Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594382 | Bioorganic & Medicinal Chemistry Letters | 2012 | 8 Pages |
Abstract
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.
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Authors
Peng Zhan, Xiao Li, Zhenyu Li, Xuwang Chen, Ye Tian, Wenmin Chen, Xinyong Liu, Christophe Pannecouque, Erik De Clercq,