Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

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


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.

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

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Article Details

Year: 2008
Page: [127 - 133]
Pages: 7
DOI: 10.2174/157018008783928517
Price: $58