Literature DB >> 16275075

5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog.

Subas M Sakya1, Kristin M Lundy DeMello, Martha L Minich, Bryson Rast, Andrei Shavnya, Robert J Rafka, David A Koss, Hengmiao Cheng, Jin Li, Burton H Jaynes, Carl B Ziegler, Donald W Mann, Carol F Petras, Scott B Seibel, Annette M Silvia, David M George, Lisa A Lund, Suzanne St Denis, Anne Hickman, Michelle L Haven, Michael P Lynch.   

Abstract

Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO(2)Me)/sulfamoyl (SO(2)NH(2))-pyridine derivatives for canine COX enzymes are described. The studies led to the identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats.

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Year:  2005        PMID: 16275075     DOI: 10.1016/j.bmcl.2005.10.006

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.  Crystal structure of 5-butyl-amino-3-methyl-1-(pyridin-2-yl)-1H-pyrazole-4-carbaldehyde obtained from a microwave-assisted reaction using caesium carbonate as catalyst.

Authors:  Mario A Macías; Jessica Orrego-Hernández; Jaime Portilla
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2016-10-28

3.  Crystal structure of 5-chloro-N1-(5-phenyl-1H-pyrazol-3-yl)benzene-1,2-di-amine.

Authors:  Yegor Yartsev; Vitaliy Palchikov; Alexandr Gaponov; Svitlana Shishkina
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2017-05-26
  3 in total

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