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American Chemical Society, ACS Medicinal Chemistry Letters, 4(1), p. 175-179, 2010

DOI: 10.1021/ml1000382

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

Journal article published in 2010 by Yan Yin, Michael D. Cameron ORCID, Li Lin, Susan Khan, Thomas Schröter, Wayne Grant, Jennifer Pocas, Yen Ting Chen, Stephan Schürer, Alok Pachori, Philip LoGrasso, Yangbo Feng
This paper is available in a repository.
This paper is available in a repository.

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Abstract

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.Keywords (keywords): Glaucoma; ROCK; IOP; kinase inhibitor; urea; pyrazole