Structure-Activity Relationship for the Oxadiazole Class of Antibacterials
; O'Daniel, Peter I. ; Leemans, Erika ; Lastochkin, Elena ; Song, Wei ; Schroeder, Valerie A. ; Wolter, William R. ; Suckow, Mark A. ; Mobashery, Shahriar ; Chang, Mayland Otros responsables
Fecha
03/2020
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American Chemical Society
Revista
ACS Medicinal Chemistry Letters
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1948-5875
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Inglés
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Resumen
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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Boudreau, Marc A.; Ding, Derong; Meisel, Jayda E.; Janardhanan, Jeshina; Spink, Edward; et al.; Structure-Activity Relationship for the Oxadiazole Class of Antibacterials; American Chemical Society; ACS Medicinal Chemistry Letters; 11; 3; 3-2020; 322-326
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