641639-16-9Relevant academic research and scientific papers
Synthesis and Selective Cyclooxygenase-2 Inhibitory Activity of a Series of Novel, Nitric Oxide Donor-Containing Pyrazoles
Ranatunge, Ramani R.,Augustyniak, Michael,Bandarage, Upul K.,Earl, Richard A.,Ellis, James L.,Garvey, David S.,Janero, David R.,Letts, L. Gordon,Martino, Allison M.,Murty, Madhavi G.,Richardson, Stewart K.,Schroeder, Joseph D.,Shumway, Matthew J.,Tam, S. William,Trocha, A. Mark,Young, Delano V.
, p. 2180 - 2193 (2007/10/03)
The synthesis of a series of novel pyrazoles containing a nitrate (ONO 2) moiety as a nitric oxide (NO)-donor functionality is reported. Their COX-1 and COX-2 inhibitory activities in human whole blood are profiled. Our data demonstrate that py
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: A novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors
Ranatunge, Ramani R.,Earl, Richard A.,Garvey, David S.,Janero, David R.,Letts, L. Gordon,Martino, Allison M.,Murty, Madhavi G.,Richardson, Stewart K.,Schwalb, David J.,Young, Delano V.,Zemtseva, Irina S.
, p. 6049 - 6052 (2007/10/03)
The synthesis of a series of novel 3-(2-methoxytetrahydrofuran-2-yl) pyrazoles and their in vitro cyclooxygenase-2 (COX-2) inhibitory activity in human whole blood (HWB) are reported. 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 μM and COX-2: 1.2 μM).
