GUANIDINOADAMANTANES - DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY.

Autor: Chayrov, Radoslav, Chuchkov, Kiril, Tencheva, Aleksandra, Galabov, Angel, Yurukov, Borislav, Stankova, Ivanka
Předmět:
Zdroj: Journal of Chemical Technology & Metallurgy; 2022, Vol. 57 Issue 4, p718-722, 5p
Abstrakt: Influenza virus is one of the most mutant viruses during the years. Since more than 30 years adamantane derivatives are successfully used for prevention and treatment of influenza virus type A. Unfortunately, due to virus mutations the effect of many medical drugs is lost or drastically diminished. Herein, we report our study where a specific modification in the amino group of two anti-influenza medical drugs amantadine and rimantadine was done. The transformation of amino to guanidine group is a possible approach to overcome the resistance of virus. This modification was realized by means of 1H-pyrazole-1-carboxamidine. The newly obtained auanidoadamantanes were tested for their antiviral activity against influenza virus strain A/Aichi/H3N2. The cytotoxicity expressed as CC50 and inhibition concentrations IC50 were determined and the selective index was calculated. The obtained data revealed that both modified compounds have high antiviral activity, which is better in the guanidinorimantadine with a selective index 3396. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index