1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV‑1 Vif Antagonists
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https://figshare.com/articles/dataset/1_2_3-Triazoles_as_Amide_Bioisosteres_Discovery_of_a_New_Class_of_Potent_HIV_1_Vif_Antagonists/3569259
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资源简介：
RN-18 based viral
infectivity factor (Vif), Vif antagonists reduce
viral infectivity by rescuing APOBEC3G (A3G) expression and enhancing
A3G-dependent Vif degradation. Replacement of amide functionality
in RN-18 (IC50 = 6 μM) by isosteric heterocycles
resulted in the discovery of a 1,2,3-trizole, 1d (IC50 = 1.2 μM). We identified several potent HIV-1 inhibitors
from a 1d based library including 5ax (IC50 = 0.01 μM), 5bx (0.2 μM), 2ey (0.4 μM), 5ey (0.6 μM), and 6bx (0.2 μM).
创建时间：
2016-08-19
