Literature DB >> 16464588

Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.

Hengmiao Cheng1, Kristin M Lundy DeMello, Jin Li, Subas M Sakya, Kazuo Ando, K Kawamura, Tomoki Kato, Robert J Rafka, Burton H Jaynes, Carl B Ziegler, Rod Stevens, Lisa A Lund, Donald W Mann, Carolyn Kilroy, Michelle L Haven, Erik L Nimz, Jason K Dutra, Chao Li, Martha L Minich, Nicole L Kolosko, Carol Petras, Annette M Silvia, Scott B Seibel.   

Abstract

The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure-activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a canine whole blood COX-2 inhibitory IC50 of 12 nM and selectivity ratio of COX-1/COX-2 greater than 4000-fold.

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Year:  2006        PMID: 16464588     DOI: 10.1016/j.bmcl.2006.01.059

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


  3 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.  Ethyl 5-(ethoxy-carbon-yl)-3-(4-methoxy-phen-yl)-1H-pyrazole-1-acetate.

Authors:  Wen-Liang Dong; Yan-Qing Ge; Bao-Xiang Zhao
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2007-12-06

3.  In vitro cytotoxic evaluation of some synthesized COX-2 inhibitor derivatives against a panel of human cancer cell lines.

Authors:  H Sadeghi-Aliabadi; M Aliasgharluo; A Fattahi; M Mirian; M Ghannadian
Journal:  Res Pharm Sci       Date:  2013-10
  3 in total

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