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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. 2017; 
Desantis Jenny,Nannetti Giulio,Massari Serena,Barreca Maria Letizia,Manfroni Giuseppe,Cecchetti Violetta,Palù Giorgio,Goracci Laura,Loregian Arianna,Tabarrini Or
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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 (EC?=?0.18-1.2?μM) at no toxic concentrations (CC?>?250?μM). This study permitted to obtain among the most potent ant... More

关键词

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