Comprehensive, Characterization and Molecular Docking of Novel 1,4-Diaryl /Alkyl Substituted Diazine Analogues for Antimicrobial Application | ||
| Egyptian Journal of Chemistry | ||
| Volume 69, Issue 1, January 2026, Pages 25-48 PDF (3.97 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2025.377743.11637 | ||
| Authors | ||
| Marwa M. Rezk* 1; A. A. F. Wasfy2; Mohamed S. Behalo3; Samar El-Kalyoubi4; Aly A. Aly2 | ||
| 1Chemistry Department, Faculty of Science, Benha University , Benha , Egypt | ||
| 2Chemistry Department, Faculty of Science, Benha University, Benha, Egypt | ||
| 3chemistry department, faculty of science, benha university | ||
| 4pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, 42511, Egypt | ||
| Abstract | ||
| A new class of phthalazinone derivatives were synthesized by the reaction of 1-(4-(4-oxo-3,4-dihydrophthalazin-1-yl) phenyl)-pyrrolidine-2,5-dione (2), and acetohydrazide (5), with several chemical reagents. According to their elemental analysis and spectrum data, all synthesized derivatives structures were characterized. Certain prepared compounds were screened versus some bacteria and fungi strains to assess their antimicrobial efficacy. The newly derivativesdemonstrated antimicrobial activity toward the selected microbes compared with the used references. Notably , compound 7 revealed activities versus Escherichia coli (inhibition zone 23±1 mm, and Staphylococcus aureus (inhibition zone 20.3±0.6mm) as compared to Gentamicin (inhibition zone 27±0.1 mm) & Ampicillin (inhibition zone 21.3±0.6 mm), and exhibiting potent inhibitory activity toward Candida albicans and Asperagillus nigar fungi (inhibition zone : 30.3±0.6 mm, 15±1.0 mm) respectively, compared to Nystatin (inhibition zone : 21.6±0.6 mm, 19.3±0.6 mm ). Morever, compounds 5 and 9 displayed anti-bacterial and anti-fungal activities against some tested strains. Also compouds 6, 14 and 18 exhibited commendable efficacy towards examined bacteria strains. A molecular docking study was conducted for the most potent compounds 5, 6, 7, 9, 14, and 18, the results demonstrating significant binding affinities with essential microbial enzymes, consistent with their observed inhibitory effects. | ||
| Keywords | ||
| Phthalazinone; acetohydrazide; A ntimicrobial activity; Molecular docking | ||
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