Benzimidazole- and benzoxazole-based inhibitors of Rho kinase

E. Hampton Sessions, Yan Yin, Thomas D. Bannister, Amiee Weiser, Evelyn Griffin, Jennifer Pocas, Michael D. Cameron, Claudia Ruiz, Li Lin, Stephan C. Schürer, Thomas Schröter, Philip LoGrasso, Yangbo Feng

Research output: Contribution to journalArticle

63 Scopus citations

Abstract

Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ROCK-II with excellent potency in both enzyme and cell-based assays were obtained. These inhibitors possess good microsomal stability, low cytochrome P-450 inhibitions and good oral bioavailability.

Original languageEnglish (US)
Pages (from-to)6390-6393
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number24
DOIs
StatePublished - Dec 15 2008
Externally publishedYes

Keywords

  • Aminopyrimidine
  • Benzimidazole
  • Benzoxazole
  • Chroman
  • Glaucoma
  • Hypertension
  • Pyrazole
  • Rho kinase
  • Rock-II

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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  • Cite this

    Sessions, E. H., Yin, Y., Bannister, T. D., Weiser, A., Griffin, E., Pocas, J., Cameron, M. D., Ruiz, C., Lin, L., Schürer, S. C., Schröter, T., LoGrasso, P., & Feng, Y. (2008). Benzimidazole- and benzoxazole-based inhibitors of Rho kinase. Bioorganic and Medicinal Chemistry Letters, 18(24), 6390-6393. https://doi.org/10.1016/j.bmcl.2008.10.095