Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 19, 2013, Pages 5437-5441

  Miles, Timothy J ^a   Hennessy, Alan J ^b   Bax, Ben ^b   Brooks, Gerald ^b   Brown, Barry S ^c   Brown, Pamela ^b   Cailleau, Nathalie ^b   Chen, Dongzhao ^c   Dabbs, Steven ^b   Davies, David T ^b   Esken, Joel M ^c   Giordano, Ilaria ^a   Hoover, Jennifer L ^c   Huang, Jianzhong ^c   Jones, Graham E ^b   Kusalakumari Sukmar, Senthill K ^c   Spitzfaden, Claus ^b   Markwell, Roger E ^b   Minthorn, Elisabeth A ^c   Rittenhouse, Steve ^c   Gwynn, Michael N ^c   Pearson, Neil D ^c   more..

^a GLAXOSMITHKLINE   (Spain)

^b GLAXOSMITHKLINE   (United Kingdom)

^c GLAXOSMITHKLINE   (United States)

Author keywords

Antibacterials; Bacterial type; Hydroxyl tricyclics; IIA topoisomerase; In vivo efficacy; Pharmacokinetic

Indexed keywords

ANTIINFECTIVE AGENT; BACTERIAL TYPE IIA TOPOISOMERASE; DNA TOPOISOMERASE; DNA TOPOISOMERASE INHIBITOR; GSK 966587; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIBACTERIAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BACTERIAL COUNT; BACTERIAL LOAD; CONTROLLED STUDY; CRYSTAL STRUCTURE; DIHYDROXYLATION; DRUG CLEARANCE; DRUG POTENCY; DRUG SYNTHESIS; HAEMOPHILUS INFLUENZAE; HYDROGEN BOND; IN VIVO STUDY; KIDNEY CLEARANCE; LIPOPHILICITY; NONHUMAN; PLASMA CLEARANCE; STREPTOCOCCUS PNEUMONIAE; STRUCTURE ACTIVITY RELATION; SUZUKI REACTION; X RAY CRYSTALLOGRAPHY;

BACTERIA (MICROORGANISMS); NEGIBACTERIA; POSIBACTERIA;

ANTIBACTERIALS; BACTERIAL TYPE IIA TOPOISOMERASE; HYDROXYL TRICYCLICS; IN VIVO EFFICACY; PHARMACOKINETIC;

ANIMALS; BACTERIA; CRYSTALLOGRAPHY, X-RAY; DOGS; ENZYME ACTIVATION; HAPLORHINI; HUMANS; MICROBIAL SENSITIVITY TESTS; MOLECULAR STRUCTURE; NAPHTHYRIDINES; RATS; TOPOISOMERASE II INHIBITORS;

EID: 84883487976     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.07.013     Document Type: Article

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