Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 21, 2012, Pages 6705-6711

  Surivet, Jean Philippe ^a   Lange, Roland ^a   Hubschwerlen, Christian ^a   Keck, Wolfgang ^a   Specklin, Jean Luc ^a   Ritz, Daniel ^a   Bur, Daniel ^a   Locher, Hans ^a   Seiler, Peter ^a   Strasser, Daniel Stefan ^a   Prade, Lars ^a   Kohl, Christopher ^a   Schmitt, Christine ^a   Chapoux, Gaëlle ^a   Ilhan, Eser ^a   Ekambaram, Nadia ^a   Athanasiou, Alcibiade ^a   Knezevic, Andreja ^a   Sabato, Daniela ^a   Chambovey, Alain ^a   Gaertner, Mika ^a   Enderlin, Michel ^a   Boehme, Maria ^a   Sippel, Virginie ^a   Wyss, Pierre ^a   more..

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

2 amino 1,8 naphthyridine 3 carboxamides; Antibacterials; DNA ligase; In vivo active; Selective inhibitors

Indexed keywords

2 AMINO 6 BROMO 7 (TRIFLUOROMETHYL)[ 1,8 ]NAPHTHYRIDINE 3 CARBOXAMIDE; 2 AMINO[ 1,8 ]NAPHTHYRIDINE 3 CARBOXAMIDE; DNA LIGASE INHIBITOR; LIGASE INHIBITOR; NAPHTHYRIDINE DERIVATIVE; POLYDEOXYRIBONUCLEOTIDE SYNTHASE; QUINOLONE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTIBACTERIAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BACTERIAL GROWTH; BACTERIAL STRAIN; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG POTENCY; DRUG SOLUBILITY; DRUG SYNTHESIS; ENZYME INHIBITION; ESCHERICHIA COLI; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LIVER CELL; MAXIMUM PLASMA CONCENTRATION; MICROSOME; MINIMUM INHIBITORY CONCENTRATION; MOUSE; NEUTROPENIA; NONHUMAN; STAPHYLOCOCCUS AUREUS; STAPHYLOCOCCUS INFECTION; STREPTOCOCCUS PNEUMONIAE; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTI-BACTERIAL AGENTS; CRYSTALLOGRAPHY, X-RAY; DNA LIGASES; DNA, BACTERIAL; DRUG DESIGN; INHIBITORY CONCENTRATION 50; MICE; MICROBIAL SENSITIVITY TESTS; MOLECULAR STRUCTURE; RATS; STAPHYLOCOCCAL INFECTIONS; STAPHYLOCOCCUS; STRUCTURE-ACTIVITY RELATIONSHIP;

BACTERIA (MICROORGANISMS); ESCHERICHIA COLI; LIGA; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PNEUMONIAE;

EID: 84867575898     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.08.094     Document Type: Article

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