الفهرس | Only 14 pages are availabe for public view |
Abstract Development of new routes in heterocyclic synthesis.: Treatment of anthranilamide with ketones to give spiro system was best achieved by running the reaction in the presence of catalytic quantities of ammonium chloride. To generate the alkyne core 331, we examined the reaction of NH-hydrochloride compound with propargyl bromide in alkaline medium. The alkyne product 331 and azide coupling partners were reacted together, under developed copper-catalyzed alkyne-azide cycloaddition (CuAAC) click conditions to deliver the new library of hybrid triazole-bio ligand. synthesis of thienopyrimidine derivatives as analogous of quinazoline compounds in order to find compounds endowed with anti-inflammatory and analgesic activity. Among the synthesized compounds, compound 330c, 330d, 332 and 333 were selected by National Cancer Institute (NCI) to be investigated. The results revealed that compounds 330c, d, 332 and 333 possess a weak to moderate cytotoxic and/or growth inhibitory effect toward different cell lines. The synthesized compounds were screened also for their ability to inhibit PDE 5 compared to sildenafil as a standard reference drug. Most of the synthesized quinazoline-4-one derivatives were found to have PDE 5 inhibitory activity at a concentration of 3 nM (as IC50 of sildenafil). |