Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.
Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA. Electronic address: [email protected]
Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
- Published Article
Bioorganic & medicinal chemistry letters
- Publication Date
Aug 13, 2020
Structure-activity relationship optimization on a series of phenylpyrazole amides led to the identification of a dual ROCK1 and ROCK2 inhibitor (25) which demonstrated good potency, kinome selectivity and favorable pharmacokinetic profiles. Compound 25 was selected as a tool molecule for in vivo studies including evaluating hemodynamic effects in telemeterized mice, from which moderate decreases in blood pressure were observed. Copyright © 2020 Elsevier Ltd. All rights reserved.
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This record was last updated on 10/16/2020 and may not reflect the most current and accurate biomedical/scientific data available from NLM.
The corresponding record at NLM can be accessed at https://www.ncbi.nlm.nih.gov/pubmed/32798651