Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593306 | Bioorganic & Medicinal Chemistry Letters | 2013 | 14 Pages |
Abstract
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 â¼Â â28.6 for a representative compound). Two of these PDE4 inhibitors showed promising cytotoxic properties against HCT-15 human colon cancer cells in vitro with IC50 â¼Â 21-22 μg/mL.
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Authors
Jyoti Mareddy, Suresh Babu Nallapati, Jayasree Anireddy, Yumnam Priyadarshini Devi, Lakshmi Narasu Mangamoori, Ravikumar Kapavarapu, Sarbani Pal,