Studies on synthesis and biological activities of trifluoroacetophenone oxime ester derivatives

Aim: Infection diseases are a serious health problem worldwide and one of the main causes of human morbidity and mortality. Existing drugs have been extensively studied to develop effective antifungal and antibacterial compounds because of their narrow spectrum of activity, toxicity, poor pharmacokinetic properties and resistance to drugs. In this thesis, it was aimed to investigate the antifungal, antibacterial and cytotoxic effects of 1-(4-trifluoromethylphenyl)-2-(1H-imidazol-1-yl)ethanone oxime esters, a series of new compounds designed based on the structure of azole group antifungal drugs. Material ve Method: In this study, 21 new compounds were synthesized and the structures of the compounds were confirmed by spectral analysis. The antifungal and antibacterial activities of the synthesized compounds were examined against three Candida species and four bacterial strains. In vitro cytotoxicity activities of the compounds were investigated against L929 and SH-SY5Y cell lines. Results: As a result of the studies performed, the compounds were found to be more effective against bacterial strains, while they were moderately effective against Candida species. Some compounds were found to have a MIC value of 4 μg/ml against S.aureus. The % cell viability and IC50 values against the cell lines of the compounds were calculated. While compounds L929 did not show significant cytotoxic effects on the cell line, they was found to be effective against SH-SYSH cell line. Conclusion: 21 compounds were synthesized and their activities were investigated. According to the results obtained, compounds which have high antifungal activity and can be more effective in the SH-SY5Y cell line will be designed. Key Words: Antibacterial, antifungal, cytotoxicity, imidazole, oxime