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Elsevier, Bioorganic and Medicinal Chemistry Letters, 6(21), p. 1844-1848

DOI: 10.1016/j.bmcl.2011.01.039

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

Journal article published in 2011 by Xingang Fang, Yen Ting Chen, E. Hampton Sessions, E. Hampton Sessions, Sarwat Chowdhury, Tomas Vojkovsky, Yan Yin, Jennifer R. Pocas, Wayne Grant, Thomas Schröter, Li Lin, Claudia Ruiz, Michael D. Cameron ORCID, Philip LoGrasso, Thomas D. Bannister and other authors.
This paper is available in a repository.
This paper is available in a repository.

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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).