Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 24, 2013, Pages 6598-6603

  Axford, Lorraine C ^a   Agarwal, Piyush K ^d   Anderson, Kelly H ^a   Andrau, Laura N ^a   Atherall, John ^c   Barker, Stephanie ^b   Bennett, James M ^b   Blair, Michael ^a   Collins, Ian ^b   Czaplewski, Lloyd G ^b   Davies, David T ^b   Gannon, Carlie T ^a   Kumar, Dushyant ^d   Lancett, Paul ^b   Logan, Alastair ^b   Lunniss, Christopher J ^a   Mitchell, Dale R ^c   Offermann, Daniel A ^a   Palmer, James T ^a   Palmer, Nicholas ^c   Pitt, Gary R W ^a   Pommier, Stéphanie ^b   Price, Daniel ^b   Narasinga Rao, B ^d   Saxena, Rashmi ^d   Shukla, Tarun ^d   Singh, Amit K ^d   Singh, Mahipal ^d   Srivastava, Anil ^d   Steele, Christopher ^c   Stokes, Neil R ^b   Thomaides Brears, Helena B ^b   Tyndall, Edward M ^a   Watson, David ^c   Haydon, David J ^b   more..

^a Biota Holdings Ltd   (Australia)

^b Biota Europe Ltd   (United Kingdom)

^c BioFocus DPI   (United Kingdom)

^d JUBILANT BIOSYS LTD   (India)

Author keywords

Antibacterial; DNA gyrase; Topoisomerase

Indexed keywords

BENZOTHIAZOLE DERIVATIVE; DNA TOPOISOMERASE INHIBITOR; DNA TOPOISOMERASE IV; GYRASE INHIBITOR; ISONIPECOTIC ACID BENZOTHIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTIBACTERIAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CHEMICAL MODIFICATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; ENTEROCOCCUS FAECALIS; ENZYME INHIBITION; HAEMOPHILUS INFLUENZAE; HUMAN; IC 50; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PYOGENES; STRUCTURE ACTIVITY RELATION;

BACTERIA (MICROORGANISMS); ENTEROCOCCUS FAECALIS; HAEMOPHILUS INFLUENZAE; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PYOGENES;

ANTIBACTERIAL; DNA GYRASE; TOPOISOMERASE;

ANIMALS; ANTI-BACTERIAL AGENTS; BENZOTHIAZOLES; DNA GYRASE; DNA TOPOISOMERASE IV; DRUG DESIGN; ENTEROCOCCUS FAECALIS; ENZYME ACTIVATION; HAEMOPHILUS INFLUENZAE; HALF-LIFE; ISONIPECOTIC ACIDS; MICE; MICROBIAL SENSITIVITY TESTS; RATS; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PYOGENES; TOPOISOMERASE II INHIBITORS;

EID: 84888868586     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.10.058     Document Type: Article

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