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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 06期

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

页码：1844 / 1848

页数：5

共 22 条

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ACS MEDICINAL CHEMISTRY LETTERS, 2010, 1 (04) :175-179

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