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Dergiler / Turkish Journal of Pharmaceutical Sciences / 2019 / Cilt: 16 - Sayı: 1

Synthesis and Aldose Reductase Inhibitory Effect of Some New Hydrazinecarbothioamides and 4-Thiazolidinones Bearing an Imidazo[2,1-b] Thiazole Moiety

İmidazo[2,1-b]Tiyazol Çekirdeği Taşıyan Bazı Yeni Hidrazinkarbotiyoamitler ve 4-Tiyazolidinonların Sentezi ve Aldoz Redüktaz İnhibitör Etkileri

Nuray GÜZELDEMİRCİ
Selin CİMOK
Net DAŞ EVCİMEN
Mutlu SARIKAYA
Sayfa
1–7
DOI
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⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

The synthesized compounds were tested for their ability to inhibit rat kidney AR.Results: Among the synthesized compounds, 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-benzoylhydrazinecarbothioamide (3d)showed the best AR inhibitory activity.Conclusion: The findings of this study indicate that the different derivatives of the compounds in this study may be considered interesting candidatesfor future research.

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Amaç & Hipotez:Objectives: To synthesize and characterize 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamide and3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinone derivatives andevaluate them for their aldose reductase (AR) inhibitory effect.Materials and Methods: 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamides (3a-f) and 3-alkyl/aryl2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinones (4a-j) were synthesized from2-[6-(4-bromophenyl)imidazo[2,1-b]thiazole-3-yl]acetohydrazide (2).
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Temel Bulgular & Veri:Their structures were elucidated by elemental analyses and spectroscopicdata.
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Sonuç & Katkı:The synthesized compounds were tested for their ability to inhibit rat kidney AR.Results: Among the synthesized compounds, 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-benzoylhydrazinecarbothioamide (3d)showed the best AR inhibitory activity.Conclusion: The findings of this study indicate that the different derivatives of the compounds in this study may be considered interesting candidatesfor future research.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:Alan Parametreleri

Özet

Objectives: To synthesize and characterize 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamide and3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinone derivatives andevaluate them for their aldose reductase (AR) inhibitory effect.Materials and Methods: 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamides (3a-f) and 3-alkyl/aryl2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinones (4a-j) were synthesized from2-[6-(4-bromophenyl)imidazo[2,1-b]thiazole-3-yl]acetohydrazide (2). Their structures were elucidated by elemental analyses and spectroscopicdata. The synthesized compounds were tested for their ability to inhibit rat kidney AR.Results: Among the synthesized compounds, 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-benzoylhydrazinecarbothioamide (3d)showed the best AR inhibitory activity.Conclusion: The findings of this study indicate that the different derivatives of the compounds in this study may be considered interesting candidatesfor future research.

Abstract

Amaç: Bu çalışmanın amacı, 2-[[6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il]asetil]-N-alkil/arilhidrazinkarbotiyoamit ve 3-alkil/aril-2-[((6-(4- bromofenil)imidazo[2,1-b]tiyazol-3-il)asetil)hidrazono]-5-nonsübstitüe/metil-4-tiyazolidinon türevlerini sentezlemek, yapılarını aydınlatmak ve aldoz redüktaz (AR) inhibitör etkilerini araştırmaktır. Gereç ve Yöntemler: 2-[6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il]asetohidrazitten (2) hareketle 2-[[6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il] asetil]-N-alkil/arilhidrazinkarbotiyoamit (3a-f) ve 3-alkil/aril-2-[((6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il)asetil)hidrazono]-5-nonsübstitüe/ metil-4-tiyazolidinon türevleri (4a-j) sentezlenmiştir. Bileşiklerin yapıları elementel analiz ve spektroskopik bulgularla kanıtlanmıştır. Sentezlenen bileşikler sıçan böbrek AR enzimini inhibe etme özellikleri açısından test edilmiştir. Bulgular: Sentezlenen bileşikler arasından, 2-[[6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il]asetil]-N-benzoilhidrazinkarbotiyoamit (3d) en iyi AR inhibitör etkiyi göstermiştir. Sonuç: Bu çalışmanın bulguları, bu çalışmadaki bileşiklerin farklı türevlerinin gelecek araştırmalar için ilginç adaylar olarak görülebileceğini göstermektedir.

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Bu Makaleye Atıf Yap

GÜZELDEMİRCİ, N., CİMOK, S., EVCİMEN, N. D., SARIKAYA, M. (2019). Synthesis and Aldose Reductase Inhibitory Effect of Some New Hydrazinecarbothioamides and 4-Thiazolidinones Bearing an Imidazo[2,1-b] Thiazole Moiety. Turkish Journal of Pharmaceutical Sciences, Cilt: 16 - Sayı: 1, 1–7. https://ajindex.com/articles/403642

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