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 ...
