Synthesis and Biological Evaluation of N-Aminoalkil Derivatives of Sulfanilamide Reaction

A series of 19 derivatives of sulfanilamide was synthesized by the reaction of chloroacetamide, trichloroacetamide and chloropropionamide with N-nucleophiles. It was shown that N-trichloroacetylsulfanilamide in reactions with amines forms products of substitution of the trichloromethyl group, while N-chloroacetylsulfanilamide and N-chloropropionylsulfanilamide react with substitution of the halogen atom. An assessment of the antibacterial properties of the synthesized structures was carried out, showing the absence of activity with respect to E. coli and St. aureus strains. Two aminoalkyl-containing sulfonamides - 2-(4-benzylpiperidin-1-yl)-N-(4-sulfamoylphenyl)acetamide and 2-(4-nitropyrazol-1-yl)-N-(4-sulfamoylphenyl)acetamide - showed inhibitory properties against the human monoamine oxidase enzyme, comparable in IC50 value to the drug zonisamide.

Keywords

сульфонамид N-алкилирование моноаминооксидаза ингибитор антимикробная активность

Date of publication

06.02.2026

Year of publication

2026

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References

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GOST	Belchenko M., Grunina E., Korovina A., Kotov A., Petzer A., Petzer J., Proskurina I., Romanycheva A., Shetnev A., Vasil'eva E. Synthesis and Biological Evaluation of N-Aminoalkil Derivatives of Sulfanilamide Reaction // Russian Journal of General Chemistry. – 2025. – V. 95. – Issue number 3-4 C. 80-91 . URL: https://genchemras.ru/s30345596s0044460x25030013-1/?version_id=123126. DOI: 10.7868/S3034559625030013
MLA	Belchenko, M. V, Grunina, E. O, Korovina, A. V, Kotov, A. D, Petzer, A., Petzer, J., Proskurina, I. K, Romanycheva, A.A, Shetnev, A. A, Vasil'eva, E.A "Synthesis and Biological Evaluation of N-Aminoalkil Derivatives of Sulfanilamide Reaction." Russian Journal of General Chemistry. 95.3-4 (2025).:80-91. DOI: 10.7868/S3034559625030013
APA	Belchenko M., Grunina E., Korovina A., Kotov A., Petzer A., Petzer J., Proskurina I., Romanycheva A., Shetnev A., Vasil'eva E. (2025). Synthesis and Biological Evaluation of N-Aminoalkil Derivatives of Sulfanilamide Reaction. Russian Journal of General Chemistry. vol. 95, no. 3-4, pp.80-91 DOI: 10.7868/S3034559625030013

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