Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma

Robert L. Davis, Mehmet Kahraman, Thomas J. Prins, Yan Beaver, Travis G. Cook, Jessica Cramp, Charmagne S. Cayanan, Elisabeth M.M. Gardiner, Marsha A. McLaughlin, Abbot F. Clark, Mark R. Hellberg, Andrew K. Shiau, Stewart A. Noble, Allen J. Borchardt

Research output: Contribution to journalArticle

20 Scopus citations

Abstract

We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intraocular pressure in a monkey model of glaucoma-associated ocular hypertension.

Original languageEnglish
Pages (from-to)3361-3366
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number11
DOIs
StatePublished - 1 Jun 2010

Keywords

  • ATP competitive
  • Adhesion
  • Benzothiophene
  • Glaucoma
  • Impedance
  • Inhibitor
  • Kinase
  • ROCK
  • Rho

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    Davis, R. L., Kahraman, M., Prins, T. J., Beaver, Y., Cook, T. G., Cramp, J., Cayanan, C. S., Gardiner, E. M. M., McLaughlin, M. A., Clark, A. F., Hellberg, M. R., Shiau, A. K., Noble, S. A., & Borchardt, A. J. (2010). Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma. Bioorganic and Medicinal Chemistry Letters, 20(11), 3361-3366. https://doi.org/10.1016/j.bmcl.2010.04.020