4-Thiazolidinone Derivatives as MMP Inhibitors in Tissue Damage: Synthesis, Biological Evaluation and Docking Studies

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dc.contributor.authorYalçın, İsmail
dc.contributor.authorErtan-Bolelli, Tuğba
dc.contributor.departmentEczacılık Fakültesitr_TR
dc.date.accessioned2020-02-18T15:34:21Z
dc.date.available2020-02-18T15:34:21Z
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 κB (NF-κB), 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). © 2018 by the authors.tr_TR
dc.description.indexWos
dc.identifier.endpage18tr_TR
dc.identifier.issn/e-issn1420-3049
dc.identifier.issue2tr_TR
dc.identifier.other415tr_TR
dc.identifier.startpage01tr_TR
dc.identifier.urihttps://doi.org/10.3390/molecules23020415tr_TR
dc.identifier.urihttp://hdl.handle.net/20.500.12575/69778
dc.identifier.volume23tr_TR
dc.language.isoentr_TR
dc.relation.isversionof10.3390/molecules23020415tr_TR
dc.relation.journal4-Thiazolidinone Derivatives as MMP Inhibitors in Tissue Damage: Synthesis, Biological Evaluation and Docking Studiestr_TR
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıtr_TR
dc.rightsCC0 1.0 Universal*
dc.rights.urihttp://creativecommons.org/publicdomain/zero/1.0/*
dc.title4-Thiazolidinone Derivatives as MMP Inhibitors in Tissue Damage: Synthesis, Biological Evaluation and Docking Studiestr_TR
dc.typeArticletr_TR

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