Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors.

@article{Eren2010SynthesisBE,
  title={Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors.},
  author={G{\"o}kçen Eren and Serdar Unl{\"u} and Maria-Teresa Nu{\~n}ez and Luis Labeaga and Francisco Ledo and Antonio Entrena and Erden Banoglu and Gabriele Costantino and Mustafa Fethi Şahin},
  journal={Bioorganic & medicinal chemistry},
  year={2010},
  volume={18 17},
  pages={
          6367-76
        }
}
Three novel series of diaryl heterocyclic derivatives bearing the 2-oxo-5H-furan, 2-oxo-3H-1,3-oxazole, and 1H-pyrazole moieties as the central heterocyclic ring were synthesized and their in vitro inhibitory activities on COX-1 and COX-2 isoforms were evaluated using a purified enzyme assay. The 2-oxo-5H-furan derivative 6b was identified as potent COX inhibitor with selectivity toward COX-1 (COX-1 IC(50)=0.061 microM and COX-2 IC(50)=0.325 microM; selectivity index (SI)=0.19). Among the 1H… CONTINUE READING

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