Synthesis and Characterization of New Pyrrole Derivatives, and Investigation of Their Monoamine Oxidase Inhibition Properties and Molecular Docking Studies

Abstract

Objective: Depression is an important psychiatric disease and its incidence is high in the world. According to the World Health Organization, 350 million people are diagnosed with depression. The use of monoamine oxidase inhibitors in this field also makes the development of new compounds valuable.
Materials and Methods: Pyrrole derivative (2a-2e) compounds consisting of 5 new molecules were synthesized. The structures of the obtained compounds were elucidated using spectroscopic methods. The in vitro monoamine oxidase enzyme inhibitory activities of the compounds were investigated.
Results: Among the synthesized compounds, compounds 2b and 2c showed significant inhibitory activity against monoamine oxidase-A enzyme.
Conclusion: When the selective monoamine oxidase-A inhibitor potentials of the synthesized compounds are examined; it is seen that promising results have been achieved. It is planned to reach more effective new compounds with the modifications made on the obtained compounds.  

Keywords

• Depression
• docking
• monoamine oxidase
• monoamine oxidase inhibitors

Yeni Pirol Türevlerinin Sentezi ve Karakterizasyonu, Monoamin Oksidaz İnhibisyon Özelliklerinin ve Moleküler Doking Çalışmalarının Araştırılması

Abstract

Amaç: Depresyon önemli bir psikiyatrik hastalıktır ve dünyada görülme sıklığı yüksektir. Dünya Sağlık Örgütü tarafından, 2012 yılında yaklaşık 350 milyon kişinin depresyon ile mücadele ettiğini belirtilmiştir. Özellikle monoamin oksidaz-A inhibitörleri depresyon tedavisinde kullanılmaktadır. Monoamin oksidaz inhibitörlerinin bu alanda kullanımı, yeni bileşiklerin geliştirilmesini de değerli kılmaktadır.
Materyal ve Metot: 5 yeni molekülden oluşan pirol türevi (2a-2e) bileşikler sentezlenmiştir. Elde edilen bileşiklerin yapıları spektroskopik yöntemler kullanılarak aydınlatılmıştır. Bileşiklerin in vitro monoamin oksidaz enzim inhibitor etkinlikleri incelenmiştir.
Bulgular: Sentezlenen bileşikler içerisinde 2b ve 2c kodlu bileşikler monoamin oksidaz-A enzimine karşı önemli düzeyde inhibitor etkinlik göstermiştir.
Sonuç: Sentezlenen bileşiklerin selektif monoamin oksidaz-A inhibitör potansiyelleri incelendiğinde umut verici sonuçlara ulaşıldığı görülmektedir. Elde edilen bileşikler üzerinde yapılan modifikasyonlar ile daha etkili yeni bileşiklere ulaşılması planlanmaktadır. 

Keywords

• Depresyon
• doking
• monoaminoksidaz
• monoamin oksidaz inhibitörleri

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