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Article

Design, Synthesis, Molecular Docking, and Evaluation Antioxidant and Antimicrobial Activities for Novel 3-Phenylimidazolidin-4-One and 2-Aminothiazol-4-One Derivatives

1
Department of Chemistry, Faculty of Science, Zagazig University, Zagazig 44519, Egypt
2
Department of Chemistry, College of Science, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Sobhi M. Gomha and Maher Fathalla
Molecules 2022, 27(3), 767; https://doi.org/10.3390/molecules27030767
Received: 20 December 2021 / Revised: 19 January 2022 / Accepted: 19 January 2022 / Published: 25 January 2022
On our way to discovering and developing compounds that have an antioxidant impact compared to ascorbic acid and other biological activities, we designed, synthesized, and evaluated a new series of heterocyclic moieties drugs (111) as antioxidants and antimicrobial agents. As starting moieties, these new candidates were derived from two promising heterocyclic compounds, imidazoldin-4-one and thiazol-4-one. Firstly, diphenylimidazol 1 was obtained because of the cyclo condensation one-pot ternary reaction of urea, aniline, and chloroacetic acid under thermal conditions. Out of this starting compound, we could design and create new vital rings such as purine and triazine as in compounds 5 and 6, respectively. Secondly, the start thiazole derivative 7 was obtained from the intermolecular cyclization of thiourea, chloroacetic acid, p-nitobezaldehyde in the presence of sodium acetate. We synthesized various derivatives from this second starting compound 7 by being subjected to different reagents such as aniline, phenylenediamine, phenylhydrazine, and barbituric acid to yield 8, 9, 10, and 11, respectively. Using ascorbic acid as the standard compound, the pharmacological testing for antioxidant activity assessment of the produced derivatives was evaluated against ABTS (2,20-azinobis (3-ethylbenzothiazoline-6-sulfonic acid). Candidate 6 exhibited the best activity as an antioxidant agent compared to ascorbic acid as a reference compound. Moreover, all compounds were evaluated as antimicrobial agents against a series of bacteria and fungi. Among all synthesized compounds, compound 6 achieved high efficiency against two types of fungi and four kinds of bacteria, as Clotrimazole and Ampicillin were used as the reference agents, respectively. All chemical structures of the novel synthesized candidates were unequivocally elucidated and confirmed utilizing spectroscopical and elemental investigations. View Full-Text
Keywords: imidazolothiazole; imidazotriazine; azabene; antioxidant activity; ABTS assay; antimicrobial agents; molecular docking imidazolothiazole; imidazotriazine; azabene; antioxidant activity; ABTS assay; antimicrobial agents; molecular docking
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MDPI and ACS Style

Shehab, W.S.; Aziz, M.A.; Elhoseni, N.K.R.; Assy, M.G.; Abdellattif, M.H.; Hamed, E.O. Design, Synthesis, Molecular Docking, and Evaluation Antioxidant and Antimicrobial Activities for Novel 3-Phenylimidazolidin-4-One and 2-Aminothiazol-4-One Derivatives. Molecules 2022, 27, 767. https://doi.org/10.3390/molecules27030767

AMA Style

Shehab WS, Aziz MA, Elhoseni NKR, Assy MG, Abdellattif MH, Hamed EO. Design, Synthesis, Molecular Docking, and Evaluation Antioxidant and Antimicrobial Activities for Novel 3-Phenylimidazolidin-4-One and 2-Aminothiazol-4-One Derivatives. Molecules. 2022; 27(3):767. https://doi.org/10.3390/molecules27030767

Chicago/Turabian Style

Shehab, Wesam S., Maged A. Aziz, Nourhan K.R. Elhoseni, Mohamed G. Assy, Magda H. Abdellattif, and Eman O. Hamed. 2022. "Design, Synthesis, Molecular Docking, and Evaluation Antioxidant and Antimicrobial Activities for Novel 3-Phenylimidazolidin-4-One and 2-Aminothiazol-4-One Derivatives" Molecules 27, no. 3: 767. https://doi.org/10.3390/molecules27030767

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