Modern Chemistry & Applications

Design, synthesis and evaluation of novel phthalimide derivatives as in vitro anti-microbial, antioxidant and anti-inflammatory agents

International Conference on Applied Chemistry

October 17-18, 2016 Houston, USA

Phoebe Farag Allah Lamie, John N Phillopes, Ahmed O El-Gendy, Lucie Rarova and Jiri Gruz

Beni-Suef University, Egypt

Scientific Tracks Abstracts: Mod Chem appl

Abstract:

Sixteen new phthalimide derivatives were synthesized and evaluated for their in vitro anti-microbial, anti-oxidant and antiinflammatory 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-(N'-{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).

Biography :

Phoebe Farag Allah Lamie has completed her PhD from Beni-Suef University, Egypt and Post-doctoral studies from the same university. She has published about 9 papers in different international journals.

Email: feby.farag@yahoo.com