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

Discovery of Potent and Selective Urea-Based ROCK Inhibitors and Their Effects on Intraocular Pressure in Rats.
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DOI:
10.1021/ml1000382
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发表时间:
2010-04
影响因子:
4.2
通讯作者:
Yan Yin;M. Cameron;Li Lin;Susan Khan;T. Schröter;Wayne Grant;J. Pocas;Y. Chen;S. Schürer
Yan Yin;M. Cameron;Li Lin;Susan Khan;T. Schröter;Wayne Grant;J. Pocas;Y. Chen;S. Schürer
中科院分区:
医学3区
文献类型:
--
作者:
Yan Yin;M. Cameron;Li Lin;Susan Khan;T. Schröter;Wayne Grant;J. Pocas;Y. Chen;S. Schürer

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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.