<p>Substituted amino-1<i>H</i>-pyrazoles have been synthesized and characterized in terms of their antimicrobial ac- tivity. A three-component synthesis was carried out using a simple environmentally friendly one-step method starting from aromatic aldehydes, hydrazines or benzhydrazides, malononitrile or cyanoacetic acid amide and water or a mixture of water–<i>i</i>-PrOH as the solvent. The antimicrobial properties of the synthesized com- pounds, including previously unknown ones, were determined against Gram-negative and Gram-positive bac- teria. 5-Amino-1-(2,4-dinitrophenyl)-3-aryl-1<i>H</i>-pyrazole-4-carboxylates with 3-nitrophenyl or 3-hydroxy- phenyl substituents showed pronounced antimicrobial activity against <i>Pseudomonas aeruginosa</i>. The results indicated that further searching for antimicrobial compounds in the series of aryl-substituted amino-1<i>H</i>-pyrazolecarbonitriles and amino-1<i>H</i>-pyrazolecarboxamides was promising.</p>

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Synthesis and Antimicrobial Activity of Substituted Amino-1H-Pyrazoles

  • A. A. Meshcheryakova,
  • E. A. Konstantinova,
  • S. V. Borisova,
  • G. L. Burygin,
  • V. V. Sorokin

摘要

Substituted amino-1H-pyrazoles have been synthesized and characterized in terms of their antimicrobial ac- tivity. A three-component synthesis was carried out using a simple environmentally friendly one-step method starting from aromatic aldehydes, hydrazines or benzhydrazides, malononitrile or cyanoacetic acid amide and water or a mixture of water–i-PrOH as the solvent. The antimicrobial properties of the synthesized com- pounds, including previously unknown ones, were determined against Gram-negative and Gram-positive bac- teria. 5-Amino-1-(2,4-dinitrophenyl)-3-aryl-1H-pyrazole-4-carboxylates with 3-nitrophenyl or 3-hydroxy- phenyl substituents showed pronounced antimicrobial activity against Pseudomonas aeruginosa. The results indicated that further searching for antimicrobial compounds in the series of aryl-substituted amino-1H-pyrazolecarbonitriles and amino-1H-pyrazolecarboxamides was promising.