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 journalArticlepeer-review

74 Scopus citations


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
Issue number24
StatePublished - Dec 15 2008
Externally publishedYes


  • 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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