Design, synthesis, and characterization of novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram-positive activity

Journal of Medicinal Chemistry

Volumn 56, Issue 18, 2013, Pages 7396-7415

  Surivet, Jean Philippe ^a   Zumbrunn, Cornelia ^a   Rueedi, Georg ^a   Hubschwerlen, Christian ^a   Bur, Daniel ^a   Bruyère, Thierry ^a   Locher, Hans ^a   Ritz, Daniel ^a   Keck, Wolfgang ^a   Seiler, Peter ^a   Kohl, Christopher ^a   Gauvin, Jean Christophe ^a   Mirre, Azely ^a   Kaegi, Verena ^a   Dos Santos, Marina ^a   Gaertner, Mika ^a   Delers, Jonathan ^a   Enderlin Paput, Michel ^a   Boehme, Maria ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

1,2 DIHYDROXY 2 (3 METHOXYQUINOXALIN 5 YL)ETHYL)TETRAHYDRO 2H PYRAN 3 YL)AMINO)METHYL) 2H PYRIDO[3,2 B] [1,4]THIAZIN 3(4H) ONE; 2 (3 FLUORO 6 METHOXY 1,5 NAPHTHYRIDIN 4YL) 1,2 DIHYDROXYETHYL)TETRAHYDRO 2H PYRAN 3 YL)AMINO)METHYL) 2H PYRIDO[3,2 B][1,4]THIAZIN 3(4H) ONE; 6 (2 (6 METHOXY 1,5 NAPHTHYRIDIN 4 YL)ETHYL)TETRAHYDRO 2H PYRAN 3 Y)AMINO)METHYL) 2H PYRIDO[3,2 B][1,4] THIAZIN 3(4H) ONE; ANTIINFECTIVE AGENT; BACTERIAL DNA; CIPROFLOXACIN; DNA TOPOISOMERASE INHIBITOR; DNA TOPOISOMERASE IV; LINEZOLID; POTASSIUM CHANNEL HERG; QUINOLONE DERIVATIVE; TETRAHYDROPYRAN DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIBACTERIAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CHEMICAL STRUCTURE; CROSS RESISTANCE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG EFFICACY; DRUG HALF LIFE; DRUG SYNTHESIS; ENANTIOMER; ENZYME INHIBITION; ESCHERICHIA COLI; IN VITRO STUDY; IN VIVO STUDY; MALE; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PSEUDOMONAS AERUGINOSA; RAT; STAPHYLOCOCCUS INFECTION; STEREOCHEMISTRY; STREPTOCOCCUS PNEUMONIAE; WILD TYPE;

ANIMALS; ANTI-BACTERIAL AGENTS; CHEMISTRY TECHNIQUES, SYNTHETIC; DNA GYRASE; DNA TOPOISOMERASE IV; DNA TOPOISOMERASES; DRUG DESIGN; FEMALE; GRAM-POSITIVE BACTERIA; HUMANS; INHIBITORY CONCENTRATION 50; MICE; MOLECULAR DOCKING SIMULATION; PROTEIN CONFORMATION; PYRANS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TOPOISOMERASE II INHIBITORS; TOPOISOMERASE INHIBITORS;

EID: 84885002688     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400963y     Document Type: Article

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