Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.

Abstract:

: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.

journal_name

J Med Chem

authors

Harrison BA,Whitlock NA,Voronkov MV,Almstead ZY,Gu KJ,Mabon R,Gardyan M,Hamman BD,Allen J,Gopinathan S,McKnight B,Crist M,Zhang Y,Liu Y,Courtney LF,Key B,Zhou J,Patel N,Yates PW,Liu Q,Wilson AG,Kimball SD,Cros

doi

10.1021/jm901226j

subject

Has Abstract

pub_date

2009-11-12 00:00:00

pages

6515-8

issue

21

eissn

0022-2623

issn

1520-4804

journal_volume

52

pub_type

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