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Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies
Zilun Hu1, Cailan Wang1, Peter W Glunz1
1Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Abstract:
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.
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