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

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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.

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作者简介

Elena Vasilyeva

Ushinsky Yaroslavl State Pedagogical University; Kosygin Russian State University

Email: a.shetnev@yspu.org
ORCID iD: 0000-0001-6855-0883
俄罗斯联邦, Yaroslavl; Moscow

Irina Proskurina

Ushinsky Yaroslavl State Pedagogical University

Email: a.shetnev@yspu.org
ORCID iD: 0000-0001-6086-1978
俄罗斯联邦, Yaroslavl

Anton Shetnev

Ushinsky Yaroslavl State Pedagogical University; Moscow Institute of Physics and Technology

编辑信件的主要联系方式.
Email: a.shetnev@yspu.org
ORCID iD: 0000-0002-4389-461X
俄罗斯联邦, Yaroslavl; Dolgoprudny

Anna Romanycheva

Ushinsky Yaroslavl State Pedagogical University

Email: a.shetnev@yspu.org
ORCID iD: 0000-0002-7931-1711
俄罗斯联邦, Yaroslavl

Alyona Korovina

Ushinsky Yaroslavl State Pedagogical University

Email: a.shetnev@yspu.org
ORCID iD: 0009-0003-5743-6948
俄罗斯联邦, Yaroslavl

Maria Belchenko

Ushinsky Yaroslavl State Pedagogical University

Email: a.shetnev@yspu.org
ORCID iD: 0009-0006-9589-0756
俄罗斯联邦, Yaroslavl

Ekaterina Grunina

Ushinsky Yaroslavl State Pedagogical University

Email: a.shetnev@yspu.org
ORCID iD: 0009-0007-4551-1866
俄罗斯联邦, Yaroslavl

Anelle Petzer

North-West University

Email: a.shetnev@yspu.org
ORCID iD: 0000-0001-8114-8223
南非, Potchefstroom

Alexander Kotov

Ushinsky Yaroslavl State Pedagogical University

Email: a.shetnev@yspu.org
ORCID iD: 0000-0002-0567-2880
俄罗斯联邦, Yaroslavl

Jacob Petzer

North-West University

Email: a.shetnev@yspu.org
ORCID iD: 0000-0002-7114-8120
南非, Potchefstroom

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