Structure–Activity Relationship for the Oxadiazole Class of Antibacterials
Marc A Boudreau
1
,
Derong Ding
1
,
Jayda E Meisel
1
,
Jeshina Janardhanan
1
,
Edward Spink
1
,
Zhihong Peng
1
,
Yuanyuan Qian
1
,
Takao Yamaguchi
1
,
Sebastian A Testero
1
,
Peter I Odaniel
1
,
Erika Leemans
1
,
Elena Lastochkin
1
,
Wei Song
1
,
Valerie A. Schroeder
2
,
William R. Wolter
2
,
Mark A. Suckow
2
,
Mayland Chang
1
Publication type: Journal Article
Publication date: 2019-10-03
scimago Q1
wos Q2
SJR: 0.805
CiteScore: 5.8
Impact factor: 4.0
ISSN: 19485875
PubMed ID:
32184964
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
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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Total citations:
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MLA
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GOST
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Boudreau M. A. et al. Structure–Activity Relationship for the Oxadiazole Class of Antibacterials // ACS Medicinal Chemistry Letters. 2019. Vol. 11. No. 3. pp. 322-326.
GOST all authors (up to 50)
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Boudreau M. A., Ding D., Meisel J. E., Janardhanan J., Spink E., Peng Z., Qian Y., Yamaguchi T., Testero S. A., Odaniel P. I., Leemans E., Lastochkin E., Song W., Schroeder V. A., Wolter W. R., Suckow M. A., Mobashery S., Chang M. Structure–Activity Relationship for the Oxadiazole Class of Antibacterials // ACS Medicinal Chemistry Letters. 2019. Vol. 11. No. 3. pp. 322-326.
Cite this
RIS
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TY - JOUR
DO - 10.1021/acsmedchemlett.9b00379
UR - https://doi.org/10.1021/acsmedchemlett.9b00379
TI - Structure–Activity Relationship for the Oxadiazole Class of Antibacterials
T2 - ACS Medicinal Chemistry Letters
AU - Boudreau, Marc A
AU - Ding, Derong
AU - Meisel, Jayda E
AU - Janardhanan, Jeshina
AU - Spink, Edward
AU - Peng, Zhihong
AU - Qian, Yuanyuan
AU - Yamaguchi, Takao
AU - Testero, Sebastian A
AU - Odaniel, Peter I
AU - Leemans, Erika
AU - Lastochkin, Elena
AU - Song, Wei
AU - Schroeder, Valerie A.
AU - Wolter, William R.
AU - Suckow, Mark A.
AU - Mobashery, Shahriar
AU - Chang, Mayland
PY - 2019
DA - 2019/10/03
PB - American Chemical Society (ACS)
SP - 322-326
IS - 3
VL - 11
PMID - 32184964
SN - 1948-5875
ER -
Cite this
BibTex (up to 50 authors)
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@article{2019_Boudreau,
author = {Marc A Boudreau and Derong Ding and Jayda E Meisel and Jeshina Janardhanan and Edward Spink and Zhihong Peng and Yuanyuan Qian and Takao Yamaguchi and Sebastian A Testero and Peter I Odaniel and Erika Leemans and Elena Lastochkin and Wei Song and Valerie A. Schroeder and William R. Wolter and Mark A. Suckow and Shahriar Mobashery and Mayland Chang},
title = {Structure–Activity Relationship for the Oxadiazole Class of Antibacterials},
journal = {ACS Medicinal Chemistry Letters},
year = {2019},
volume = {11},
publisher = {American Chemical Society (ACS)},
month = {oct},
url = {https://doi.org/10.1021/acsmedchemlett.9b00379},
number = {3},
pages = {322--326},
doi = {10.1021/acsmedchemlett.9b00379}
}
Cite this
MLA
Copy
Boudreau, Marc A., et al. “Structure–Activity Relationship for the Oxadiazole Class of Antibacterials.” ACS Medicinal Chemistry Letters, vol. 11, no. 3, Oct. 2019, pp. 322-326. https://doi.org/10.1021/acsmedchemlett.9b00379.