Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors

被引:29
作者
Fang, Xingang
Chen, Yen Ting [1 ]
Sessions, E. Hampton
Chowdhury, Sarwat
Vojkovsky, Tomas
Yin, Yan
Pocas, Jennifer R.
Grant, Wayne
Schroeter, Thomas
Lin, Li
Ruiz, Claudia
Cameron, Michael D.
LoGrasso, Philip
Bannister, Thomas D.
Feng, Yangbo
机构
[1] Scripps Res Inst, Translat Res Inst, Jupiter, FL 33458 USA
关键词
Rho kinase; Quinazolinone; Pyrazole; ROCK inhibitor; Protein kinase A; INTRAOCULAR-PRESSURE; ROCK INHIBITORS; POTENT; DISCOVERY;
D O I
10.1016/j.bmcl.2011.01.039
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Rho kinase ( ROCK) is an attractive therapeutic target for various diseases including glaucoma, hypertension, and spinal cord injury. Herein, we report the development of a series of ROCK-II inhibitors based on 4-quinazolinone and quinazoline scaffolds. SAR studies at three positions of the quinazoline core led to the identification of analogs with high potency against ROCK-II and good selectivity over protein kinase A (PKA). (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1844 / 1848
页数:5
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