title: 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.
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Yan
authors.initials: Y
authors.lastname: Yin
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Michael D
authors.initials: MD
authors.lastname: Cameron
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Susan
authors.initials: S
authors.lastname: Khan
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Thomas
authors.initials: T
authors.lastname: Schröter
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Wayne
authors.initials: W
authors.lastname: Grant
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Jennifer
authors.initials: J
authors.lastname: Pocas
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Yen Ting
authors.initials: YT
authors.lastname: Chen
authors.affiliation: Department of Pharmacology and Center for Computational Science, University of Miami, Miami, Florida 33136.
authors.forename: Stephan
authors.initials: S
authors.lastname: Schürer
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Alok
authors.initials: A
authors.lastname: Pachori
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Philip
authors.initials: P
authors.lastname: LoGrasso
authors.affiliation: Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
authors.forename: Yangbo
authors.initials: Y
authors.lastname: Feng
keywords: Glaucoma; IOP; ROCK; kinase inhibitor; pyrazole; urea