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Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors |
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| Authors: | Fang Xingang Chen Yen Ting Sessions E Hampton Chowdhury Sarwat Vojkovsky Tomas Yin Yan Pocas Jennifer R Grant Wayne Schröter Thomas Lin Li Ruiz Claudia Cameron Michael D LoGrasso Philip Bannister Thomas D Feng Yangbo |
| Affiliation: | Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #2A1, Jupiter, FL 33458, USA |
| Abstract: | 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). |
| Keywords: | Rho kinase Quinazolinone Pyrazole ROCK inhibitor Protein kinase A |
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