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- Sabine Hadida, Fredrick Van Goor, Jinglan Zhou, Vijayalaksmi Arumugam, Jason McCartney, Anna Hazlewood, Caroline Decker, Paul Negulescu, and Peter D J Grootenhuis.
- Vertex Pharmaceuticals Incorporated , 11010 Torreyana Road, San Diego, California 92121, United States.
- J. Med. Chem. 2014 Dec 11; 57 (23): 9776-95.
AbstractQuinolinone-3-carboxamide 1, a novel CFTR potentiator, was discovered using high-throughput screening in NIH-3T3 cells expressing the F508del-CFTR mutation. Extensive medicinal chemistry and iterative structure-activity relationship (SAR) studies to evaluate potency, selectivity, and pharmacokinetic properties resulted in the identification of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, 48, ivacaftor), an investigational drug candidate approved by the FDA for the treatment of CF patients 6 years of age and older carrying the G551D mutation.
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