Literature DB >> 15546727

3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.

Ramani R Ranatunge1, Richard A Earl, David S Garvey, David R Janero, L Gordon Letts, Allison M Martino, Madhavi G Murty, Stewart K Richardson, David J Schwalb, Delano V Young, Irina S Zemtseva.   

Abstract

A series of 3-(2-methoxytetrahydrofuran-2-yl)pyrazoles (4-10) was synthesized. The compounds were evaluated for their ability to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) activity in human whole blood (HWB). The compound, 5-(4-methanesulfonylphenyl)-3-(2-methoxytetrahydrofuran-2-yl)-1-p-tolyl-1H-pyrazole 5 showed potent and selective COX-2 inhibition (IC50 for COX-1: >100 microM and COX-2: 1.2 microM).

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Year:  2004        PMID: 15546727     DOI: 10.1016/j.bmcl.2004.09.073

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


  4 in total

1.  2-{5-[2-(4-Nitro-phen-oxy)phen-yl]-1-phenyl-1H-pyrazol-3-yl}phenol.

Authors:  Ali Haider; Zareen Akhter; Michael Bolte; Muhammad Zia-Ul Haq; Humaira M Siddiqi
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-03-10

2.  (Z)-Ethyl 2-cyano-2-{2-[5,6-dimethyl-4-(thio-phen-2-yl)-1H-pyrazolo-[3,4-b]pyridin-3-yl]hydrazinylidene}acetate.

Authors:  Hoong-Kun Fun; Madhukar Hemamalini; Hatem A Abdel-Aziz; Tarek Aboul-Fadl
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-07-30

3.  Synthesis of novel 1-[(2,6-dichloro-4-trifluoromethyl)phenyl]-3-aryl-1H-pyrazole-4-carbaldehydes.

Authors:  Huanan Hu; Changhua Ge; Lisheng Ding; Anjiang Zhang
Journal:  Molecules       Date:  2010-10-25       Impact factor: 4.411

4.  4-[5-(4-Chloro-phen-yl)-3-methyl-1H-pyrazol-1-yl]benzene-sulfonamide.

Authors:  Muhammad A Farrukh; Shaaban K Mohamed; Maqsood Ahmed; Adel A Marzouk; Samir M El-Moghazy
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-01-26
  4 in total

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