Yeni 3,5-disübstitüe-2-pirazolin türevlerinin sentezi ve biyolojik aktivitelerinin incelenmesi

Nuran Kahriman

Öz


Bu çalışmada elektronca zengin azot atomu içeren 5 üyeli heterosikliklerden biri olan pirazolin türevi 3 adet yeni bileşik kalkonlardan başlanarak sentezlendi.  Pirazolinlerin sahip oldukları biyolojik ve farmakolojik özelliği sebebiyle bu bileşiklerin DPPH radikal süpürme ve fosfomolibdenyum indirgeyici güç (PRAP) aktiviteleri ile tirozinaz ve α-glikozidaz enzim inhibisyon aktiviteleri araştırıldı.  Elde edilen veriler doğrultusunda 4 (IC50=16.68 ± 0.19 μM) ve 6 (IC50=22.60 ± 0.83 μM) nolu bileşiklerin standart kojik asitten (IC50=35.41 ± 0.19 μM) daha iyi tirozinaz inhibisyon aktiviteye sahip oldukları belirlendi.  Bileşiklerin α-glukozidaz enzim inhibisyon aktiviteleri çok yüksek olmamakla birlikte 4 (IC50=134.24 ± 2.51 μM) nolu bileşik en yüksek aktiviteyi gösterdi.  Bileşiklerin antioksidan aktivite değerlerine bakıldığında ise 5 nolu bileşik en yüksek DPPH radikal süpürme (%67.59 ± 0.44) ve fosfomolibdenyum indirgeyici güç (PRAP, Abs= 0.815 ± 0.009) aktivitesini sergiledi.  Sonuç olarak bileşik yapılarında farklılık gösteren -NH2 grubunun bağlanma pozisyonu, bileşiklerin biyolojik özelliklerinde belirgin bir farklılığa sebep olmuştur.


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