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Your search keyword '"Hadida, Sabine"' showing total 2 results
Start Over Author "Hadida, Sabine" Journal journal of medicinal chemistry
2 results on '"Hadida, Sabine"'

2. Discovery of N-(2,4-Di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide(VX-770, Ivacaftor), a Potent and Orally Bioavailable CFTR Potentiator.

Author

Hadida, Sabine, Van Goor, Fredrick, Zhou, Jinglan, Arumugam, Vijayalaksmi, McCartney, Jason, Hazlewood, Anna, Decker, Caroline, Negulescu, Paul, and Grootenhuis, Peter D. J.

Subjects
*PHARMACEUTICAL chemistry, *CARBOXAMIDES, *QUINOLINE, *BIOAVAILABILITY, *CYSTIC fibrosis transmembrane conductance regulator, *HIGH throughput screening (Drug development), *STRUCTURE-activity relationship in pharmacology
Abstract

Quinolinone-3-carboxamide 1, a novel CFTR potentiator,was discovered using high-throughput screening in NIH-3T3 cells expressingthe F508del-CFTR mutation. Extensive medicinal chemistry and iterativestructure–activity relationship (SAR) studies to evaluate potency,selectivity, and pharmacokinetic properties resulted in the identificationof N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide(VX-770, 48, ivacaftor), an investigational drug candidateapproved by the FDA for the treatment of CF patients 6 years of ageand older carrying the G551D mutation. [ABSTRACT FROM AUTHOR]

Published
2014
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