Synthesis, antiproliferative and antimicrobial activity of new Mannich bases bearing 1,2,4-triazole moiety

J Enzyme Inhib Med Chem. 2014 Dec;29(6):786-95. doi: 10.3109/14756366.2013.855926. Epub 2014 Feb 10.

Abstract

Abstract This study presents the synthesis, antiproliferative and antimicrobial evaluation of a new series of Mannich base derivatives containing 1,2,4-triazole system. New compounds were prepared by the reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with formaldehyde and various amines. The structures of the prepared compounds were confirmed by means of (1)H NMR, (13)C NMR and elemental analyses. Twelve compounds were evaluated for their in vitro antiproliferative activities against six chosen cancer cell lines. All synthesized compounds were screened for their in vitro antimicrobial activity by using the agar dilution technique. For 17 potentially active compounds, their antibacterial activity was confirmed on the basis of MIC (minimal inhibitory concentration) by broth microdilution method using the reference Gram-positive and Gram-negative bacterial strains.

Keywords: 1,2,4-Triazole derivatives; Mannich base derivatives; antimicrobial activity; antiproliferative activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Drug Design
  • Formaldehyde / chemistry
  • Gram-Negative Bacteria / drug effects
  • Gram-Negative Bacteria / growth & development
  • Gram-Positive Bacteria / drug effects
  • Gram-Positive Bacteria / growth & development
  • Humans
  • Mannich Bases / chemical synthesis*
  • Mannich Bases / pharmacology
  • Mice
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship
  • Triazoles / chemistry*

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Mannich Bases
  • Triazoles
  • Formaldehyde
  • 1,2,4-triazole