کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370755 | 981828 | 2011 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
We have synthesized and evaluated a new series of acyclic P4-benzoxaborole-based HCV NS3 protease inhibitors. Structure–activity relationships were investigated, leading to the identification of compounds 5g and 17 with low nanomolar potency in the enzymatic and cell-based replicon assay. The linker-truncated compound 5j was found to exhibit improved absorption and oral bioavailability in rats, suggesting that further reduction of molecular weight and polar surface area could result in improved drug-like properties of this novel series.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 7, 1 April 2011, Pages 2048–2054
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 7, 1 April 2011, Pages 2048–2054
نویسندگان
Xianfeng Li, Suoming Zhang, Yong-Kang Zhang, Yang Liu, Charles Z. Ding, Yasheen Zhou, Jacob J. Plattner, Stephen J. Baker, Wei Bu, Liang Liu, Wieslaw M. Kazmierski, Maosheng Duan, Richard M. Grimes, Lois L. Wright, Gary K. Smith, Richard L. Jarvest,