Design, synthesis and biological evaluation of oxalamide derivatives as potent neuraminidase inhibitors

In recent decades, the world has gained experience of the dangerous effects of pandemic events caused by emerging respiratory viruses. In particular, annual epidemics of influenza are responsible for severe illness and deaths. Even if conventional influenza vaccines represent the most effective tool for preventing virus infections, they are not completely effective in patients with severe chronic disease and immunocompromised and new small molecules have emerged to prevent and control the influenza viruses. Thus, the attention of chemists is continuously focused on the synthesis of new antiviral drugs able to interact with the different molecular targets involved in the virus replication cycle. To date, different classes of influenza viruses inhibitors able to target neuraminidase enzyme, hemagglutinin protein, Matrix-2 (M2) protein ion channel, nucleoprotein or RNA-dependent RNA polymerase have been synthesized using several synthetic strategies comprising the chemical modification of currently used drugs. The best results, in terms of inhibitory activity, are in the nanomolar range and have been obtained from the chemical modification of clinically used drugs such as Peramivir, Zanamivir, Oseltamir, Rimantadine, as well as sialylated molecules, and hydroxypyridinone derivatives. The aim of this review is to report, covering the period 2016-2022, the most recent routes related to the synthesis of effective influenza virus inhibitors.

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Design, synthesis and biological evaluation of oxalamide derivatives as potent neuraminidase inhibitors

Abstract: Neuraminidase (NA) is an effective target for research and development of anti-influenza drugs. Herein, based on structure-based virtual screening, it was found that ZINC05250774, a oxalamide derivative, was a lead...

Cited by 2 publications

References 26 publications

TBN-promoted regioselective C–C bond cleavage: a new strategy for the synthesis of unsymmetrically substituted N-aryl oxalamides

TBN-promoted regioselective C–C bond cleavage: a new strategy for the synthesis of unsymmetrically substituted N-aryl oxalamides

Antiviral Compounds to Address Influenza Pandemics: An Update from 2016-2022

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