Synthesis of new hetero- and carbocyclic aromatic amides of glycyrrhizic acid as potential anti-HIV agents |
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Authors: | R. M. Kondratenko,L. A. Baltina,L. A. Baltina. Suffix" >Jr.,O. A. Plyasunova,A. G. Pokrovskii,G. A. Tolstikov |
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Affiliation: | (1) Bashkir State Medical University, Ufa, Russia;(2) Institute of Organic Chemistry, Ufa Scientific Centre, Russian Academy of Sciences, Ufa, Russia;(3) State Scientific Center VB “Vektor”, Novosibirsk Region, Kol’tsovo, Russia; |
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Abstract: | Members of a new group of di- and trisubstituted amides of glycyrrhizic acid (GA), the major component of licorice root extract, were synthesized; derivatives contained fragments of heterocyclic and aromatic amines (2-aminopyridine, 4-aminopyridine, 5-aminouracil, sulfadimezine, sulfapyridazine, and L-histidine methyl ester) using the dicyclohexylcarbodiimide method. Amides of GA containing 2-aminopyridine and 5-aminopurine residues had anti-HIV-1 activity in MT-4 cell cultures. The index of selectivity (IS) of the amide of GA with 5-aminouracil was, using various parameters, from 27.73 to 277.32, exceeding values for GA (from 4.45 to 24.0). |
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