Synthesis and selective cyclooxygenase-2 (COX-2) inhibitory activity of a series of novel bicyclic pyrazoles

RR Ranatunge, DS Garvey, DR Janero, LG Letts…

Index: Ranatunge, Ramani R.; Garvey, David S.; Janero, David R.; Letts, L. Gordon; Martino, Allison M.; Murty, Madhavi G.; Richardson, Stewart K.; Young, Delano V.; Zemetseva, Irina S. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 6 p. 1357 - 1366

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Citation Number: 47

Abstract

Novel series of pyrazolo [5, 1-b] 1, 3-oxazolidines, pyrazolo [5, 1-b] 1, 3-oxazines and imidazolidino [1, 2-d] pyrazoles were synthesized. These compounds were evaluated in vitro for their ability to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) in human whole blood (HWB). Several of the compounds were found to be novel and selective COX-2 inhibitors, the most potent and selective being 1-(5-cyclohexyl (2H, 3H-pyrazolo [5, ...