| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372102 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Inhibition of rho kinase (ROCK) has been recognized as an important target for a number of diseases, including glaucoma. Herein we report SAR development around two hits from a kinase library that led to the discovery of the ROCK inhibitor compound 38. In vitro and in vivo analysis of this compound, including its effects in a monkey model of glaucoma will be discussed.
Graphical abstractA series of 2,3-diaminopyrazines were synthesized and evaluated as rho kinase inhibitors. Compound 38 was found to have highly favorable in vitro properties, and demonstrated excellent efficacy in a monkey model of glaucoma.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Alan J. Henderson, Mark Hadden, Cheng Guo, Neema Douglas, Helene Decornez, Mark R. Hellberg, Andrew Rusinko, Marsha McLaughlin, Naj Sharif, Colene Drace, Raj Patil,