99702-70-2Relevant articles and documents
Synthesis, anti-inflammatory, analgesic and COX-1/2 inhibition activities of anilides based on 5,5-diphenylimidazolidine-2,4-dione scaffold: Molecular docking studies
Abdel-Aziz, Alaa A.-M.,El-Azab, Adel S.,Abou-Zeid, Laila A.,Eltahir, Kamal Eldin H.,Abdel-Aziz, Naglaa I.,Ayyad, Rezk R.,Al-Obaid, Abdulrahman M.
, p. 121 - 131 (2016/04/05)
The design, synthesis and pharmacological activities of a group of 5,5-diphenylimidazolidine-2,4-dione bearing anilide, phenacyl and benzylidene fragments 2-27 were reported. The prepared 5,5-diphenylimidazolidine-2,4-dione derivatives were evaluated in vivo for anti-inflammatory, analgesic activities and in vitro for COX-1/2 inhibition assay. Among the tested compounds, derivatives 5, 9, 10, 13, and 14 showed significant and potent anti-inflammatory and analgesic activities almost equivalent to reference drug celecoxib. In COX-1/2 inhibition assay, compounds 5, 9, 10 and 14 showed high COX-2 inhibitory activity (IC50 = 0.70 μM, 0.44 μM, 0.61 μM and 0.41 μM; respectively) and selectivity index (SI) range of 142-243 comparable to celecoxib [COX-2 (SI) > 333]. These potent COX-2 inhibitors 9, 10, 13, and 14 were docked into the active site pocket of COX-2 to explore the binding mode and possible interactions of these ligands.
Antimicrobial activity of new synthesized [(oxadiazolyl)methyl]phenytoin derivatives
Ali, Omar M.,El-Sayed, Wael A.,Eid, Shorok A.,Abdelwahed, Nayera A. M.,Abdel-Rahman, Adel A.-H.
experimental part, p. 657 - 667 (2012/09/05)
A number of substituted phenytoin derivatives in addition to their sugar hydrazones were newly synthesized. Furthermore, the corresponding derived 1,3,4-oxadiazole and their thioglycoside as well as their acyclic analogs were prepared. The antimicrobial activity of the prepared compounds was evaluated against Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Aspergillus niger and Candida albicans. The dithiohydrazone as well as oxadiazole thiole derivatives, sugar hydrazones and acyclic nucleoside analogs were the highly active compounds.
