/16)
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.
ANTIBACTERIAL COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 14, (2010/11/03)
Embodiments of the present invention provide novel antibacterials that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.
ANTIBACTERIAL COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 33-34, (2009/05/29)
Embodiments of the present invention provide novel antibactehals that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.
