کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369550 | 981782 | 2014 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 2,3,6-pyrazine Rho Kinase inhibitors were optimized for in vivo activity for topical ocular dosing. Modifications of the 2-(piperazin-1-yl)pyrazine derivatives produced compounds with improved solubility and physicochemical properties. Modifications of the 6-pyrazine substituent led to improvements in in vitro potency. Compound 9 had the best in vitro and in vivo potency of EC50 = 260 nM with a 30% reduction of IOP in a non-human primate model at a dose of 0.33%.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 8, 15 April 2014, Pages 1875–1879
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 8, 15 April 2014, Pages 1875–1879
نویسندگان
Hwang-Hsing Chen, Abdelmoulah Namil, Bryon Severns, Jennifer Ward, Curtis Kelly, Colene Drace, Marsha A. McLaughlin, Shenouda Yacoub, Byron Li, Raj Patil, Naj Sharif, Mark R. Hellberg, Andrew Rusinko, Iok-Hou Pang, Keith D. Combrink,