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

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.

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

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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