Science and Technology Production
Article
Authorship
Boudreau, Marc A.
;
Ding, Derong
;
Meisel, Jayda E.
;
Janardhanan, Jeshina
;
Spink, Edward
;
Peng, Zhihong
;
Qian, Yuanyuan
;
Yamaguchi, Takao
;
TESTERO, SEBASTIAN ANDRES
;
O'Daniel, Peter I.
;
Leemans, Erika
;
Lastochkin, Elena
;
Song, Wei
;
Schroeder, Valerie A.
;
Wolter, William R.
;
Suckow, Mark A.
;
Mobashery, Shahriar
;
Chang, Mayland
Date
2020
Publishing House and Editing Place
American Chemical Society
Magazine
ACS Medicinal Chemistry Letters,
vol. 11
(pp. 322-326)
- ISSN 1948-5875
American Chemical Society
American Chemical Society
ISSN
1948-5875
Summary
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SIGEVA
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 cl...
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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Key Words
PENICILLIN-BINDING PROTEINSOXADIAZOLESANTIBACTERIALSSTRUCTURE-ACTIVITY RELATIONSHIP
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