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  • Title: Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.
    Author: Fang X, Chen YT, Sessions EH, Chowdhury S, Vojkovsky T, Yin Y, Pocas JR, Grant W, Schröter T, Lin L, Ruiz C, Cameron MD, LoGrasso P, Bannister TD, Feng Y.
    Journal: Bioorg Med Chem Lett; 2011 Mar 15; 21(6):1844-8. PubMed ID: 21349713.
    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).
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