Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma
BA Harrison, NA Whitlock, MV Voronkov… - Journal of medicinal …, 2009 - ACS Publications
BA Harrison, NA Whitlock, MV Voronkov, ZY Almstead, K Gu, R Mabon, M Gardyan…
Journal of medicinal chemistry, 2009•ACS PublicationsThe 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.
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.
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.
ACS Publications