Synthesis, characterization and in vitro biological studies of novel cyano derivatives of N-alkyl and N-aryl piperazine

Cyano derivatives of N-alkyl and N-aryl piperazine have been synthesized and screened for antibacterial and antifungal activities. All the synthesized compounds showed the antibacterial activity against pathogenic strains of Staphylococcus aureus (MTCCB 737), Pseudomonas aeruginosa (MTCCB 741), Streptomyces epidermidis (MTCCB 1824) and Escherichia coli (MTCCB 1652) and antifungal activity against pathogenic strains of Aspergillus fumigatus (ITCC 4517), Aspergillus flavus (ITCC 5192) and Aspergillus niger (ITCC 5405). All compounds showed mild to moderate antimicrobial activity. However, compounds 3c, 4a and 6 showed potent antibacterial activity against pathogenic strains used in the study. Compounds 3a, 3b, 4b, and 4d showed mild to moderate antifungal activity against Aspergillus pathogenic strains. The compounds reported in this study were assessed for there cytotoxicity using MTT colorimetric assay on Hela cells. All the compounds showed cell viability more than the control drug gentamicin, with compound 2 having highest i.e. 95% cell viability.

A series of cyano derivatives of N-alkyl and N-aryl piperazine were synthesized and evaluated for antibacterial and antifungal activity. Compound 3-(4-methyl-piperazin-1-yl)-propanitrile 4a showed potent antibacterial activity by broth dilution method with MIC at 19.5 μg/ml and 39.0 μg/ml against P. aeruginosa and E. coli, respectively, comparable to gentamicin as control drug. Compounds (4-benzyl-piperazin-1-yl)-acetonitrile 3c and 3-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-acetonitrile 6 showed a significant antibacterial activity with MIC at 19.5 μg/ml against S. aureus. In vitro cytotoxic studies of compound 3b exhibit 95% cell viability at the concentration used for antibacterial studies on Hela cells by using MTT colorimetric method.Figure optionsDownload as PowerPoint slide