Abstract <p>The article discusses the synthesis of non-cyclic three-unit products (TUP) with substituted phenoxy groups and their metal complexes with gallium, copper, and zinc. The synthesis uses 3,5-diamino-1,2,4-triazole (guanazole) and phthalonitriles with 2-carboxyphenoxy or 4-cyclohexylphenoxy groups. The antibacterial activity of these compounds was assessed using biological activity spectrum prediction and the disk diffusion method. At the first stage, phenoxy-substituted three-unit products were synthesized based on the corresponding phenoxy-substituted phthalonitriles and guanazole. The synthesis of metal complexes of three-unit products with copper, zinc and gallium was carried out by heating a mixture consisting of phenoxy-substituted three-unit products obtained at the first stage and acetate of copper, zinc or gallium in 2-ethoxyethanol. Computer screening of the biological activity of triazole-containing phenoxy-substituted three-unit products and their metal complexes with copper, zinc and gallium was performed using the Way 2 Drug software. It has been found that these compounds can be active against Gram-positive coccoid bacteria, i.e. potentially used for the treatment of various purulent-inflammatory diseases. When assessing the toxicity of the synthesized compounds, it was found that carboxyphenoxy-substituted compounds are low- or practically non-dangerous, and compounds with cyclohexylphenoxy groups belong to the class of moderately dangerous substances when administered subcutaneously and intravenously and are low-risk when administered orally and intraperitoneally. The assessment of the antibacterial activity spectra prediction correctness was carried out on the basis of the M.B. Stoyunin Regional Tuberculosis Dispensary on three strains of bacteria, such as <i>Escherichia coli</i>, <i>Staphylococcus aureus</i>, <i>Staphylococcus Epidermidis</i>.</p>

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Synthesis of Biologically Active Triazole-Containing Three-Unit Products with Substituted Phenoxy Groups

  • S. A. Znoyko,
  • T. V. Kustova,
  • N. S. Fomin,
  • E. I. Demidova

摘要

Abstract

The article discusses the synthesis of non-cyclic three-unit products (TUP) with substituted phenoxy groups and their metal complexes with gallium, copper, and zinc. The synthesis uses 3,5-diamino-1,2,4-triazole (guanazole) and phthalonitriles with 2-carboxyphenoxy or 4-cyclohexylphenoxy groups. The antibacterial activity of these compounds was assessed using biological activity spectrum prediction and the disk diffusion method. At the first stage, phenoxy-substituted three-unit products were synthesized based on the corresponding phenoxy-substituted phthalonitriles and guanazole. The synthesis of metal complexes of three-unit products with copper, zinc and gallium was carried out by heating a mixture consisting of phenoxy-substituted three-unit products obtained at the first stage and acetate of copper, zinc or gallium in 2-ethoxyethanol. Computer screening of the biological activity of triazole-containing phenoxy-substituted three-unit products and their metal complexes with copper, zinc and gallium was performed using the Way 2 Drug software. It has been found that these compounds can be active against Gram-positive coccoid bacteria, i.e. potentially used for the treatment of various purulent-inflammatory diseases. When assessing the toxicity of the synthesized compounds, it was found that carboxyphenoxy-substituted compounds are low- or practically non-dangerous, and compounds with cyclohexylphenoxy groups belong to the class of moderately dangerous substances when administered subcutaneously and intravenously and are low-risk when administered orally and intraperitoneally. The assessment of the antibacterial activity spectra prediction correctness was carried out on the basis of the M.B. Stoyunin Regional Tuberculosis Dispensary on three strains of bacteria, such as Escherichia coli, Staphylococcus aureus, Staphylococcus Epidermidis.