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pubmed-article:20471253pubmed:abstractTextThe discovery and SAR of a series of beta-aryl substituted pyrrolidine 2H-isoquinolin-1-one inhibitors of Rho-kinase (ROCK) derived from 2 is herein described. SAR studies have shown that aryl groups in the beta-position are optimal for potency. Our efforts focused on improving the ROCK potency of this isoquinolone class of inhibitors which led to the identification of pyrrolidine 32 which demonstrated a 10-fold improvement in aortic ring (AR) potency over 2.lld:pubmed
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pubmed-article:20471253pubmed:copyrightInfoCopyright 2010 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:20471253pubmed:articleTitleSubstituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.lld:pubmed
pubmed-article:20471253pubmed:affiliationDepartment of Medicinal Chemistry, Boehringer-Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877-0368, USA. todd.bosanac@boehringer-ingelheim.comlld:pubmed
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