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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties
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
نویسندگان
, , , , , , , , , , , , , , , ,