Antidiyabetik etkili yeni bazı kromonil-tiyazolidindion türevleri üzerinde araştırmalar
| dc.contributor.advisor | Ertan, Rahmiye | |
| dc.contributor.author | Ceylan Ünlüsoy, Meltem | |
| dc.date.accessioned | 2019-02-07T22:31:58Z | |
| dc.date.available | 2009 | |
| dc.date.available | 2019-02-07T22:31:58Z | |
| dc.date.issued | 2009 | |
| dc.description.abstract | Bu çalışmada, 2/3-formil kromon (Ia-b) ile 2,4-tiyazolidindion / imidazolidindion / 2-tiyokso-imidazolin-4-on (IIa-c) halkalarının Knoevenagel kondensasyonu yöntemi kullanılarak reaksiyona sokulmasıyla elde edilen türevlerin (IIIa-c, IVa-c) daha sonra etil veya metil iyodür ile alkilasyonu sonucunda bir seri tekabül eden N-alkil ve S-alkil kromonil-2,4-tiyazolidindion / imidazolidindion / 2-tiyokso-imidazolin-4-on (IIId-i, IVd-i) bileşikleri sentezlenmiştir. Böylece elde edilen toplam 18 orijinal kimyasal maddenin yapı tayinlerinde Elementel Analiz, IR, 1H-NMR, Mass spektral yöntemlerine ilaveten IVd, IVg ve IVi bileşikleri için de X-Işınları kristallografik incelemelerinden yararlanılmıştır. Sentezlenen bileşikler, insülinotropik etki yönünden incelenmiş ve sonuçta IVb, IVc bileşikleri, düşük konsantrasyonda (1 μg/ml), 5.6 mmol/l glukoz varlığında referans bileşik Glibenklamid’den biraz daha yüksek insülin salgılattırıcı aktivite göstermişlerdir. Sentezlenen bileşiklerin kimyasal okunuşları aşağıda topluca bir arada verilmiştir;IIIa5-(4-Okso-4H-kromen-2-il metilen)-tiyazolidin-2,4-dionIIIb5-(4-Okso-4H-kromen-2-il metilen)-imidazolidin-2,4-dionIIIc5-(4-Okso-4H-kromen-2-il metilen)-2-tiyokso-imidazolidin-4-onIIId3-Metil-5-(4-okso-4H-kromen-2-il metilen)-tiyazolidin-2,4-dionIIIe3-Etil-5-(4-okso-4H-kromen-2-il metilen)-tiyazolidin-2,4-dionIIIf1,3-Dimetil-5-(4-okso-4H-kromen-2-il metilen)-imidazolidin-2,4-dionIIIg3-Etil-5-(4-okso-4H-kromen-2-il metilen)-imidazolidin-2,4-dionIIIh3-Metil-2-(metiltiyo)-5-(4-okso-4H-kromen-2-il metilen)-imidazolidin-4-onIIIi3-Etil-2-(etiltiyo)-5-(4-okso-4H-kromen-2-il metilen)-imidazolidin-4-onIVa5-(4-Okso-4H-kromen-3-il metilen)-tiyazolidin-2,4-dionIVb5-(4-Okso-4H-kromen-3-il metilen)-imidazolidin-2,4-dionIVc5-(4-Okso-4H-kromen-3-il metilen)-2-tiyokso-imidazolidin-4-onIVd3-Metil-5-(4-okso-4H-kromen-3-il metilen)-tiyazolidin-2,4-dionIVe3-Etil-5-(4-okso-4H-kromen-3-il metilen)-tiyazolidin-2,4-dionIVf1,3-Dimetil-5-(4-okso-4H-kromen-3-il metilen)-imidazolidin-2,4-dionIVg3-Etil-5-(4-okso-4H-kromen-3-il metilen)-imidazolidin-2,4-dionIVh3-Metil-2-(metiltiyo)-5-(4-okso-4H-kromen-3-il metilen)-imidazolidin-4-onIVi3-Etil-2-(etiltiyo)-5-(4-okso-4H-kromen-3-il metilen)-imidazolidin-4-onAbstractA series of chromonyl-2,4-thiazolidinediones / imidazolidinediones / 2-thioxo-imidazolidine-4-ones (IIIa-i, IVa-i) was prepared by Knoevenagel reaction of 2,4-thiazolidinedione / 2,4-imidazolidinedione / 2-thioxo-imidazolidine-4-one (IIa-c) with 2/3-formyl chromone (Ia-b) and then alkylation with methyl / ethyl iodide . The structure of the synthesized 18 compounds was elucidated by IR, 1H NMR, Mass spectral data and elementary analysis findings and X-Ray analysis of compounds IVd, IVg and IVi was performed. The synthesized compounds were tested for their insulinotropic activities in INS-1 cells. Compounds IVb, IVc (at lower concentration; 1 μg/ml) were able to increase insulin release in the presence of 5.6 mmol/l glucose better than reference compound Glibenclamide. Chemical names of the synthesized compounds are given below;IIIa5-(4-Oxo-4H-chromen-2-yl methylene)-thiazolidine-2,4-dioneIIIb5-(4-Oxo-4H-chromen-2-yl methylene)-imidazolidine-2,4-dioneIIIc5-(4-Oxo-4H- chromen-2-yl methylene)-2-thioxo-imidazolidine-4-oneIIId3-Methyl-5-(4-oxo-4H- chromen-2-yl methylene)-thiazolidine-2,4-dioneIIIe3-Ethyl-5-(4-oxo-4H- chromen-2-yl methylene)-thiazolidine-2,4-dioneIIIf1,3-Dimethyl l-5-(4-oxo-4H- chromen-2-yl methylene)-imidazolidine-2,4-dioneIIIg3-Ethyl-5-(4-oxo-4H- chromen-2-yl methylene)-imidazolidine-2,4-dioneIIIh3-Methyl-2-(metiltiyo)-5-(4-oxo-4H- chromen-2-yl methylene)-imidazolidine-4-oneIIIi3-Ethyl-2-(ethylthio)-5-(4-oxo-4H- chromen-2-yl methylene)-imidazolidine-4-oneIVa5-(4-Oxo-4H- chromen-3-yl methylene)-thiazolidine-2,4-dioneIVb5-(4-Oxo-4H- chromen-3-yl methylene)-imidazolidine-2,4-dioneIVc5-(4-Oxo-4H- chromen-3-yl methylene)-2-tiyokso-imidazolidine-4-oneIVd3-Methyl-5-(4-oxo-4H- chromen-3-yl methylene)-thiazolidine-2,4-dioneIVe3-Ethyl-5-(4-oxo-4H- chromen-3-yl methylene)-thiazolidine-2,4-dioneIVf1,3-Dimethyl-5-(4-oxo-4H- chromen-3-yl methylene)-imidazolidine-2,4-dioneIVg3-Ethyl-5-(4-oxo-4H- chromen-3-yl methylene)-imidazolidine-2,4-dioneIVh3-Methyl-2-(methylthio)-5-(4-oxo-4H- chromen-3-yl methylene)-imidazolidine-4-oneIVi3-Ethyl-2-(ethylthio)-5-(4-oxo-4H-chromen-3-yl methylene)-imidazolidine-4-one | |
| dc.identifier.uri | http://hdl.handle.net/20.500.12575/35457 | |
| dc.language.iso | tr | TR_tr |
| dc.publisher | Sağlık Bilimleri Enstitüsü | |
| dc.subject | TIP, Eczaneler ve medikal depolar | tr |
| dc.title | Antidiyabetik etkili yeni bazı kromonil-tiyazolidindion türevleri üzerinde araştırmalar | |
| dc.type | doctoralThesis |