Literature DB >> 14684306

Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.

Jin Li1, Kristin M Lundy DeMello, Henry Cheng, Subas M Sakya, Brian S Bronk, Robert J Rafka, Burton H Jaynes, Carl B Ziegler, Carolyn Kilroy, Donald W Mann, Eric L Nimz, Michael P Lynch, Michelle L Haven, Nicole L Kolosko, Martha L Minich, Chao Li, Jason K Dutra, Bryson Rast, Rhonda M Crosson, Barry J Morton, Glen W Kirk, Kathleen M Callaghan, David A Koss, Andrei Shavnya, Lisa A Lund, Scott B Seibel, Carol F Petras, Annette Silvia.   

Abstract

Structure-activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes are described. This led to the identification of 12a as a lead candidate for further progression. The in vitro and in vivo activity of 12a for the canine COX-2 enzyme as well as its in vivo efficacy and pharmacokinetic properties in dog are highlighted.

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Year:  2004        PMID: 14684306     DOI: 10.1016/j.bmcl.2003.10.004

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Mono- and Mixed Metal Complexes of Eu3+, Gd3+, and Tb3+ with a Diketone, Bearing Pyrazole Moiety and CHF2-Group: Structure, Color Tuning, and Kinetics of Energy Transfer between Lanthanide Ions.

Authors:  Victoria E Gontcharenko; Mikhail A Kiskin; Vladimir D Dolzhenko; Vladislav M Korshunov; Ilya V Taydakov; Yury A Belousov
Journal:  Molecules       Date:  2021-05-01       Impact factor: 4.411

  2 in total

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