APPLICATION OF A TRICYCLIC SULPHUR-CONTAINING DERIVATIVE OF 1,2-DIHYDROQUINOLINE FOR INHIBITING THE REPLICATION OF BETACORONAVIRUSES, INCLUDING SARS-COV-2 Russian patent published in 2022 - IPC C07D495/04 A61K31/4365 A61P31/14 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to the field of pharmacology and medicine, namely, to an application of a tricyclic sulphur-containing derivative of 1,2-dihydroquinoline by the general formula (I) for inhibiting the replication of a betacoronavirus, including SARS-CoV-2. Compounds by the formula (I) exhibit low toxicity and can be used to treat diseases caused by betacoronaviruses, including SARS-CoV-2. In the general formula (I), R1 constitutes a substituent selected from a methyl, ethyl, methoxy, ethoxy group; R2 constitutes a substituent selected from a methyl, ethyl, methoxy, ethoxy group; R3 constitutes a substituent selected from a methyl, ethyl, methoxy, ethoxy group; R4 constitutes a substituent selected from a methyl, benzyl, 3-phenylacryloyl, 3-(4-methoxyphenyl)acryloyl, 3-phenylpropanoyl, phenylethyl, 2-(4-fluorophenoxy)acetyl, 4-chlorophenoxyacetyl, 2-(2,4-dichlorophenoxy)acetyl, 4-nitrobenzoyl, 2-(1,3-dioxoisoindoline-2-yl)-3-phenylpropanoyl) group; 3,4-dichlorophenylcarbamoyl, furan-2-carbonyl, ethylcarbamoyl, 2-naphthylyloxyacetyl, 2-(1,3-dioxoisoindoline-2-yl)acetyl, 2-(1,3-dioxohexahydro-1H-isoindole-2(3H)-yl)acetyl, 2-morpholinoacetyl, piperidine-1-ylacetyl, 2-(4-carbamoylpiperidine-1-yl)acetyl, 2-(2,5-dioxopyrrolidine-1-yl)acetyl, 2-phenoxyacetyl, 2-1,3-dioxo-1H-benzo[de]isoquinoline-2(3H)-yl)acetyl, 2-benzo[d]oxazole-2-ylthio)acetyl, 2-(benzo[d]thiazole-2-yloxy)acetyl, benzoxazole-2-ylmercaptoacetyl, furanoyl, 2-naphlinylyoxymethylcarbonyl, 3,4-dichlorophenylcarbamoyl; X constitutes a substituent selected from sulphur, unsubstituted or substituted in positions 2,3,4,5,6-arylamine selected from a group including 4-(4-chlorobenzyloxy)phenylimino, 4-isopropylphenylimino, 4-(6-methylbenzo[d]thiazole-2-yl)phenylimino, 4-(N-benzoylsulphamoyl)phenylimino, 4-ethoxyphenylimino, 4-ethoxycarbonylphenylimino, phenylimino, 4-chlorphenylimino, 3-chlorphenylimino, 4-sulphamoylphenylimino, 4-(N-acetylsulphamoyl)phenylimino, 4-(N-(thiazole-2-yl)sulphamoyl)phenylimino, 2-nicotinoylhydrazono, 4-((4-chlorobenzyl)oxy)phenylimino, 2-methoxyphenylimino, 4-(N-(pyrimidine-2-yl)sulphamoyl)phenylimino, 4-(N-(4,6-dimethylpyrimidine-2-yl)sulphamoyl)phenylimino.

EFFECT: effective inhibition of the replication of betacoronaviruses, including SARS-CoV-2, characterised by high efficiency of inhibiting the replication of coronavirus in the Vero E6 cell culture at low values of the effective EC50 concentration, low cytotoxicity, and high value of selectivity index SI.

4 cl, 1 dwg, 1 tbl, 20 ex