Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors

A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.

ROCK inhibitors have been developed from 2-chromanyl- and 2-carboxamido-benzothiazoles. SAR studies and lead optimizations are described, which result in novel ROCK-II inhibitors with sub-nanomolar IC50s and good kinase selectivity.Figure optionsDownload as PowerPoint slide