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Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.

Authors
  • Hu, Zilun1
  • Wang, Cailan2
  • Glunz, Peter W2
  • Li, Julia2
  • Cheadle, Nathan L2
  • Chen, Alice Y2
  • Chen, Xue-Qing2
  • Myers, Joseph E2
  • Guarino, Victor R2
  • Rose, Anne2
  • Sack, John S2
  • Sitkoff, Doree2
  • Taylor, David S2
  • Xu, Songmei2
  • Yan, Chunhong2
  • Zhang, Hongwei2
  • Zhang, Lisa2
  • Hennan, James2
  • Adam, Leonard P2
  • Wexler, Ruth R2
  • And 1 more
  • 1 Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA. Electronic address: [email protected]
  • 2 Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Aug 13, 2020
Volume
30
Issue
21
Pages
127495–127495
Identifiers
DOI: 10.1016/j.bmcl.2020.127495
PMID: 32798651
Source
Medline
Keywords
Language
English
License
Unknown

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. Copyright © 2020 Elsevier Ltd. All rights reserved.

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