Potansiyel MAO-B İnhibitörü Olarak Propargil Yan Zinciri İçeren Yeni Bileşiklerin Sentezi ve Karakterizasyonu

Abstract

Bu çalışma kapsamında, propargil grubunun Monoaminoksidaz-B (MAO-B) enzimi üzerindeki potansiyel inhibitör etkinliği dikkate alınarak bazı yeni propargil grubu içeren bileşikler sentezlenmiştir. Sentez çalışmalarında, 2- klorobenzimidazol NaH varlığında propargil bromür ile reaksiyona sokulmuş bileşik 1 elde edilmiştir. Bileşik 1 çeşitli benzilamin türevleri ile potasyum karbonat katalizörlüğünde muamele edilerek sonuç ürünlerine (2a-2c) ulaşılmıştır. Elde edilen bileşiklerin yapıları 1HNMR ve 13C-NMR ve HRMS spektroskopik yöntemleri ile doğrulanmıştır. Sentezlenen bileşiklerin MAO enzimleri üzerindeki etkileri in-vitro şartlarda florimetrik yöntem kullanılarak araştırılmıştır. Yapılan aktivite çalışmaları sonucunda sentezlenen bileşiklerin MAO enzimlerini değişen düzeylerde inhibe ettiği tespit edilmiştir.

Keywords

• Propargil
• Benzimidazol
• NMR
• Monoamin Oksidaz
• Parkinson Hastalığı

Synthesis and Characterization of New Compounds Including Propargyl Side Chain as Potential MAO-B Inhibitor

Abstract

In this study, some new propargyl derivatives were synthesized considering potential monoamine oxidase-B (MAO-B) inhibition potency of propargyl moiety. In synthesis studies, 2-chlorobenzimidazole was reacted with propargyl bromide in the presence of NaH and compound 1 was obtained. Compound 1 was treated with various benzylamine derivatives and final products (2a-2c) were gained. Structures of obtained compounds were established by spectroscopic methods. Effects of the synthesized compounds against MAO enzymes were observed by using in-vitro fluorimetric method. Activity studies revealed that synthesis compounds inhibited MAO enzymes to different extends. .

Keywords

• Propargyl
• Benzimidazole
• NMR
• Monoamine Oxydase
• Parkinson’s Disease

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