Synthesis of some newer carbazole derivatives and evaluation for their pharmacological activity

Carbazole on reaction with chloroacetyl chloride afforded N⁹-(chloroacetyl)-carbazole (1) which on treatment with hydrazine hydrate has yielded N⁹-(hydrazinoacetyl)-carbazole (2), Condensation of (2) with various aromatic aldehydes afforded N9-(arylidene hydrazinoacetyl)-carbazoles (3a-3k), which on cycloaddition with isatin in the presense of ammonium acetate yielded 1-Carbazole-9-yl-2-(substitutedphenyl)-1,4-dihydroimidazo[4,5-b]indole 1- ylamino)-ethanone (4a-4k). All the synthesized compounds were evaluated for their antibacterial, antifungal, and anticancer activity. The structures of the newly synthesized compounds were confirmed by FTIR, ¹H NMR, MASS spectral data and elemental analysis. Compounds were screened for in-vitro antibacterial activity against the representative panel of two gram positive bacterial strains like Staphylococcus aureus and Bacillus subtilis and two gram negative bacterial strain like Pseudomonas aeruginosa and Escherichia coli and antifungal activity by inhibitory action against two fungal strains like Candida albicans and Aspergillus niger. The synthesized compounds were also evaluated for their anticancer activity by SRB assay method on A549 cell lines. All the newly synthesized substituted carbazoles have shown moderate to good antibacterial, antifungal and anticancer activity.

Author(s): Kapil Kaushik, Nitin Kumar and Devender Pathak

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