Synthesis, In Vitro Antimicrobial and Cytotoxic Activities of Some New Pyrazolo[1,5- a]pyrimidine Derivatives

Molecules. 2019 Mar 19;24(6):1080. doi: 10.3390/molecules24061080.

Abstract

A new series of pyrazole 47 and pyrazolo[1,5-a]pyrimidine 813 were synthesized by using a simple, efficient procedure, and screened for their in-vitro antimicrobial and antitumor activities. Symmetrical and asymmetrical 3,6-diarylazo-2,5,7-triaminopyrazolo[1,5-a]pyrimidine were synthesized by the conventional method and also subjected to microwave irradiation and under ultrasound conditions. The biological results revealed that most of the tested compounds proved to be active as antibacterial and antifungal agents. The antitumor activity of the synthesized compounds was evaluated against human cancer cell lines, MCF-7, HCT-116, and HepG-2, as compared with Doxorubicin as a control.

Keywords: 3,5-diaminopyrazole; antimicrobial; antitumor activities; microwave; pyrazole; pyrazolo[1,5-a]pyrimidine.

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Doxorubicin / chemistry
  • Doxorubicin / pharmacology
  • HCT116 Cells
  • Hep G2 Cells
  • Humans
  • MCF-7 Cells
  • Microbial Sensitivity Tests
  • Microwaves*
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antineoplastic Agents
  • Pyrazoles
  • Pyrimidines
  • pyrazole
  • Doxorubicin
  • pyrimidine