title: Thiazolo[3,2-b]-1,2,4-triazole-5(6H)-one substituted with ibuprofen: novel non-steroidal anti-inflammatory agents with favorable gastrointestinal tolerance.
abstract: 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.
authors: Hacettepe University, Faculty of Science, Department of Chemistry, 06800 Ankara, Turkey.
authors: Ayşe
authors: A
authors: Uzgören-Baran
authors: Banu Cahide
authors: BC
authors: Tel
authors: Deniz
authors: D
authors: Sarıgöl
authors: Elif İnci
authors: Eİ
authors: Oztürk
authors: Inci
authors: I
authors: Kazkayası
authors: Gürol
authors: G
authors: Okay
authors: Mevlüt
authors: M
authors: Ertan
authors: Birsen
authors: B
authors: Tozkoparan
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D002351:Carrageenan; D004305:Dose-Response Relationship, Drug; D004361:Drug Tolerance; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D007052:Ibuprofen / Q000737:chemistry* / Q000494:pharmacology; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D051379:Mice; D010147:Pain Measurement; D013270:Stomach / Q000187:drug effects* / Q000473:pathology; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D014230:Triazoles; D002351:Carrageenan; D007052:Ibuprofen; D007213:Indomethacin