Synthesis and Monoamine Oxidase Inhibition Properties of (Sulfamoylphenyl)quinoline-4-carboxylic Acids

By reaction between acetylbenzenesulfonamides with several substituted isatins, we have synthesized a series of 22 primary sulfonamides, 16 of which were tested for inhibition activity against MAO-A and MAO-B. At the same time, in order to diversify the resulting structures, we have carried out decarboxylation as well as further functionalization at the carboxylic acid. The results of the study show that methyl 6-chloro-2-(3-sulfamoylphenyl)quinoline-4-carboxylate selectively inhibited MAO-B with a value of IC50 = 13.7 μM.

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Journal
Russian Journal of General Chemistry
Published
2024-10-01
DOI
https://doi.org/10.1134/s1070363224100049
Primary Topic
Synthesis and Biological Evaluation
Type
article
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article

Synthesis and Monoamine Oxidase Inhibition Properties of (Sulfamoylphenyl)quinoline-4-carboxylic Acids

Jacobus P. Petzer, Anton A. Shetnev, М. К. Корсаков, Julia A. Efimova et al.
Russian Journal of General Chemistry
Synthesis and Biological Evaluation
article

Synthesis and Monoamine Oxidase Inhibition Properties of (Sulfamoylphenyl)quinoline-4-carboxylic Acids

Jacobus P. Petzer, Anton A. Shetnev, М. К. Корсаков, Julia A. Efimova, Anél Petzer, Eugene E. Petersen
article en

Abstract

By reaction between acetylbenzenesulfonamides with several substituted isatins, we have synthesized a series of 22 primary sulfonamides, 16 of which were tested for inhibition activity against MAO-A and MAO-B. At the same time, in order to diversify the resulting structures, we have carried out decarboxylation as well as further functionalization at the carboxylic acid. The results of the study show that methyl 6-chloro-2-(3-sulfamoylphenyl)quinoline-4-carboxylate selectively inhibited MAO-B with a value of IC50 = 13.7 μM.

Russian Journal of General ChemistryVol. 94(10)
A. N. Kosygin Moscow State Textile University (RU), Moscow Institute of Physics and Technology (RU), North-West University (ZA), Yaroslavl State Pedagogical University (RU)
Clean water and sanitation
Openalex Percentile: Top 85%
Synthesis and Biological Evaluation
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