Pharmacological studies on 1,4-disubstituted-l,2,3-triazoles

Abstract

The present study aimed at screening a set of newly synthesized l,4-disubstituted 1,2,3 triazoles for their possible biological activities including antimicrobial, antitumor, antioxidant and cytotoxic activities. These newly synthesized 1,2,3 triazoles included 15 compounds with position 1 of the central triazole ring containing phenyl and 1-hydroxycyclohexyl groups and position 4 containing alkyl, phenyl, and substituted aryl groups. All of these compounds were subjected to antibacterial assay using agar well diffusion method for determining zones of inhibition and minimum inhibitory concentrations (MIC). The assay was done against five bacterial strains including three gram negative (Brodetella bronchiseptica, Escherichia coli and Enterobacter aero genes) and two gram positive strains (Staphylococcus aureus and Micrococcus luteus). Only compound CCl7 showed some antibacterial activity with MIC values ranging from 0.2 to 0.8 against different strains, however, it did not give any activity against E.coli bacteria. The antifungal activity of these compounds was tested by agar tube dilution method. Compound CC17 gave highly significant results and showed 100% inhibition against A. flavus, 80% inhibition against F. solani and more than 60% inhibition against A. niger and A. fumigatus. Cytotoxic analysis of compounds was done using Brine shrimp lethality assay some of the compounds proved highly toxic against shrimp larvae e.g. CC6, CC8, CC16 and CC17. Antitumor potato disc assay was carried out to examine antitumor activity of the compounds at four different concentrations of all 15 compounds. Highest tumor inhibition was exhibited by compound CC16. Antioxidant and prooxidant nature of the compounds was studied by free radical induced DNA damage analysis. Some compounds like CC1 and CC8 gave DNA protective activity at 3000 ppm concentration. Others were protective against free radical damage at lower concentrations, however, the extent of protective activity against radical damage was not very pronounced. Data obtained from these tests indicate potential of these compounds as biological agents and also enabled us to compare their antimicrobial, antifungal and antitumor properties.