Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593472 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
Structure-based evolution of the original fragment leads resulted in the identification of 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, (S)-21, a potent, selective phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor with favourable in vivo antiplatelet effect. Despite its antiplatelet action, (S)-21 did not significantly increase bleeding time in dogs. Additionally, due to its enhanced selectivity over p110α, (S)-21 did not induce any insulin resistance in rats.
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Authors
Fabrizio Giordanetto, Andreas Wållberg, Saswati Ghosal, Tommy Iliefski, Johan Cassel, Zhong-Qing Yuan, Henrik von Wachenfeldt, Søren M. Andersen, Tord Inghardt, Anders Tunek, Sven Nylander,