Discovery of Potent and Selective Urea-Based ROCK Inhibitors and Their Effects on Intraocular Pressure in Rats

Yin, Yan; Cameron, Michael D.; Lin, Li; Khan, Susan; Schröter, Thomas; Grant, Wayne; Pocas, Jennifer; Chen, Yen Ting; Schürer, Stephan; Pachori, Alok; LoGrasso, Philip; Feng, Yangbo

doi:10.1021/ml1000382.s001

ml1000382_si_001.pdf (303.95 kB)

Discovery of Potent and Selective Urea-Based ROCK Inhibitors and Their Effects on Intraocular Pressure in Rats

journal contribution

posted on 2010-07-08, 00:00 authored by Yan Yin, Michael D. Cameron, Li Lin, Susan Khan, Thomas Schröter, Wayne Grant, Jennifer Pocas, Yen Ting Chen, Stephan Schürer, Alok Pachori, Philip LoGrasso, Yangbo Feng

A series of urea-based Rho kinase (ROCK) inhibitors were designed and evaluated. The discovered compounds had excellent enzyme and cellular potency, high kinase selectivity, high aqueous solubility, good porcine corneal penetration, and appropriate DMPK profiles for topical applications as antiglaucoma therapeutics.