Source:http://linkedlifedata.com/resource/pubmed/id/20471253
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
2010-6-4
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pubmed:abstractText |
The 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.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3746-9
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pubmed:meshHeading |
pubmed-meshheading:20471253-Animals,
pubmed-meshheading:20471253-Aorta,
pubmed-meshheading:20471253-Crystallography, X-Ray,
pubmed-meshheading:20471253-Drug Design,
pubmed-meshheading:20471253-Hypertension,
pubmed-meshheading:20471253-Inhibitory Concentration 50,
pubmed-meshheading:20471253-Isoquinolines,
pubmed-meshheading:20471253-Molecular Structure,
pubmed-meshheading:20471253-Protein Kinase Inhibitors,
pubmed-meshheading:20471253-Pyrrolidines,
pubmed-meshheading:20471253-Rats,
pubmed-meshheading:20471253-Structure-Activity Relationship,
pubmed-meshheading:20471253-rho-Associated Kinases
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pubmed:year |
2010
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pubmed:articleTitle |
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
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pubmed:affiliation |
Department of Medicinal Chemistry, Boehringer-Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877-0368, USA. todd.bosanac@boehringer-ingelheim.com
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pubmed:publicationType |
Journal Article
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