Synthesis and Evaluation of Antibacterial and Antifungal Activities of 1,3-Disubstituted-4-thioxoimidazolidin-2-one Derivatives

Abstract

1,3-Disubstituted-4-thioxoimidazolidin-2-one derivatives with various substituents at N1 and N3 were synthesized with high yields and excellent purity by the reaction of various N-arylcyanothioformamide derivatives with isocyanate derivatives. The activity of these products as antibacterial and antifungal agents was studied to through some light on structural activity relationship. Some of synthesized compounds showed significant antibacterial and antifungal activities. Most of the imidazole derivatives possess significant antifungal activity aginst S. cerevisiae (MIC 1–10 μg mL–1). As comparision with ketoconazole, most of the imidazole derivatives showed activity ranging from 50 % less activity to fourfold activity.