Sıçan Eritrosit Glukoz 6-Fosfat Dehidrogenaz Enzim İnhibitörleri Olarak Tiyosemikarbazon Temelli Aza-Ylidlerin Sentezi

Year 2019, , 1503 - 1512, 01.09.2019

Yusuf Temel , Sinan Bayındır

https://doi.org/10.21597/jist.518012

Cited By: 6

Abstract

Glukoz 6-fosfat dehidrogenaz (G6PD) enzimi NADPH, bazı amino asitler, sfingozin, steroid hormonları, kolesterol, yağ asitleri ve riboz 5-fosfat sentezi gibi pek çok biyokimyasal prosesin gerçekleşmesinde çok önemli bir role sahiptir. Bu çalışmada, tiyoasetazon, ambazon ve perklozon gibi birçok ilacın ana iskeletini oluşturan tiyosemikarbazon temelli aza-ylid (TSCAs) türevi 3a-3e moleküllerinin sentezi çevreci bir yaklaşımla gerçekleştirilerek, G6PD enzim aktivitesi üzerine in vitro şartlarda inhibisyon ve aktivasyon etkisi araştırılmıştır. Çalışmalar neticesinde, sentezlenen TSCAs türevleri 3a-3d moleküllerinin G6PD enzim aktivitesini 40.77 μM ile 58.0 μM aralığındaki IC50 değerlerinde inhibe ettiği belirlenmiştir.

Keywords

Tiyosemikarbazon, aza-ylid, sıçan eritrosit, enzim, G6PD

The Synthesis of Thiosemicarbazone-Based Aza-Ylides as Inhibitors of Rat Erythrocyte Glucose 6-Phosphate Dehydrogenase Enzyme

Abstract

Glucose 6-phosphate dehydrogenase (G6PD) enzyme plays an important role in various biochemical processes such as synthesis of cholesterol, fatty acids, sphingosine, steroid hormones, NADPH, some amino acids and ribose 5-phosphate. In this study, thiosemicarbazone-based aza-ylide (TSCAs) derivatives 3a-3e, which form the main framework of many drugs such as thioacetazone, ambazone, and perchlozone, were synthesized with a green approach and in vitro inhibitor or activator effects on G6PD enzyme activity was investigated. As a result of studies, TSCAs derivatives 3a-3d inhibited the G6PD enzyme activity with IC50 in the range of 40.77 μM to 58.0 μM for G6PD.

Keywords

Thiosemicarbazone, aza-ylides, rat eritrosit, enzyme, 6PGD

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