Rat lung aldose reductase inhibition capacity of substituted indole hydrazide/hydrazone derivatives

Simple item page
dc.contributor.authorSüzen, Sibel
dc.contributor.departmentEczacılık Fakültesitr_TR
dc.contributor.otherDaş Evcimen, Net
dc.contributor.otherSarikaya, Mutlu
dc.contributor.otherKaraaslan, Cigdem
dc.contributor.otherYilmaz, Ayşe Didem
dc.contributor.otherShirinzadeh, Hanif
dc.date.accessioned2020-03-18T11:00:09Z
dc.date.available2020-03-18T11:00:09Z
dc.date.issued2012
dc.description.abstractDiabetes Mellitus is one of the most serious health problem facing both developed and developing countries. Long term complications lead to morbidity and mortality in patients with diabetes. Increased polyol pathway has been implicated in the pathogenesis of microvascular complications and cataract. Aldose reductase (AR) is the key enzyme of the polyol pathway, which converts glucose to sorbitol. Excessive accumulation of sorbitol is associated to the diabetic complications. Avoidance of sorbitol accumulation by inhibiting AR would be an efficient treatment. Due to the significance of AR as a potential drug target in the treatment of diabetic complications, there are increasing interests in the design and synthesis of AR inhibitors. In this study, 2-fluorophenylindol and 5-chloroindole hydrazide/hydrazone derivatives were tested for measuring the AR enzyme inhibitory activity. The enzyme activity was assayed by spectrophotometrically monitoring NADPH oxidation, which accompanies the reduction of D,L-glyceraldehyde used as substrate. Results showed in general 52-60 % inhibitory activity in halogen substituted indole derivatives. This study proposes a new approach for the in vitro AR inhibition activity properties and structure activity relationship of 2, 3-and 5-substituted indole ring. For the inhibitory activity, not only the indole ring is important, but also is the side chain containing the amide group and halogens.tr_TR
dc.description.indexScopus
dc.identifier.endpage174tr_TR
dc.identifier.issue4tr_TR
dc.identifier.startpage169tr_TR
dc.identifier.urihttps://doi.org/10.13140/RG.2.1.2049.9283tr_TR
dc.identifier.urihttp://hdl.handle.net/20.500.12575/70729
dc.identifier.volume37tr_TR
dc.language.isoentr_TR
dc.relation.isversionof10.13140/RG.2.1.2049.9283tr_TR
dc.relation.journalFabad Journal of Pharmaceutical Sciencestr_TR
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıtr_TR
dc.subjectAldose reductasetr_TR
dc.subjectDiabetestr_TR
dc.subjectIndoletr_TR
dc.subjectInhibitiontr_TR
dc.subjectPolyol pathwaytr_TR
dc.titleRat lung aldose reductase inhibition capacity of substituted indole hydrazide/hydrazone derivativestr_TR
dc.typeArticletr_TR

Files

Original bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
2012-FABAD.pdf
Size:
374.73 KB
Format:
Adobe Portable Document Format
Description:
Download
License bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
license.txt
Size:
1.62 KB
Format:
Item-specific license agreed upon to submission
Description:
Download

Collections

Makale
Scopus İndeksli Yayınlar