Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656)

Journal of Medicinal Chemistry

Volumn 60, Issue 19, 2017, Pages 8011-8026

  Li, Xianfeng ^a   Hernandez, Vincent ^a   Rock, Fernando L ^a   Choi, Wai ^a   Mak, Yvonne S L ^a   Mohan, Manisha ^a   Mao, Weimin ^a   Zhou, Yasheen ^a   Easom, Eric E ^a   Plattner, Jacob J ^a   Zou, Wuxin ^b   Pérez Herrán, Esther ^c   Giordano, Ilaria ^c   Mendoza Losana, Alfonso ^c   Alemparte, Carlos ^c   Rullas, Joaquín ^c   Angulo Barturen, Iñigo ^c,d   Crouch, Sabrinia ^c   Ortega, Fátima ^c   Barros, David ^c   Alley, M R K ^a   more..

^a PFIZER INC   (United States)

^b BioDuro LLC   (China)

^c GLAXOSMITHKLINE   (Spain)

^d SL   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

3 (AMINOMETHYL) 4 CHLORO 7 (2 HYDROXYETHOXY)BENZO[C][1,2]OXABOROL 1(3H) OL; ENZYME INHIBITOR; GSK 656; LEUCINE TRANSFER RNA LIGASE; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; BORON DERIVATIVE; FUSED HETEROCYCLIC RINGS; GSK656;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIBACTERIAL ACTIVITY; ARTICLE; CONTROLLED STUDY; CYTOPLASM; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; DRUG SPECIFICITY; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; MINIMUM INHIBITORY CONCENTRATION; MITOCHONDRION; MOUSE; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; STRUCTURE ACTIVITY RELATION; TUBERCULOSIS; ANIMAL; ANTAGONISTS AND INHIBITORS; C57BL MOUSE; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYME SPECIFICITY; ENZYMOLOGY; SYNTHESIS;

ANIMALS; ANTITUBERCULAR AGENTS; BORON COMPOUNDS; DRUG DISCOVERY; ENZYME INHIBITORS; FEMALE; HETEROCYCLIC COMPOUNDS, 2-RING; HUMANS; LEUCINE-TRNA LIGASE; MICE; MICE, INBRED C57BL; MYCOBACTERIUM TUBERCULOSIS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 85031286759     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.7b00631     Document Type: Article

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