Generic placeholder image

Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and X. M. Sun

Volume 5, Issue 2, 2008

Page: [127 - 133] Pages: 7

DOI: 10.2174/157018008783928517

Price: $65

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.

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


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy