학술논문
Synthesis and pharmacological evaluation of new pyrazolyl benzenesulfonamides linked to polysubstituted pyrazoles and thiazolidinones as anti-inflammatory and analgesic agents
Document Type
Original Paper
Source
Monatshefte für Chemie - Chemical Monthly: An International Journal of Chemistry. March 2016 147(3):605-618
Subject
Language
English
ISSN
0026-9247
1434-4475
1434-4475
Abstract
New compounds comprising the pyrazolyl benzenesulfonamide scaffold linked to polysubstituted pyrazoles and thiazolidinones were synthesized and evaluated for their anti-inflammatory and analgesic activities. The results revealed that most of the compounds displayed distinctive anti-inflammatory and analgesic activity. Two thiazolidinone derivatives emerged with the highest anti-inflammatory activity in this study, whereas two pyrazole derivatives displayed high analgesic activity with a fast onset of action compared to the reference drug. Moreover, the active compounds showed minimal potential for gastric injury in addition to a good safety margin (ALD50 >0.25 g/kg). In vitro COX-1/COX-2 inhibition study revealed that the most active compounds showed relatively more selectivity toward COX-2 than COX-1. Among the test compounds, a thiazolidinone derivative possessed the lowest IC50 value against both COX-1 and COX-2.Graphical abstract: