1201935-73-0Relevant articles and documents
Identification and optimization of a new series of anti-tubercular quinazolinones
Couturier, Cédric,Lair, Christine,Pellet, Alain,Upton, Anna,Kaneko, Takushi,Perron, Corinne,Cogo, Eric,Menegotto, Jérome,Bauer, Armin,Scheiper, Bodo,Lagrange, Sophie,Bacqué, Eric
, p. 5290 - 5299 (2016)
A high throughput phenotypic screening against Mycobacterium smegmatis led us to the discovery of a new class of bacteriostatic, highly hydrophobic antitubercular quinazolinones that potently inhibited the in vitro growth of either extracellular or intramacrophagic M. tuberculosis (Mtb), via modulation of an unidentified but yet novel target. Optimization of the initial hit compound culminated in the identification of potent but poorly soluble Mtb growth inhibitors, three of which were progressed to in vivo efficacy studies. Despite nanomolar in vitro potency and attractive PK properties, none of these compounds was convincingly potent in our in vivo mouse tuberculosis models. This lack of efficacy may be linked to the poor drug-likeness of the test molecules and/or to the properties of the target.[Figure presented]
PYRIDINE COMPOUNDS
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Page/Page column 197, (2010/01/12)
The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.
