Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK)

Journal of Medicinal Chemistry

Volumn 55, Issue 22, 2012, Pages 10010-10021

  Martínez Botella, Gabriel ^a,c   Breen, John N ^a   Duffy, James E S ^b   Dumas, Jacques ^a   Geng, Bolin ^a   Gowers, Ian K ^b   Green, Oluyinka M ^a   Guler, Satenig ^a   Hentemann, Martin F ^a   Hernandez Juan, Felix A ^b   Joseph McCarthy, Diane ^a   Kawatkar, Sameer ^a   Larsen, Nicholas A ^a   Lazari, Ovadia ^b   Loch, James T ^a   Macritchie, Jacqueline A ^b   McKenzie, Andrew R ^a   Newman, Joseph V ^a   Olivier, Nelson B ^a   Otterson, Linda G ^a   Owens, Andrew P ^b   Read, Jon ^a   Sheppard, David W ^b   Keating, Thomas A ^a   more..

^a ASTRAZENECA   (United Kingdom)

^b BioFocus DPI   (United Kingdom)

^c Sage Therapeutics Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (3 BROMOPHENOXY) 4 [1 [3 (5 METHYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H) YL)PIPERIDIN 1 YL]HEXYL]BENZOIC ACID; 2 (3 BROMOPHENOXY) 4 [3,3 DIMETHYL 1 [(5 METHYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H) YL)PIPERIDIN 1 YL]BUTYL]BENZOIC ACID; ANTIINFECTIVE AGENT; BACTERIAL ENZYME; ENZYME INHIBITOR; LEVOFLOXACIN; THYMIDINE PHOSPHATE; THYMIDYLATE KINASE; THYMIDYLATE KINASE INHIBITOR; TK 666; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DIASTEREOISOMER; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; ENZYME INHIBITION; GRAM POSITIVE BACTERIUM; HUMAN; HUMAN CELL; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; SINGLE DRUG DOSE; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PNEUMONIAE; VANCOMYCIN RESISTANT ENTEROCOCCUS; X RAY CRYSTALLOGRAPHY;

ANTI-BACTERIAL AGENTS; BENZOATES; CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; ENTEROCOCCUS; HUMANS; METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS; MICROBIAL SENSITIVITY TESTS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NUCLEOSIDE-PHOSPHATE KINASE; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PNEUMONIAE; STRUCTURE-ACTIVITY RELATIONSHIP; THYMINE; VANCOMYCIN RESISTANCE;

EID: 84870049171     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3011806     Document Type: Article

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