Details

Autor(en) / Beteiligte

• Uzgören-Baran, Ayşe
• Tel, Banu Cahide
• Sarıgöl, Deniz
• Öztürk, Elif İnci
• Kazkayası, İnci
• Okay, Gürol
• Ertan, Mevlüt
• Tozkoparan, Birsen

Titel

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

Ist Teil von

• European journal of medicinal chemistry, 2012-11, Vol.57, p.398-406

Ort / Verlag

Kidlington: Elsevier Masson SAS

Erscheinungsjahr

2012

Quelle

Elsevier ScienceDirect Journals

Beschreibungen/Notizen

• 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. [Display omitted] A series of thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones carrying ibuprofen residue (1a–1o) were prepared and tested for their analgesic/anti-inflammatory activities as well as gastric toxicity. ► In this manuscript, a series of thiazolo[3,2-b]-1,2,4-triazole-5(6H)-one derivatives of ibuprofen were synthesized. ► Compounds were evaluated for their potency as analgesic/anti-inflammatory agents. ► Some compounds exhibited potent analgesic/anti-inflammatory activity. ► The gastric risk of the compounds are, in general, lower than with the reference compounds ibuprofen and indomethacin.