874119-96-7Relevant academic research and scientific papers
Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases
Sehon, Clark A.,Wang, Gren Z.,Viet, Andrew Q.,Goodman, Krista B.,Dowdell, Sarah E.,Elkins, Patricia A.,Semus, Simon F.,Evans, Christopher,Jolivette, Larry J.,Kirkpatrick, Robert B.,Dul, Edward,Khandekar, Sanjay S.,Yi, Tracey,Wright, Lois L.,Smith, Gary K.,Behm, David J.,Bentley, Ross,Doe, Christopher P.,Hu, Erding,Lee, Dennis
, p. 6631 - 6634 (2008)
Recent studies using known Rho-associated kinase isoform 1 (ROCK1) inhibitors along with cellular and molecular biology data have revealed a pivotal role of this enzyme in many aspects of cardiovascular function. Here we report a series of ROCK1 inhibitors which were originally derived from a dihydropyrimidinone core 1. Our efforts focused on the optimization of dihydropyrimidine 2, which resulted in the identification of a series of dihydropyrimidines with improved pharmacokinetics and P450 properties.
