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Medicinal Chemistry

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ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Research Article

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

Author(s): Samir Y. Abbas*, Marwa A.M. Sh. El-Sharief, Reem A.K. Al-Harbi, Eman W. El-Gammal and Ahmed M.S. El-Sharief

Volume 17, Issue 6, 2021

Published on: 27 December, 2019

Page: [638 - 645] Pages: 8

DOI: 10.2174/1573406416666191227112648

Price: $65

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 the 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.

Keywords: N-Arylcyanothioformamides, 5-imino-4-thioxoimidazolidin-2-ones, imidazolidineiminothiones, antibacterial activity, antifungal activity, antimicrobial activity.

Graphical Abstract
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