| Literature DB >> 19831390 |
Bryce A Harrison1, N Andrew Whitlock, Michael V Voronkov, Zheng Y Almstead, Kun-jian Gu, Ross Mabon, Michael Gardyan, Brian D Hamman, Jason Allen, Suma Gopinathan, Beth McKnight, Mike Crist, Yulian Zhang, Ying Liu, Lawrence F Courtney, Billie Key, Julia Zhou, Nita Patel, Phil W Yates, Qingyun Liu, Alan G E Wilson, S David Kimball, Craig E Crosson, Dennis S Rice, David B Rawlins.
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.Entities:
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Year: 2009 PMID： 19831390 DOI： 10.1021/jm901226j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446