کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10596167 981897 2013 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Inhibitors of HIV-1 attachment. Part 8: The effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Inhibitors of HIV-1 attachment. Part 8: The effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors
چکیده انگلیسی
Optimization of the early lead compound 2 with heteroaryl substitution at the C7 position identified inhibitors with picomolar inhibitory activity. These C7-heteroaryl-indole analogs maintained the ligand efficiency (LE) of 2 and were also lipophilic efficient as measured by LLE and LELP. The highly permeable 1,2,4-oxadiazole analog 13 exhibited the highest oral exposure in rats.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 1, 1 January 2013, Pages 203-208
نویسندگان
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