Water-soluble PDE4 inhibitors for the treatment of dry eye.

Article Details

Citation

Govek SP, Oshiro G, Anzola JV, Beauregard C, Chen J, Coyle AR, Gamache DA, Hellberg MR, Hsien JN, Lerch JM, Liao JC, Malecha JW, Staszewski LM, Thomas DJ, Yanni JM, Noble SA, Shiau AK

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. Epub 2010 Mar 7.

PubMed ID
20378348 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PiclamilastcAMP-specific 3',5'-cyclic phosphodiesterase 4BIC 50 (nM)2N/AN/ADetails