Artículo

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 AndresIcon ; O'Daniel, Peter I.; Leemans, Erika; Lastochkin, Elena; Song, Wei; Schroeder, Valerie A.; Wolter, William R.; Suckow, Mark A.; Mobashery, Shahriar; Chang, Mayland
Fecha de publicación: 03/2020
Editorial: American Chemical Society
Revista: ACS Medicinal Chemistry Letters
ISSN: 1948-5875
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:

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.
Palabras clave: ANTIBACTERIALS , OXADIAZOLES , PENICILLIN-BINDING PROTEINS , STRUCTURE-ACTIVITY RELATIONSHIP
 
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution 2.5 Unported (CC BY 2.5)
Identificadores
URI: http://hdl.handle.net/11336/117105
URL: http://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00379
DOI: http://dx.doi.org/10.1021/acsmedchemlett.9b00379
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Articulos de INST.DE QUIMICA ROSARIO
Citación
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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