Uzgoren-Baran, AyseTel, Banu CahideSarigol, DenizOzturk, Elif InciKazkayasi, InciOkay, GurolErtan, Mevlut2024-12-242024-12-2420120223-5234https://doi.org/10.1016/j.ejmech.2012.07.009https://hdl.handle.net/20.500.12604/6470In an effort to establish new candidates with improved analgesic and anti-inflammatory activities and lower ulcerogenic risk, a series of thiazolo[3,2-b]-1,2,4-triazole-5(6H)-one derivatives of ibuprofen were synthesized. All compounds were evaluated for their in vivo anti-inflammatory and analgesic activities in mice. Furthermore, the ulcerogenic risks of the compounds were determined. In general, none of the compounds represent a risk for developing stomach injury as much as observed in the reference drugs ibuprofen and indomethacin. The compounds carrying a 3-phenyl-2-propenylidene (1a), (biphenyl-4-yl) methylidene (1f) and (1-methylpyrrol-2-yl)methylidene (1n) at the 6th position of the fused ring have been evaluated as potential analgesic/anti-inflammatory agents without a gastrointestinal side effect. These new compounds, therefore, deserve further attention to develop new lead drugs. (C) 2012 Elsevier Masson SAS. All rights reserved.eninfo:eu-repo/semantics/closedAccessIbuprofen derivativesThiazolo[3,2-b]-1,2,4-triazole-5(6H)-oneAnalgesic activityAnti-inflammatory activityGastric riskThiazolo[3,2-b]-1,2,4-triazole-5(6H)-one substituted with ibuprofen: Novel non-steroidal anti-inflammatory agents with favorable gastrointestinal toleranceArticle57398406Q1WOS:000312621700041Q12-s2.0-848700609332284049410.1016/j.ejmech.2012.07.009