Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2

On the basis of our recent results on a novel series of imidazopyridazine-based antimalarials, we focused on identifying compounds with improved aqueous solubility and hERG profile while maintaining metabolic stability and in vitro potency. Toward this objective, 41 compounds were synthesized and ev...

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Veröffentlicht in:Journal of medicinal chemistry 2014-11, Vol.57 (21), p.8839-8848
Hauptverfasser: Le Manach, Claire, Paquet, Tanya, Gonzàlez Cabrera, Diego, Younis, Yassir, Taylor, Dale, Wiesner, Lubbe, Lawrence, Nina, Schwager, Sylva, Waterson, David, Witty, Michael J, Wittlin, Sergio, Street, Leslie J, Chibale, Kelly
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Sprache:eng
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