Document Type : Original Article
Authors
1
Chemistry Department, Faculty of Science, Benha University , Benha , Egypt
2
Chemistry Department, Faculty of Science, Benha University, Benha, Egypt
3
chemistry department, faculty of science, benha university
4
pharmaceutical 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.
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