Published in
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
,
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 ,
Philip LoGrasso,
Thomas D. Bannister
and other authors.
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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).