Thiazolo[3,2-b]-1,2,4-triazole-5(6H)-one substituted with ibuprofen: Novel non-steroidal anti-inflammatory agents with favorable gastrointestinal tolerance

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• 作者：Ay?e Uzgö ; ren-Baran^a ; Banu Cahide Tel^b ; Deniz Sar?gö ; l^a ; Elif ?nci Ö ; ztü ; rk^b ; ?nci Kazkayas?^b ; Gü ; rol Okay^c ; Mevlü ; t Ertan^d ; Birsen Tozkoparan^d ; ^{tbirsen@hacettepe.edu.tr}
• 关键词：Ibuprofen derivatives ; Thiazolo[3 ; 2-b]-1 ; 2 ; 4-triazole-5(6H)-one ; Analgesic activity ; Anti-inflammatory activity ; Gastric risk
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：November, 2012
• 年：2012
• 卷：57
• 期：Complete
• 页码：398-406
• 全文大小：508 K

文摘

In 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.