Design, Synthesis, in Vitro and Molecular Dynamic Study of Antifungal Activity of the Alcoholic Extract of Sygysium aromaticum in Comparison to Some New Sulphonamide Derivatives

• Published in: Azerbaijan Pharmaceutical and Pharmacotherapy Journal Vol. 22; no. 1; pp. 45 - 52
• Main Authors: Humadi, Suhad Sami, Awad, Samir Mohamed, El-Shehery, Mohamed Fathy, El-Rashedy, Ahmed Abd Elkader, Mansour, Yara Essam, Hassan, Saif M
• Format: Journal Article
• Language: English
• Published: Baku Azerbaijan Medical University 01.01.2023
• Subjects: Antifungal agents; Flowers & plants; Fungi; Fungicides; Pesticides; R&D; Research & development; Simulation; Egypt; Indonesia
• ISSN: 1994-1951
• DOI: 10.61336/appj/22-l-11

Five synthetic 2-Thiouracil-5-sulphonamides were evaluated as antifungal agents against the same fungal isolates. Their synergistic effect with clove extract was assessed in an attempt to formulate a potential combination therapy for the future. The goal was to evaluate whether thiouracil derivatives and clove extract can enhance antifungal activity against drug-resistant strains of locally isolated fungi. Both natural and synthetic samples were tested against fungal isolates including Geotrichum candidum, Altemaria altemata, Fusarium oxysporum, and Mucorhiemalis, which are responsible for infections in potato and tomato plants. Clove extract demonstrated varying potent wide-spectram activity against all fungal isolates, while the effectiveness of thiouracil derivatives depended on their chemical structures. Compounds 3b and 3e exhibited the most potent antifungal activity and showed a broad spectrum of effectiveness. Compound 3d displayed moderate antifungal activity compared to clove extract, while compound 3a exhibited weaker activity and was inactive against F. oxysporum and G. candidum. Compound 3c displayed the weakest antifungal activity and was inactive against A. altemata, F. oxysporum, and G. candidum. Both clove extract and 3e demonstrated synergistic antifungal activity. Moreover, the combination of clove extract and 2-thiouracil-5-sulphonamides displayed variable antifungal activity, suggesting the potential for synergistic effects in their activity.