Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization. A promising alternative to random screening

Journal of Medicinal Chemistry

Volumn 43, Issue 14, 2000, Pages 2664-2674

  Boehm, Hans Joachim ^a   Boehringer, Markus ^a   Bur, Daniel ^a   Gmuender, Hans ^a   Huber, Walter ^a   Klaus, Werner ^a   Kostrewa, Dirk ^a   Kuehne, Holger ^a   Luebbers, Thomas ^a   Meunier Keller, Nathalie ^a   Mueller, Francis ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

7 [4 (4 TERT BUTYL BENZYLOXY) 1H INDAZOL 3 YLMETHYLSULFANYL] 4 METHYLCOUMARIN; CIPROFLOXACIN; GYRASE INHIBITOR; INDAZOLE DERIVATIVE; INDOLE DERIVATIVE; NOVOBIOCIN; PHENOL DERIVATIVE; PYRIMIDINE DERIVATIVE; PYRROLOPYRIMIDINE DERIVATIVE; RO 09 1437; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; DRUG BINDING; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; VALIDATION PROCESS;

ANTI-INFECTIVE AGENTS; COUMARINS; CRYSTALLOGRAPHY, X-RAY; DNA TOPOISOMERASES, TYPE II; ENZYME INHIBITORS; INDAZOLES; MAGNETIC RESONANCE SPECTROSCOPY; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NOVOBIOCIN; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP; SURFACE PLASMON RESONANCE; ULTRACENTRIFUGATION;

EID: 1642288258     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000017s     Document Type: Article

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