4-Thiazolidinone derivatives as mmp ınhibitors in tissue damage: synthesis, biological evaluation and docking studies

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dc.contributor.authorYalçın, İsmail
dc.contributor.authorErtan, Tuğba Bolelli
dc.contributor.departmentEczacılık Fakültesitr_TR
dc.date.accessioned2019-06-27T13:06:13Z
dc.date.available2019-06-27T13:06:13Z
dc.date.issued2018
dc.description.abstractNine 2-(1,2-benzothiazol-3-yl)-N-(4-oxo-2-phenyl-1,3-thiazolidin-3-yl)propanamides combining a benzisothiazole and 4-thiazolidinone in one framework were designed and synthesized. The aim of the study was to verify their effectiveness to affect the inflammatory/oxidative process in which free oxygen and nitrite (ROS and RNS) radicals, inflammatory mediators, such as nuclear factor kappa B (NF-kappa B), and matrix metalloproteinases (MMPs) are involved. Docking studies of all the compounds were performed in order to explore their binding mode at the MMP-9 protein. An appreciable anti-inflammatory/potential wound healing effects of the tested compounds was highlighted. Derivative 23, bearing a 4-carboxyphenyl substituent at C2 of the 4-thiazolidinone ring, exhibited the highest activity, being able to inhibit MMP-9 at nanomolar level(IC50 = 40 nM).tr_TR
dc.description.indexScopus
dc.identifier.endpage18tr_TR
dc.identifier.issue02tr_TR
dc.identifier.other10.3390/molecules23020415
dc.identifier.startpage01tr_TR
dc.identifier.urihttp://hdl.handle.net/20.500.12575/66841
dc.identifier.volume23tr_TR
dc.language.isoentr_TR
dc.relation.journalMoleculestr_TR
dc.subject4-Thiazolidinonestr_TR
dc.subjectORAC assaytr_TR
dc.subjectMetalloproteinase-9tr_TR
dc.subjectDocking studytr_TR
dc.subjectKeratinocytes culturestr_TR
dc.title4-Thiazolidinone derivatives as mmp ınhibitors in tissue damage: synthesis, biological evaluation and docking studiestr_TR
dc.typeArticletr_TR

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