Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors.

@article{Alegaon2014SynthesisON,
  title={Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors.},
  author={Shankar G. Alegaon and Mita B. Hirpara and Kallanagouda Ramappa Alagawadi and Kirankumar Hullatti and Kamlesh Kashniyal},
  journal={Bioorganic & medicinal chemistry letters},
  year={2014},
  volume={24 22},
  pages={5324-9}
}
A series of 1,3,4-trisubstituted pyrazole derivatives (3 a-f), (4 a-f), and (5 a-f) have been synthesized and evaluated for their cyclooxygenase (COX-1 and COX-2) inhibitory activity. The structures of newly synthesized compounds were characterized by IR, 1H NMR, and mass spectral analysis. All of the compounds showed good inhibition of COX-2 with IC50 of 1.33-17.5 μM. Among these derivatives, compound (5c) was the most potent and selective COX-2 inhibitor (IC50 = 1.33 μM), with a significant… CONTINUE READING