Synthesis and Evaluation of Thiazole - Pyrimidine Derivatives as New Anticandidal and Cytotoxic Agents

Abstract

The aim of this study was to describe the synthesis of four new 2-(3,4-diphenyl-3H-thiazol-2-ylidene)amino-4,6-dimethylpyrimidine derivatives, which were screened for their anticandidal activity and cytotoxicity. The title compounds (2a - 2d) were synthesized via the reaction of 1-phenyl-3-(4,6-dimethylpyrimidin-2-yl)thiourea with phenacyl bromides. Anticandidal activity of the synthesized compounds was evaluated using microbroth dilution method. All compounds were also investigated for their cytotoxic effects on A549 and NIH3T3 cell lines. Compound 2c can be considered as the most promising anticandidal agent due to its inhibitory effects on Candida albicans, C. glabrata, C. tropicalis with a MIC value of 125 mu g/mL and low toxicity to NIH3T3 cells (IC50 =193.32 mu g/mL). Although compound 2a was the most effective derivative against A549 cells with an IC50 value of 0.0623 mM, it is not a good candidate for cancer treatment because of its high toxicity against NIH3T3 cells (IC50 =0.00316 mM).