کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594382 | 981826 | 2012 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs](/preview/png/10594382.png)
چکیده انگلیسی
The 1,2,4-triazin-6-ylthioacetamides were identified as potent NNRTIs designed by structure-based bioisosterism strategy. The HIV-1(IIIB) inhibitory activity of compound 8b15 (EC50 = 0.018 ± 0.007 μM) was about seventy-eight, eleven and two fold more active than that of positive control drugs DDC, NVP and DLV respectively, and displayed similar anti-HIV-1 activity as that of EFV. Because of their excellent potency, these 1,2,4-triazin-6-yl thioacetamide derivatives may have antiviral potential and should be further pursued as next-generation NNRTIs.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7155-7162
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7155-7162
نویسندگان
Peng Zhan, Xiao Li, Zhenyu Li, Xuwang Chen, Ye Tian, Wenmin Chen, Xinyong Liu, Christophe Pannecouque, Erik De Clercq,