Synthesis and biological activity of piperazine derivatives of phenothiazine

Drug Res (Stuttg). 2015 Jan;65(1):5-8. doi: 10.1055/s-0033-1364001. Epub 2014 Jan 27.

Abstract

Some novel piperazine derivatives of phenothiazine were synthesized. The structures of the synthesized compounds were characterized by elemental analysis, FT-IR, (1)H- and (13)C-NMR and Mass Spectroscopy. The compounds were evaluated for antibacterial, antifungal and antitubercular activity by cup plate, disc diffusion and Lowenstein-Jensen medium methods respectively. All the compounds showed good antibacterial activity against Staphylococcus aureus and Bacillus subtilis. Compound V showed equipotent antibacterial activity with streptomycin standard and showed better antibacterial activity against gram positive bacteria profile than gram negative bacteria. Zone of inhibition was not found for the compounds against Escherichia coli and Pseudomonas aeruginosa. All the compounds exhibited good antifungal activity against Aspergillus species and no activity against Candida albicans. All the compounds at a concentration of 100, 10 and 1 µg/L showed inhibition against the growth of Mycobacterium tuberculosis.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology
  • Bacteria / drug effects
  • Dose-Response Relationship, Drug
  • Fungi / drug effects
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Phenothiazines / chemical synthesis
  • Phenothiazines / chemistry
  • Phenothiazines / pharmacology*
  • Piperazines / chemical synthesis
  • Piperazines / chemistry
  • Piperazines / pharmacology*
  • Spectrum Analysis

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Antitubercular Agents
  • Phenothiazines
  • Piperazines
  • phenothiazine