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dc.creatorSavić, Jelena
dc.creatorDilber, Sanda
dc.creatorMarković, Bojan
dc.creatorMilenković, Marina
dc.creatorVladimirov, Sote
dc.creatorJuranić, Ivan O.
dc.date.accessioned2019-09-02T11:23:40Z
dc.date.available2019-09-02T11:23:40Z
dc.date.issued2011
dc.identifier.issn1420-3049
dc.identifier.urihttps://farfar.pharmacy.bg.ac.rs/handle/123456789/1483
dc.description.abstractSix beta-hydroxy-beta-aryl propanoic acids were synthesised using a modification of Reformatsky reaction which has already been reported. These acids belong to the aryl propanoic acid class of compounds, structurally similar to the NSAIDs, such as ibuprofen, and an anti-inflammatory activity is thus expected. The aim of this work was to determine anti-inflammatory activity, examine gastric tolerability, and to carry out molecular docking experiments to identify potential COX-2 inhibitors among the beta-hydroxy-beta-aryl propanoic acids, and to elucidate the effect a-methyl substitution on the anti-inflammatory activity. Anti-inflammatory activity and gastric tolerability were determined on rats using carragenan induced paw oedema method, and docking studies were carried out using Autodock v4.0.1. The range of ED(50) values is between 127 mu mol/kg and 15 mu mol/kg, while the result for ibuprofen is 51.7 mu mol/kg. Only slight hyperaemia or few petechiae were spotted on rat's stomach. The results indicate that all compounds possess significant anti-inflammatory activity after oral administration, and that 2-methyl-3-hydroxy-3,3-diphenylpropanoic acid has greatest activity, surpassing that of ibuprofen, a standard NSAID. Another compound, 3-hydroxy-3,3-diphenylpropanoic acid, shows activity matching that of ibuprofen, and is non-chiral and is proven to be non-toxic. The most of investigated compounds have interactions with P3 anchor site like COX-2 selective inhibitors. No tested substances or ibuprofen produced any significant gastric lesions.en
dc.publisherMDPI, Basel
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.sourceMolecules
dc.subjectbeta-hydroxy-beta-arylpropanoic acidsen
dc.subjectReformatsky reactionen
dc.subjectanti-inflammatory activityen
dc.subjectmolecular docking simulationsen
dc.subjectCOX-2 selective inhibitoren
dc.titleDocking Studies and alpha-Substitution Effects on the Anti-Inflammatory Activity of beta-Hydroxy-beta-arylpropanoic Acidsen
dc.typearticle
dc.rights.licenseBY
dcterms.abstractМарковић, Бојан; Дилбер, Санда; Савић, Јелена; Владимиров, Соте; Јуранић, Иван О.; Миленковић, Марина;
dc.citation.volume16
dc.citation.issue8
dc.citation.spage6645
dc.citation.epage6655
dc.citation.other16(8): 6645-6655
dc.citation.rankM22
dc.identifier.wos000294249100036
dc.identifier.doi10.3390/molecules16086645
dc.identifier.pmid25134768
dc.identifier.scopus2-s2.0-80052214202
dc.identifier.fulltexthttps://farfar.pharmacy.bg.ac.rs//bitstream/id/362/1481.pdf
dc.type.versionpublishedVersion


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