Synthesis and Antiviral Activity of Substituted Ethyl-2-Aminomethyl-5-Hydroxy-1H-Indole-3-Carboxylic Acids and Their Derivatives

Autor:	O. M. Korzinov, V. Yu. Vedenskii, Vadim V. Bichko, Andrey Alexandrovich Ivashchenko, Ya. A. Ivanenkov, Elena A. Bulanova, Oleg D. Mitkin, Ilya Okun, Alexandre Vasilievich Ivachtchenko, I. A. Leneva, V. M. Kisil, Pavel M. Yamanushkin
Rok vydání:	2015
Předmět:	Pharmacology Indole test Chemistry Stereochemistry viruses Hepatitis C virus Pharmacology toxicology virus diseases Influenza a Ethyl ester INFLUENZA PNEUMONIA medicine.disease_cause Virology Virus Drug Discovery medicine Viral diarrhea
Zdroj:	Pharmaceutical Chemistry Journal. 49:151-162
ISSN:	1573-9031 0091-150X
DOI:	10.1007/s11094-015-1244-6
Popis:	Novel substituted 5-hydroxy-2-aminomethyl-1H-indole-3-carboxylic acids and their derivatives were synthesized. The antiviral properties of these compounds were investigated in relation to bovine viral diarrhea virus (BVDV), hepatitis C virus (HCV), and influenza A/Aichi/2/69 (H3N2) virus. Of the compounds synthesized here, only the 5-hydroxy-2-(dimethylaminomethyl)-1-methyl-6-pyridin-3-yl- and 5-hydroxy-2-(dimethylaminomethyl)-1-methyl-6-fluoro-1H-indole-3-carboxylic acid ethyl ester hydrochlorides had significant activity against these viruses, these agents not only suppressing the replication of influenza A/Aichi/2/69 (H3N2) virus in cell cultures at micromolar concentrations, but also demonstrating high efficacy, greater than that of Arbidol, in a model of influenza pneumonia in mice infected with influenza A/Aichi/2/69 (H3N2) virus, when given at a dose of 25 mg/kg/day.
Databáze:	OpenAIRE
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