Synthesis and Evaluation of 5-imino-4-thioxoimidazolidin-2-one Derivatives as Antibacterial and Antifungal Agents

Author:

Abbas Samir Y.1,El-Sharief Marwa A.M. Sh.2,Al-Harbi Reem A.K.3,El-Gammal Eman W.4,El-Sharief Ahmed M.S.5

Affiliation:

1. Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt

2. Applied Organic Chemistry Department, National Research Centre, Cairo, Egypt

3. Department of Chemistry, Faculty of Science, Taibah University, Almadinah Almunawarrah, Saudi Arabia

4. Department of Chemistry of Natural and Microbial Products, National Research Centre, Cairo, Egypt

5. Chemistry Department, Faculty of Science, Al-Azhar University (Boys), Cairo, Egypt

Abstract

Objective: It was interesting to synthesize some new 5-imino-4-thioxoimidazolidin-2- one derivatives with different halogenated and alkylated aromatic substituents at N-(1) and N-(3) and evaluation of their expected antibacterial and antifungal activities. Methods: New 5-imino-4-thioxoimidazolidin-2-one derivatives were synthesized through the reaction of different halogenated and alkylated N-arylcyanothioformamides with halogenated and alkylated aryl isocyanates. Results: 5-Imino-4-thioxoimidazolidin-2-ones were obtained in high yields with excellent purity. The activities of imidazolidines as antibacterial and antifungal agents were studied. Some of imidazolidine derivatives displayed significant antibacterial and antifungal activities. Conclusion: 5-Imino-4-thioxoimidazolidin-2-ones were obtained in 77-90% yields with excellent purity. The antibacterial and antifungal activities suggest that some of the imidazole derivatives possess significant antimicrobial activity against B. subtilis, K. pneumonia and C. albicans and moderate activity against S. aureus.

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery

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