Screening and evaluation of rat kidney aldose reductase inhibitory activity of some pyridazine derivatives

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dc.contributor.authorSüzen, Sibel
dc.contributor.departmentEczacılık Fakültesitr_TR
dc.contributor.otherŞüküroğlü, Mürat Kadir
dc.contributor.otherÇalışkan, Burcu
dc.contributor.otherDaş-Evci̇Men, Net
dc.contributor.otherSarikaya, Mutlu
dc.contributor.otherBanoğlu, Erden
dc.date.accessioned2020-03-18T06:40:58Z
dc.date.available2020-03-18T06:40:58Z
dc.date.issued2007
dc.description.abstractAldose reductase (AR) is an enzyme that catalyzes the conversion of glucose to sorbitol, which is in turn converted to fructose by sorbitol dehydrogenase. The increased glucose flux through this metabolic pathway has been linked to the development of diabetic complications such as neuropathy, nephropathy, retinopathy, and cataract. Inhibitors of AR thus seem to have the potential to prevent or treat diabetic complications. AR inhibitors belong to different chemical classes, one of which comprises pyridazinone analogues. At present, however, side effects and/or insufficient pharmacokinetic profiles have made most of the drug candidates undesirable. We evaluated a series of 2H-pyridazine-3-one and 6-chloropyridazine analogues via an in vitro spectrophotometric assay for their ability to inhibit rat kidney AR. The study showed that the introduction of a pyrazole ring on pyridazinone led to a marked decrease in AR inhibitory potency. Moreover, introduction of an acetic acid side chain on 2H-pyridazine-3-one and 6-chloropyridazine did not improve the AR inhibitory activity, which was an unexpected result. On the basis of preliminary AR inhibitory screening results on 2H-pyridazine-3-one and 6-chloropyridazine derivatives, we embarked on the synthesis of more derivatives to discover more active molecules.tr_TR
dc.description.indexwos
dc.description.indexScopus
dc.identifier.endpage451tr_TR
dc.identifier.issue7-8tr_TR
dc.identifier.startpage443tr_TR
dc.identifier.urihttps://doi.org/10.1007/s00044-006-0021-1tr_TR
dc.identifier.urihttp://hdl.handle.net/20.500.12575/70713
dc.identifier.volume15tr_TR
dc.language.isoentr_TR
dc.relation.isversionof10.1007/s00044-006-0021-1tr_TR
dc.relation.journalMedicinal Chemistry Researchtr_TR
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıtr_TR
dc.subjectAldose reductasetr_TR
dc.subjectDiabetes mellitusInhibitorytr_TR
dc.subjectPyridazinetr_TR
dc.subjectSynthesistr_TR
dc.titleScreening and evaluation of rat kidney aldose reductase inhibitory activity of some pyridazine derivativestr_TR
dc.typeArticletr_TR

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