期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 17, 页码 5153-5156出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.014
关键词
Rho-kinase inhibitors
Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this series to improve metabolic stability and rat oral exposure. Piperidine analog 20 which demonstrates sustained blood pressure normalization in an SHR blood pressure reduction model was identified through this effort. (C) 2010 Elsevier Ltd. All rights reserved.
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