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Bioorg Med Chem Lett. 2010 Feb 1;20(3):1137-40. doi: 10.1016/j.bmcl.2009.12.012. Epub 2009 Dec 5.
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.
抑制 Rho 激酶（ROCK）已被认为是许多疾病的重要靶点，包括青光眼。在此，我们报告了从激酶文库中发现两个苗头化合物开始的 SAR 研究进展，这导致了 ROCK 抑制剂化合物 38 的发现。将讨论该化合物的体外和体内分析，包括其在青光眼猴模型中的作用。
