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5-(2-Pyrimidinyl)-imidazo[1,2- a]pyridines are antibacterial agents targeting the ATPase domains of DNA gyrase and topoisomerase IV

Dual inhibitors of bacterial gyrB and parE based on a 5-(2-pyrimidinyl)-imidazo[1,2- a]pyridine template exhibited MICs (μg/mL) of 0.06–64 (Sau), 0.25–64 (MRSA), 0.06–64 (Spy), 0.06–64 (Spn), and 0.03–64 (FQR Spn). Selected examples were efficacious in mouse sepsis and lung infection models at...

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Published in:Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (18), p.5302-5306
Main Authors: Starr, Jeremy T., Sciotti, Richard J., Hanna, Debra L., Huband, Michael D., Mullins, Lisa M., Cai, Hongliang, Gage, Jeffrey W., Lockard, Mandy, Rauckhorst, Mark R., Owen, Robert M., Lall, Manjinder S., Tomilo, Mark, Chen, Huifen, McCurdy, Sandra P., Barbachyn, Michael R.
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Language:English
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Summary:Dual inhibitors of bacterial gyrB and parE based on a 5-(2-pyrimidinyl)-imidazo[1,2- a]pyridine template exhibited MICs (μg/mL) of 0.06–64 (Sau), 0.25–64 (MRSA), 0.06–64 (Spy), 0.06–64 (Spn), and 0.03–64 (FQR Spn). Selected examples were efficacious in mouse sepsis and lung infection models at
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.07.141