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 C Schuerer, Alok Pachori, Philip Lograsso, Yangbo Feng

Research output: Contribution to journalArticle

33 Citations (Scopus)

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
Pages (from-to)175-179
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume1
Issue number4
DOIs
StatePublished - Aug 27 2010

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rho-Associated Kinases
Intraocular Pressure
Solubility
Urea
Rats
Phosphotransferases
Swine
Enzymes
Therapeutics

Keywords

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

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

Cite this

Discovery of potent and selective urea-based ROCK inhibitors and their effects on intraocular pressure in rats. / Yin, Yan; Cameron, Michael D.; Lin, Li; Khan, Susan; Schröter, Thomas; Grant, Wayne; Pocas, Jennifer; Chen, Yen Ting; Schuerer, Stephan C; Pachori, Alok; Lograsso, Philip; Feng, Yangbo.

In: ACS Medicinal Chemistry Letters, Vol. 1, No. 4, 27.08.2010, p. 175-179.

Research output: Contribution to journalArticle

Yin, Y, Cameron, MD, Lin, L, Khan, S, Schröter, T, Grant, W, Pocas, J, Chen, YT, Schuerer, SC, Pachori, A, Lograsso, P & Feng, Y 2010, 'Discovery of potent and selective urea-based ROCK inhibitors and their effects on intraocular pressure in rats', ACS Medicinal Chemistry Letters, vol. 1, no. 4, pp. 175-179. https://doi.org/10.1021/ml1000382
Yin, Yan ; Cameron, Michael D. ; Lin, Li ; Khan, Susan ; Schröter, Thomas ; Grant, Wayne ; Pocas, Jennifer ; Chen, Yen Ting ; Schuerer, Stephan C ; Pachori, Alok ; Lograsso, Philip ; Feng, Yangbo. / Discovery of potent and selective urea-based ROCK inhibitors and their effects on intraocular pressure in rats. In: ACS Medicinal Chemistry Letters. 2010 ; Vol. 1, No. 4. pp. 175-179.
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