Synthesis, Antioxidant, Xanthine Oxidase and Urease Inhibitory Activities of Some Chlorine Containing Benzimidazoles

Year 2016, Volume: 44 Issue: 3, 293 - 305, 01.09.2016

Nimet Baltaş Fatih Yılmaz Emre Menteşe

Abstract

Aseries of tetra-substitued benzimidazole derivatives were synthesized and screened for their urease inhibi- tion, anti-xanthine oxidase XO and antioxidant activities. Some of them were found to possess significant antioxidant activity, especially, compounds 4, 5a, 5b, 5c, 5d and 6b exhibited highly scavenging activity in ABTS•+ radical cation decolorization assay SC50: 9.51-70.43 μg/mL and cupric reducing antioxidant capacity CUPRAC assay. Compound 6d exhibited the highest XO inhibition at 125 μg/mL. All compounds were evalua- ted with regard to Jack Bean urease activity and the most active compound concerning urease enzyme inhibi- tion was 5b , with an IC50 value of 7.41±0.13 μg/mL.

Keywords

urease, Xanthine oxidase, enzyme inhibition, antioxidant activity, benzimidazole

Bazı Klor İçeren Benzimidazollerin Sentezi ve Antioksidan, Ksantin Oksidaz ve Üreaz İnhibitör Aktivitelerinin İncelenmesi

Abstract

B ir seri tetra-substitüe benzimidazol türevi sentezlendi ve üreaz inhibisyon, anti-ksantin oksidaz XO ve antioksidan aktiviteleri incelendi. Bazı bileşiklerin önemli derecede antioksidan aktivite gösterdiği tespit edildi. Özellikle, bileşik 4, 5a, 5b, 5c, 5d ve 6b ABTS•+ radikal katyon temizleme SC: 9.51-70.43 µg/mL ve bakır indirgeyici antioksidan kapasite CUPRAC tayininde yüksek derecede aktivite gösterdiği belirlendi. Bileşik 6d ise, 125 µg/mL derişimde en yüksek anti-ksantin oksidaz XO aktivitesi gösterdi. Bütün bileşikler Jack Bean üreaz aktivite tayin yöntemine göre incelendi ve en aktif üreaz inhibisyonuna sahip bileşiğin 7.41±0.13 µg/mL IC değeriyle 5b olduğu tespit edildi

Keywords

Üreaz, ksantin oksidaz, enzim inhibisyon, antioksidan aktivite, benzimidazol

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