A new class of 1,2,3-triazol derivatives derived from nimesulide was designed as potential inhibitors of PDE4B. Synthesis of these compounds was carried out via a multi-step sequence consisting of copper-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step in aqueous media. The required azide was prepared via the reaction of aryl amine (obtained from nimesulide) with α-chloroacetyl chloride followed by displacing the α-chloro group by an azide. Some of the synthesized compounds showed encouraging PDE4B inhibitory properties in vitro that is >50% inhibition at 30 μM that were supported by the docking studies of these compounds at the active site of PDE4B enzyme (dock scores ~ -28.6 for a representative compound). Two of these PDE4 inhibitors showed promising cytotoxic properties against HCT-15 human colon cancer cells in vitro with IC50 ~ 21-22 μg/mL.
The nimesulide based novel glycolamide esters were designed and synthesized for the first timeviaa three-step method starting from nimesulide. Structures of the synthesized compounds were confirmed by spectroscopic analysis. All the synthesized compounds were examined for their cytotoxic effectsin vitro,some of which showed significant cytotoxic activities against HCT-15 human colon cancer cell line.
Some novel 1,2,3-triazole derivatives (V) (9 examples) derived from the non-steroidal antiinflammatory drug nimesulide are designed and synthesized via a multi-step sequence involving a copper-catalyzed azide-alkyne cycloaddition as key step. Two of the title compounds, i.e. (VIa) and (VIb), show promising cytotoxic properties against HCT-15 human colon cancer cells in vitro. -(MAREDDY, J.; NALLAPATI, S. B.; ANIREDDY, J.; DEVI, Y. P.; MANGAMOORI, L. N.; KAPAVARAPU, R.; PAL*, S.; Bioorg. Med. Chem. Lett. 23 (2013) 24, 6721-6727, http://dx.
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