Phoebe Farag Allah Lamie
Beni-Suef University, Egypt
Title: Design, synthesis and evaluation of novel phthalimide derivatives as in vitro anti-microbial, antioxidant and anti-inflammatory agents
Biography
Biography: Phoebe Farag Allah Lamie
Abstract
Sixteen new phthalimide derivatives were synthesized and evaluated for their
in vitro anti-microbial, anti-oxidant and anti-inflammatory activities. The cytotoxicity for all synthesized compounds was also determined in cancer cell lines and in normal human cells. None of the target derivatives had any cytotoxic activity. (ZE)-2-[4-(1-Hydrazono-ethyl) phenyl] isoindoline-1, 3- dione showed remarkable anti-microbial activity. Its activity against Bacillus subtilis was 133%, 106% and 88.8% when compared with the standard antibiotics ampicillin, cefotaxime and gentamicin, respectively. (ZE)-2-[4-(1-Hydrazonoethyl)phenyl]isoindoline-1,3-dione also showed its highest activities in Gram negative bacteria against Pseudomonas aeruginosa where the percentage activities were 75% and 57.6% when compared sequentially with the standard antibiotics cefotaxime and gentamicin. It was also found that the compounds 2-[4-(4-ethyl-3-methyl-5-thioxo-1,2,4-triazolidin-3-yl)phenyl]isoindoline-1,3-dione and 2-[4-(3-methyl-5-thioxo-4-phenyl-1,2,4-triazolidin-3-yl)phenyl]isoindoline-1,3-dione had anti-oxidant activity. 4-(N'-{1-[4-(1, 3-Dioxo-1, 3-dihydro-isoindol-2-yl)-phenyl]-ethylidene}-hydrazino)-benzenesulfonamide showed the highest in vitro anti-inflammatory activity of the tested compounds (a decrease of 32%). To determine the mechanism of the anti-inflammatory activity of 4-(Nʹ-{1-[4-(1, 3-dioxo-1, 3-dihydro-isoindol-2-yl)-phenyl]-ethylidene}-hydrazino)-benzenesulfonamide, a docking study was carried out on the COX-2 enzyme. The results confirmed that the latter had a higher binding energy score (-17.89 kcal/mol) than that of the ligand celecoxib (−17.27 kcal/mol).