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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dc.contributor.authorUzgoren-Baran, Ayse
dc.contributor.authorTel, Banu Cahide
dc.contributor.authorSarigol, Deniz
dc.contributor.authorOzturk, Elif Inci
dc.contributor.authorKazkayasi, Inci
dc.contributor.authorOkay, Gurol
dc.contributor.authorErtan, Mevlut
dc.date.accessioned2024-12-24T19:27:01Z
dc.date.available2024-12-24T19:27:01Z
dc.date.issued2012
dc.departmentSiirt Üniversitesi
dc.description.abstractIn 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.
dc.description.sponsorshipHacettepe University Research Center [04A601005]
dc.description.sponsorshipThis study is supported by a grant from Hacettepe University Research Center (Project no: 04A601005). The authors gratefully thank Allison Block (Nova Translation Ltd.) for her editing work, Tugba Taskin-Tok for her computational study.
dc.identifier.doi10.1016/j.ejmech.2012.07.009
dc.identifier.endpage406
dc.identifier.issn0223-5234
dc.identifier.pmid22840494
dc.identifier.scopus2-s2.0-84870060933
dc.identifier.scopusqualityQ1
dc.identifier.startpage398
dc.identifier.urihttps://doi.org/10.1016/j.ejmech.2012.07.009
dc.identifier.urihttps://hdl.handle.net/20.500.12604/6470
dc.identifier.volume57
dc.identifier.wosWOS:000312621700041
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherElsevier France-Editions Scientifiques Medicales Elsevier
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_20241222
dc.subjectIbuprofen derivatives
dc.subjectThiazolo[3,2-b]-1,2,4-triazole-5(6H)-one
dc.subjectAnalgesic activity
dc.subjectAnti-inflammatory activity
dc.subjectGastric risk
dc.titleThiazolo[3,2-b]-1,2,4-triazole-5(6H)-one substituted with ibuprofen: Novel non-steroidal anti-inflammatory agents with favorable gastrointestinal tolerance
dc.typeArticle

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