1. Academic Validation
  2. Water-soluble PDE4 inhibitors for the treatment of dry eye

Water-soluble PDE4 inhibitors for the treatment of dry eye

  • Bioorg Med Chem Lett. 2010 May 1;20(9):2928-32. doi: 10.1016/j.bmcl.2010.03.023.
Steven P Govek 1 Guy Oshiro John V Anzola Clay Beauregard Jasmine Chen Avery R Coyle Daniel A Gamache Mark R Hellberg Jennifer N Hsien Julia M Lerch John C Liao James W Malecha Lena M Staszewski David J Thomas John M Yanni Stewart A Noble Andrew K Shiau
Affiliations

Affiliation

  • 1 Kalypsys, Inc., 10420 Wateridge Circle, San Diego, CA 92121, United States. sgovek@san.rr.com
Abstract

PDE4 inhibitors have the potential to alleviate the symptoms and underlying inflammation associated with dry eye. Disclosed herein is the development of a novel series of water-soluble PDE4 inhibitors. Our studies led to the discovery of coumarin 18, which is effective in a rabbit model of dry eye and a tear secretion test in rats.

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