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

  作者 YIN YAN; CAMERON MICHAEL D; LIN LI; KHAN SUSAN; SCHROETER THOMAS; GRANT WAYNE; POCAS JENNIFER; CHEN YEN TING; SCHUERER STEPHAN; PACHORI ALOK; LOGRASSO PHILIP; FENG YANGBO  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2010年1-4;  页码  175-179  
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[摘要]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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