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Amphiphilic Sialic Acid Derivatives as Potential Dual-Specific Inhibitors of Influenza Hemagglutinin and Neuraminidase

EB. Lőrincz, M. Herczeg, J. Houser, M. Rievajová, Á. Kuki, L. Malinovská, L. Naesens, M. Wimmerová, A. Borbás, P. Herczegh, I. Bereczki

. 2023 ; 24 (24) : . [pub] 20231208

Jazyk angličtina Země Švýcarsko

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc24000277

Grantová podpora
FK 142315 National Research, Development and Innovation Office
RRF-2.3.1-21-2022-00010 National Laboratory of Virology in Hungary
LM2023042 MEYS CR
CZ.02.1.01/0.0/0.0/18_046/0015974 European Regional Development Fund-Project

In the shadow of SARS-CoV-2, influenza seems to be an innocent virus, although new zoonotic influenza viruses evolved by mutations may lead to severe pandemics. According to WHO, there is an urgent need for better antiviral drugs. Blocking viral hemagglutinin with multivalent N-acetylneuraminic acid derivatives is a promising approach to prevent influenza infection. Moreover, dual inhibition of both hemagglutinin and neuraminidase may result in a more powerful effect. Since both viral glycoproteins can bind to neuraminic acid, we have prepared three series of amphiphilic self-assembling 2-thio-neuraminic acid derivatives constituting aggregates in aqueous medium to take advantage of their multivalent effect. One of the series was prepared by the azide-alkyne click reaction, and the other two by the thio-click reaction to yield neuraminic acid derivatives containing lipophilic tails of different sizes and an enzymatically stable thioglycosidic bond. Two of the three bis-octyl derivatives produced proved to be active against influenza viruses, while all three octyl derivatives bound to hemagglutinin and neuraminidase from H1N1 and H3N2 influenza types.

Citace poskytuje Crossref.org

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