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Exploring the cycloheptathiophene-3-carboxamide scaffold to disrupt the interactions of the influenza polymerase subunits and obtain potent anti-influenza activity

Eur J Med Chem.. 2018-08; 
Desantis J, Nannetti G, Massari S, Barreca ML, Manfroni G, Cecchetti V, Palù G, Goracci L, Loregian A, Tabarrini O.
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摘要

With the aim to identify small molecules able to disrupt PA-PB1 subunits interaction of influenza virus (flu) RNA-dependent RNA polymerase, and based on previous structural and computational information, in this paper we have designed and synthesized a new series of cycloheptathiophene-3-carboxamide (cHTC) derivatives. Their biological evaluation led to highlight important structural insights along with new interesting compounds, such as the 2-hydroxybenzamido derivatives 29, 31, and 32, and the 4- aminophenyl derivative 54, which inhibited viral growth in the low micromolar range (EC50 ¼ 0.18 e1.2 mM) at no toxic concentrations (CC50 > 250 mM). This study permitted to obtain among the most potent anti-... More

关键词

PA-PB1 interaction Influenza virus polymerase Protein-protein interaction inhibitors Influenza virus inhibitors