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Original scientific paper

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

Marwa A. M. Sh. El-Sharief ; Applied Organic Chemistry Department, National Research Centre, Cairo, Egypt
Samir Y. Abbas ; Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt
Ziad Moussa ; Department of Chemistry, Faculty of Science, Taibah University, Almadinah Almunawarrah, Saudi Arabia
Eman W. El-Gammal ; Department of Chemistry of Natural and Microbial Products, National Research Centre, Cairo, Egypt
Ahmed M. Sh. El-Sharief ; Chemistry Department, Faculty of Science, Al-Azhar University (Boys), Cairo, Egypt

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page 335-340

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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.

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N-arylcyanothioformamides, imidazolidineiminothiones, isocyanates, antimicrobial activity

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