Probing the antiamoebic and cytotoxicity potency of novel tetrazole and triazine derivatives

A series of compounds bearing a Tetrazole and Triazine ring motif conjugated with a SO2NH function were synthesized and investigated for their antiamoebic potency. Cytotoxicity of the compounds was checked on human hepatocellular carcinoma cell line HepG2. Incorporation of Triazine ring in place of tetrazole resulted in a precipitous increase in the antiamoebic activity of the compounds. Antiamoebic activity of the investigated compounds was found to be position and substituent dependent. In vitro cytotoxicity results revealed noncytotoxic nature of all the tested compounds up to a concentration of 25 μM. Compound 5c and 5d were obtained as least cytotoxic (IC50 > 100 μM) and excellent Entamoeba histolytica inhibitors with IC50 values of 1.05 μM and 1.02 μM respectively.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Synthesis of tetrazole and triazine ring containing sulfonamide derivatives. ► Characterization of compounds with various Spectroscopic techniques. ► Evaluated for compounds for antiamoebic activity using HM1:IMSS strain. ► Effective compounds were screened for cell viability using H9C2 cell line. ► Compound 5c and 5d were found as leading targets for Entamoeba histolytica.