TY - JOUR
T1 - 1,2,3-triazoles as amide bioisosteres
T2 - Discovery of a new class of potent HIV-1 Vif antagonists
AU - Mohammed, Idrees
AU - Kummetha, Indrasena Reddy
AU - Singh, Gatikrushna
AU - Sharova, Natalia
AU - Lichinchi, Gianluigi
AU - Dang, Jason
AU - Stevenson, Mario
AU - Rana, Tariq M.
N1 - Publisher Copyright:
© 2016 American Chemical Society.
PY - 2016/8/25
Y1 - 2016/8/25
N2 - 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, Id (IC50 = 1.2 μM). We identified several potent HIV-1 inhibitors from a Id based library including 5ax (IC50 = 0.01 μM), 5bx (0.2 μM), 2ey (0.4 μM), 5ey (0.6 μM), and 6bx (0.2 μ M).
AB - 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, Id (IC50 = 1.2 μM). We identified several potent HIV-1 inhibitors from a Id based library including 5ax (IC50 = 0.01 μM), 5bx (0.2 μM), 2ey (0.4 μM), 5ey (0.6 μM), and 6bx (0.2 μ M).
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U2 - 10.1021/acs.jmedchem.6b00247
DO - 10.1021/acs.jmedchem.6b00247
M3 - Article
C2 - 27509004
AN - SCOPUS:84983627592
SN - 0022-2623
VL - 59
SP - 7677
EP - 7682
JO - Journal of medicinal chemistry
JF - Journal of medicinal chemistry
IS - 16
ER -
