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

Autor:	Hongliang Cai, Mark Tomilo, Sandra P. McCurdy, Jeremy T. Starr, Manjinder S. Lall, Mandy Lockard, Mark R. Rauckhorst, Jeffrey W. Gage, Barbachyn Michael R, Huifen Chen, Robert M. Owen, Michael D. Huband, Debra Hanna, Lisa Mullins, Richard J. Sciotti
Rok vydání:	2009
Předmět:	DNA Topoisomerase IV Pyridines Topoisomerase IV Gram-positive bacteria Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Pharmacology Gram-Positive Bacteria medicine.disease_cause Biochemistry DNA gyrase Microbiology Mice Structure-Activity Relationship Sepsis Drug Discovery medicine Animals Lung Molecular Biology Antibacterial agent chemistry.chemical_classification biology Topoisomerase Organic Chemistry Imidazoles biochemical phenomena metabolism and nutrition biology.organism_classification Anti-Bacterial Agents Rats Pyrimidines Enzyme chemistry DNA Gyrase Staphylococcus aureus Streptococcus pyogenes biology.protein Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:5302-5306
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2009.07.141
Popis:	Dual inhibitors of bacterial gyrB and parE based on a 5-(2-pyrimidinyl)-imidazo[1,2-a]pyridine template exhibited MICs (microg/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
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b0e2071aabace46a4d35df913c184d5 https://doi.org/10.1016/j.bmcl.2009.07.141 Zobrazit plný text záznamu Full Text from ScienceDirect