Design, green synthesis and biological evaluation of fluorinated N-acyl sulfonamides as novel anti-inflammatory agents: an in vivo and in silico study

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dc.contributor.authorLitim, Zaineb
dc.contributor.authorBen Abdeljaoued, Ameni
dc.contributor.authorAbdelhamid, Amal
dc.contributor.authorBouraoui, Abderrahman
dc.contributor.authorOzdemir, Ismail
dc.contributor.authorHamdi, Naceur
dc.contributor.authorSoussi, Mohamed Ali
dc.date.accessioned2026-04-04T13:34:40Z
dc.date.available2026-04-04T13:34:40Z
dc.date.issued2026
dc.departmentİnönü Üniversitesi
dc.description.abstractThe N-acylsulfonamide functional group constitutes a key moiety in numerous successful drugs, primarily due to its high chemical stability and favorable human tolerance profile. Herein, we report the development of a new eco-friendly and highly efficient approach for the preparation of N-acylsulfonamides. This method involves the synthesis of N-sulfonyloxaziridines via oxidation of the corresponding N-sulfonylimines, followed by a facile rearrangement into N-acylsulfonamides under mild and green conditions. The methodology afforded a diverse range of N-acylsulfonamides in good yields and high atom economy (AE). The synthesized compounds were subsequently evaluated for their in vivo anti-inflammatory activity. Specifically, the fluorinated N-acylsulfonamides 3c, 3e, and 3f exhibited potent inhibitory activity against carrageenan-induced inflammation, surpassing the reference drug (diclofenac). Analysis of the structure-activity relationship (SAR) highlighted the critical role of fluorine in enhancing this anti-inflammatory potential. Molecular docking and ADME-T studies were undertaken to elucidate the molecular mechanisms of action and predict the pharmacokinetic profile of these compounds on their biological targets.
dc.identifier.doi10.1039/d6ra01380e
dc.identifier.endpage16000
dc.identifier.issn2046-2069
dc.identifier.issue18
dc.identifier.startpage15992
dc.identifier.urihttps://doi.org/10.1039/d6ra01380e
dc.identifier.urihttps://hdl.handle.net/11616/109306
dc.identifier.volume16
dc.identifier.wosWOS:001720437500001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.language.isoen
dc.publisherRoyal Soc Chemistry
dc.relation.ispartofRsc Advances
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.snmzKA_WOS_20250329
dc.subjectOne-Pot Synthesis
dc.subjectEfficient Method
dc.subjectSolvent-Free
dc.subjectOrganic-Reactions
dc.subjectAcylsulfonamides
dc.subjectInhibitors
dc.subjectAldehydes
dc.subjectCyclooxygenase
dc.subjectSulfonylation
dc.subjectAmidation
dc.titleDesign, green synthesis and biological evaluation of fluorinated N-acyl sulfonamides as novel anti-inflammatory agents: an in vivo and in silico study
dc.typeArticle

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