Synthesis and Evaluation of Curcuminoid Analogues as Antioxidant and Antibacterial Agents

Molecules. 2017 Jun 11;22(6):971. doi: 10.3390/molecules22060971.

Abstract

Diazocoupling reaction of curcumin with different diazonium salts of p-toluidine, 2-aminopyridine, and 4-aminoantipyrine in pyridine yielded the arylhydrazones 2a-c. Arylhydrazone of p-toluidine reacted with urea, thiourea, and guanidine nitrate to produce 5,6-dihydropyrimidines. Further reaction of 2a with 2,3-diaminopyrdine in sodium ethoxide solution yielded 1H-pyrido[2,3-b][1,4]diazepine derivative. Bis(2,5-dihydroisoxazole) is obtained from the reaction of 2a with hydroxylamine hydrochloride, while its reactions with hydrazines afforded the respective 4,5-dihydro-1H-pyrazoles. The target compounds were evaluated as antioxidant and antibacterial agents. The tested compounds showed good to moderate activities compared to ascorbic acid and chloramphenicol, respectively.

Keywords: antibacterial activity; antioxidant activity; curcumin; isoxazole; pyrazole; pyrimidine.

MeSH terms

  • Aminopyridines / chemical synthesis
  • Aminopyridines / chemistry
  • Ampyrone / chemical synthesis
  • Ampyrone / chemistry
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antioxidants / chemical synthesis
  • Antioxidants / chemistry
  • Antioxidants / pharmacology*
  • Ascorbic Acid / pharmacology
  • Chloramphenicol / pharmacology
  • Curcumin / analogs & derivatives
  • Curcumin / chemical synthesis
  • Curcumin / chemistry
  • Curcumin / pharmacology*
  • Diazonium Compounds / chemical synthesis
  • Diazonium Compounds / chemistry
  • Gram-Negative Bacteria / drug effects*
  • Gram-Negative Bacteria / pathogenicity
  • Gram-Positive Bacteria / drug effects*
  • Gram-Positive Bacteria / pathogenicity
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Structure-Activity Relationship
  • Toluidines / chemical synthesis
  • Toluidines / chemistry

Substances

  • Aminopyridines
  • Anti-Bacterial Agents
  • Antioxidants
  • Diazonium Compounds
  • Toluidines
  • Ampyrone
  • Chloramphenicol
  • 4-toluidine
  • Curcumin
  • Ascorbic Acid
  • alpha-aminopyridine