کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10595140 981858 2013 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility
چکیده انگلیسی
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 18, 15 September 2013, Pages 5213-5216
نویسندگان
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