Design, synthesis, characterization and in vitro and in vivo anti-inflammatory evaluation of novel pyrazole-based chalcones
Journal of enzyme inhibition and medicinal chemistry, 2015•Taylor & Francis
A series of novel pyrazole-based chalcones have been designed, synthesized from 1-methyl-
5-(2, 4, 6-trimethoxyphenyl)-1 H-pyrazole (6). The structures of regioisomers 6 and 7 were
determined by 2D 1H–1H COSY, 1H–13C HSQC and 1H–13C HMBC experiments. The
newly synthesized compounds were tested for their inhibitory activity against COX-1 and
COX-2 using an in vitro cyclooxygenase (COX) inhibition assay. Moreover, they were
investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw …
5-(2, 4, 6-trimethoxyphenyl)-1 H-pyrazole (6). The structures of regioisomers 6 and 7 were
determined by 2D 1H–1H COSY, 1H–13C HSQC and 1H–13C HMBC experiments. The
newly synthesized compounds were tested for their inhibitory activity against COX-1 and
COX-2 using an in vitro cyclooxygenase (COX) inhibition assay. Moreover, they were
investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw …
Abstract
A series of novel pyrazole-based chalcones have been designed, synthesized from 1-methyl-5-(2,4,6-trimethoxyphenyl)-1H-pyrazole (6). The structures of regioisomers 6 and 7 were determined by 2D 1H–1H COSY, 1H–13C HSQC and 1H–13C HMBC experiments. The newly synthesized compounds were tested for their inhibitory activity against COX-1 and COX-2 using an in vitro cyclooxygenase (COX) inhibition assay. Moreover, they were investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw edema model for acute inflammation and cotton pellet-induced granuloma model for chronic inflammation. All the synthesized compounds showed potential to demonstrate anti-inflammatory activities, of particular interest compounds 10i, 10e, 10f, and 10h were found to be potent anti-inflammatory agents.
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