الفهرس | Only 14 pages are availabe for public view |
Abstract The present investigation comprises a survey covering the chemistry and the biological activities of some compounds containing the indole ring system. In this work, diclofenac sodium was used as a precursor to obtain compounds with higher activity and selectivity towards COX-2 enzyme. Acid catalyzed cyclization for diclofenac sodium used to obtain the indole ring.One known and five novel intermediate compounds were prepared, in addition to twenty nine novel final compounds, a detailed discussion of the experimental results attained is presented with an adequate interpretation. The new compounds were subjected to a molecular modeling simulation study using Molegro Virtual Docking software (MVD), to predict their antiinflammatory activity and selectivity towards COX-2 enzyme. Finally, all final compounds were subjected to in vivo evaluation of analgesic activity using acetic acid induced writhing method, and antiinflammatory activity using carrageenan induced paw edema, as well as ulcerogenicity via oral administration of test compounds, the results revealed that compounds V1, V5, V10, VI1, VI5, VI6, VI8, VI9, VI11, VIII2, IX2, and IX4 were the most active. |