Synthesis and pharmacological evaluation of new pyrazolyl benzenesulfonamides linked to polysubstituted pyrazoles and thiazolidinones as anti-inflammatory and analgesic agents

Autor:	Aida E. Bayad, Ibrahim M. El-Ashmawy, Hayam M. A. Ashour
Rok vydání:	2015
Předmět:	010405 organic chemistry Stereochemistry medicine.drug_class Analgesic General Chemistry Pyrazole 010402 general chemistry Reference drug 01 natural sciences Analgesic agents In vitro Anti-inflammatory 0104 chemical sciences chemistry.chemical_compound chemistry medicine Selectivity IC50
Zdroj:	Monatshefte für Chemie - Chemical Monthly. 147:605-618
ISSN:	1434-4475 0026-9247
DOI:	10.1007/s00706-015-1549-x
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::08bda665f8740c5acee29134152e4163 https://doi.org/10.1007/s00706-015-1549-x Zobrazit plný text záznamu Full text from SpringerLink