Discovery of potent and selective urea-based ROCK inhibitors and their effects on intraocular pressure in rats

Yan Yin, Michael D. Cameron, Li Lin, Susan Khan, Thomas Schröter, Wayne Grant, Jennifer Pocas, Yen Ting Chen, Stephan Schürer, Alok Pachori, Philip Lograsso, Yangbo Feng

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

A series of urea-based Rho kinase (ROCK) inhibitors were designed and evaluated. The discovered compounds had excellent enzyme and cellular potency, high kinase selectivity, high aqueous solubility, good porcine corneal penetration, and appropriate DMPK profiles for topical applications as antiglaucoma therapeutics.

Original languageEnglish (US)
Pages (from-to)175-179
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume1
Issue number4
DOIs
StatePublished - 2010

Keywords

  • Glaucoma
  • IOP
  • kinase inhibitor
  • pyrazole
  • ROCK
  • urea

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

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