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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.
Afiliação
  • Yin Y; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Cameron MD; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Lin L; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Khan S; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Schröter T; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Grant W; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Pocas J; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Chen YT; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Schürer S; Department of Pharmacology and Center for Computational Science, University of Miami, Miami, Florida 33136.
  • Pachori A; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • LoGrasso P; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
  • Feng Y; Translational Research Institute and Department of Molecular Therapeutics, 130 Scripps Way, #2A1, Jupiter, Florida 33458.
ACS Med Chem Lett ; 1(4): 175-9, 2010 Jul 08.
Article em En | MEDLINE | ID: mdl-24900192
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2010 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2010 Tipo de documento: Article