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

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.

SUBMITTER: Yin Y

PROVIDER: S-EPMC4007833 | biostudies-other | 2010 Jul

REPOSITORIES: biostudies-other

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

Yin Yan Y Cameron Michael D MD Lin Li L Khan Susan S Schröter Thomas T Grant Wayne W Pocas Jennifer J Chen Yen Ting YT Schürer Stephan S Pachori Alok A LoGrasso Philip P Feng Yangbo Y

ACS medicinal chemistry letters 20100405 4

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. ...[more]

PMID: 24900192

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