Design and Synthesis of Novel Diaryl Heterocyclic Derivatives as Selective Cyclooxygenase-2

Title: Design and Synthesis of Novel Diaryl Heterocyclic Derivatives as Selective Cyclooxygenase-2

Volume: 5 Issue: 2

Author(s): S. X. Li, X. D. Deng, F. L. Jiang, Y. J. Zhao, W. S. Xiao, X. Z. Kuang and X. M. Sun

Affiliation:

Keywords: NSAIDs, COX-2, Potency, Anti-inflammatory, Analgesic, Synthesis

Abstract: In this work we reported the design, synthesis and evaluation of the new diaryl heterocyclic derivatives based on the lead compounds of Rofecoxib and Celecoxib by application of the principle of isosterism. The in vivo pharmacological evaluation of these new compounds lead us to select the compounds (Ia) and (IIc) as a new prototype which a substituent ortho to the methylsulfone or sulfonamide group was introduced for further development, more active that celecoxib at the same mass concentration.

Cite this article as:

Li X. S., Deng D. X., Jiang L. F., Zhao J. Y., Xiao S. W., Kuang Z. X. and Sun M. X., Design and Synthesis of Novel Diaryl Heterocyclic Derivatives as Selective Cyclooxygenase-2, Letters in Drug Design & Discovery 2008; 5 (2) . https://dx.doi.org/10.2174/157018008783928517