Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV
Mark J Mitton Fry
1
,
Steven J. Brickner
1
,
Judith C. Hamel
1
,
Rose Barham
1
,
Lori Brennan
1
,
Jeffrey M. Casavant
1
,
Xiaoyuan Ding
1
,
Steven Finegan
1
,
Joel Hardink
1
,
Thuy Hoang
1
,
Michael D. Huband
1
,
Meghan Maloney
1
,
Anthony Marfat
1
,
Sandra McCurdy
1
,
Dale Mcleod
1
,
Chakrapani Subramanyam
1
,
Michael Plotkin
1
,
Usa Reilly
1
,
John R Schafer
1
,
Gregory G Stone
1
,
Daniel P Uccello
1
,
Todd Wisialowski
1
,
Kwansik Yoon
1
,
Richard Zaniewski
1
,
Christopher Zook
1
1
Pfizer Worldwide Research and Development, Groton, CT 06340, USA.
|
Publication type: Journal Article
Publication date: 2017-08-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
28610977
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Novel (non-fluoroquinolone) inhibitors of bacterial type II topoisomerases (NBTIs) are an emerging class of antibacterial agents. We report an optimized series of cyclobutylaryl-substituted NBTIs. Compound 14 demonstrated excellent activity both in vitro (S. aureus MIC90=0.125μg/mL) and in vivo (systemic and tissue infections). Enhanced inhibition of Topoisomerase IV correlated with improved activity in S. aureus strains with mutations conferring resistance to NBTIs. Compound 14 also displayed an improved hERG IC50 of 85.9μM and a favorable profile in the anesthetized guinea pig model.
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Total citations:
33
Citations from 2024:
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(12.12%)
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GOST
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Mitton Fry M. J. et al. Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 15. pp. 3353-3358.
GOST all authors (up to 50)
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Mitton Fry M. J., Brickner S. J., Hamel J. C., Barham R., Brennan L., Casavant J. M., Ding X., Finegan S., Hardink J., Hoang T., Huband M. D., Maloney M., Marfat A., McCurdy S., Mcleod D., Subramanyam C., Plotkin M., Reilly U., Schafer J. R., Stone G. G., Uccello D. P., Wisialowski T., Yoon K., Zaniewski R., Zook C. Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 15. pp. 3353-3358.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmcl.2017.06.009
UR - https://doi.org/10.1016/j.bmcl.2017.06.009
TI - Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Mitton Fry, Mark J
AU - Brickner, Steven J.
AU - Hamel, Judith C.
AU - Barham, Rose
AU - Brennan, Lori
AU - Casavant, Jeffrey M.
AU - Ding, Xiaoyuan
AU - Finegan, Steven
AU - Hardink, Joel
AU - Hoang, Thuy
AU - Huband, Michael D.
AU - Maloney, Meghan
AU - Marfat, Anthony
AU - McCurdy, Sandra
AU - Mcleod, Dale
AU - Subramanyam, Chakrapani
AU - Plotkin, Michael
AU - Reilly, Usa
AU - Schafer, John R
AU - Stone, Gregory G
AU - Uccello, Daniel P
AU - Wisialowski, Todd
AU - Yoon, Kwansik
AU - Zaniewski, Richard
AU - Zook, Christopher
PY - 2017
DA - 2017/08/01
PB - Elsevier
SP - 3353-3358
IS - 15
VL - 27
PMID - 28610977
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2017_Mitton Fry,
author = {Mark J Mitton Fry and Steven J. Brickner and Judith C. Hamel and Rose Barham and Lori Brennan and Jeffrey M. Casavant and Xiaoyuan Ding and Steven Finegan and Joel Hardink and Thuy Hoang and Michael D. Huband and Meghan Maloney and Anthony Marfat and Sandra McCurdy and Dale Mcleod and Chakrapani Subramanyam and Michael Plotkin and Usa Reilly and John R Schafer and Gregory G Stone and Daniel P Uccello and Todd Wisialowski and Kwansik Yoon and Richard Zaniewski and Christopher Zook},
title = {Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2017},
volume = {27},
publisher = {Elsevier},
month = {aug},
url = {https://doi.org/10.1016/j.bmcl.2017.06.009},
number = {15},
pages = {3353--3358},
doi = {10.1016/j.bmcl.2017.06.009}
}
Cite this
MLA
Copy
Mitton Fry, Mark J., et al. “Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV.” Bioorganic and Medicinal Chemistry Letters, vol. 27, no. 15, Aug. 2017, pp. 3353-3358. https://doi.org/10.1016/j.bmcl.2017.06.009.