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The discovery of a pyrrolopyrimidine class of LIM-kinase 2 (LIMK2) inhibitors is reported. These LIMK2 inhibitors show good potency in enzymatic and cellular assays and good selectivity against ROCK. After topical dosing to the eye in a steroid induced mouse model of ocular hypertension, the compounds reduce intraocular pressure to baseline levels. The compounds also increase outflow facility in a pig eye perfusion assay. These results suggest LIMK2 may be an effective target for treating ocular hypertension and associated glaucoma.
B. A. Harrison. Department of Medicinal Chemistry, Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States. bharrison@lexpharma.com
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)