Show simple item record

dc.creatorSavić, Jelena
dc.creatorDilber, Sanda
dc.creatorMilenković, Marina
dc.creatorKotur-Stevuljević, Jelena
dc.creatorMarković, Bojan
dc.creatorVladimirov, Sote
dc.creatorBrborić, Jasmina
dc.date.accessioned2019-09-02T11:59:41Z
dc.date.available2019-09-02T11:59:41Z
dc.date.issued2017
dc.identifier.issn1573-4064
dc.identifier.urihttp://farfar.pharmacy.bg.ac.rs/handle/123456789/2891
dc.description.abstractBackground: Nonsteriodal anti-inflammatory drugs (NSAIDs) are numerous and widely used for more than 60 years, but there is still a strong need for developing novel selective NSAIDs. The need is justified by the fact that nonselective NSAIDs can produce serious gastric side effects and that some of the selective NSAID are withdrawn due to their cardiotoxic side effects. Methods: Eight beta-hydroxy-beta-arylpropanoic acids, which belong to the arylpropanoic acid class of compounds, structurally similar to some nonsteroidal anti-inflammatory drugs (NSAIDs), were docked into 3D catalytic site of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). Seven out of those eight acids were synthesized using already published modification of Reformatsky reaction additionally optimized by increasing temperature. Synthesized compounds were tested in vivo in order to elucidate anti-inflammatory activity, gastric tolerability and impact on liver function of rats. Results: Results of docking studies have indicated that all compounds have potential to selectively inhibit COX-2 isoform, but that the compounds containing polar substituents on phenyl ring are better inhibitors. Results of carrageenan-induced rat paw oedema test have shown that all compounds exhibit dose dependence and good gastric tolerability and none of the tested compounds have shown negative effect on liver function compared to ibuprofen. Conclusion: The compound containing polar nitro group in para position has shown the best docking results, anti-inflammatory activity, low hepatotoxicity and good gastric tolerability.en
dc.publisherBentham Science Publ Ltd, Sharjah
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS//
dc.rightsrestrictedAccess
dc.sourceMedicinal Chemistry
dc.titleDocking Studies, Synthesis and Biological Evaluation of beta-aryl-beta-hydroxy Propanoic Acids for Anti-inflammatory Activityen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractМарковић, Бојан; Савић, Јелена; Котур-Стевуљевић, Јелена; Дилбер, Санда; Владимиров, Соте; Брборић, Јасмина; Миленковић, Марина;
dc.citation.volume13
dc.citation.issue2
dc.citation.spage186
dc.citation.epage195
dc.citation.other13(2): 186-195
dc.citation.rankM22
dc.identifier.wos000402476700009
dc.identifier.doi10.2174/1573406412666160907150247
dc.identifier.pmid27605092
dc.identifier.scopus2-s2.0-85013862353
dc.identifier.rcubconv_3867
dc.type.versionpublishedVersion


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record