An Efficient One-Pot Protocol for the Synthesis of Substituted 3,4-Dihydropyrimidin-2(1H)-ones Using Metallophthalocyanines (MPcs) as Potent Heterogeneous Catalysts: Synthesis, Characterization, Aggregation and Antimicrobial Activity

Molecules. 2017 Apr 9;22(4):605. doi: 10.3390/molecules22040605.

Abstract

In this study, novel phthalonitrile 3 and their corresponding metal-free 4 and metallophthalocyanine derivatives 5-7 bearing 2-isopropenyl-4-methoxy-1-methylbenzene groups were synthesized and characterized. 3,4-Dihydropyrimidinones have been synthesized by a modified Biginelli-type reaction with various metallophthalocyanines 5-7 as catalysts. Compared to the classical Biginielli reaction, the new method has the advantages of good yield and short reaction time. Among the various metallophthalocyanines studied, cobalt (II)-phthalocyanine was found to be most active for this transformation. The newly prepared compounds were characterized using elemental analyses, MS, IR, ¹H/13C-NMR and UV-Vis spectroscopy. In addition; the 3,4-dihydropyrimidinones (DHPMs) 8-12 were investigated for antimicrobial activities and revealed good activity. The minimum inhibitory concentration (MIC) was determined by the microdilution technique in Mueller-Hinton broth. The MICs were recorded after 24 hours of incubation at 37 °C. These results are promising, showing these compounds are biologically active.

Keywords: Biginelli reaction; aggregation; antimicrobial activity; dihydropyrimidinones; metallophthalocyanine derivatives.

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology*
  • Bacteria / drug effects
  • Catalysis
  • Chemistry Techniques, Synthetic*
  • Indoles / chemistry*
  • Isoindoles
  • Metals / chemistry*
  • Microbial Sensitivity Tests
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology*
  • Solvents
  • Spectrum Analysis

Substances

  • Anti-Infective Agents
  • Indoles
  • Isoindoles
  • Metals
  • Pyrimidines
  • Solvents
  • phthalocyanine