Tassini, S; Sun, L; Lanko, K; Crespan, E; Langron, E; Falchi, F; Kissova, M; ... Radi, M; + view all Tassini, S; Sun, L; Lanko, K; Crespan, E; Langron, E; Falchi, F; Kissova, M; Armijos-Rivera, JI; Delang, L; Mirabelli, C; Neyts, J; Pieroni, M; Cavalli, A; Costantino, G; Maga, G; Vergani, P; Leyssen, P; Radi, M; - view fewer (2017) Discovery of Multi-Target Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) for Associated Pulmonary Diseases. Journal of Medicinal Chemistry 10.1021/acs.jmedchem.6b01521. (In press).

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Abstract

Enteroviruses (EVs) are among the most frequent infectious agents in humans worldwide and represent the leading cause of upper respiratory tract infections. No drugs for the treatment of EV infections are currently available. Recent studies have also linked enterovirus infection with pulmonary exacerbations, especially in cystic fibrosis (CF) patients, and the importance of this link is probably underestimated. The aim of this work was to develop a new class of multi-target agents active both as broad-spectrum antivirals and as correctors of the F508del-CFTR folding defect responsible for >90% of CF cases. We report herein the discovery of the first small-molecules able to simultaneously act as correctors of the F508del-CFTR folding defect and as broad-spectrum antivirals against a panel of enteroviruses representative of all major species.

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