Journals / Online Türk Sağlık Bilimleri Dergisi / 2022 / Cilt: 7 - Sayı: 2

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

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

Pages
180–187
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

It is planned to reach more effective new compounds with the modifications made on the obtained compounds.

📌 3 Key Takeaways

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Objective & Hypothesis:Objective: Depression is an important psychiatric disease and its incidence is high in the world.
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Key Findings & Data:According to the World Health Organization, 350 million people are diagnosed with depression.
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Conclusion & Impact:It is planned to reach more effective new compounds with the modifications made on the obtained compounds.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Depresyon · doking · monoaminoksidaz

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.

Özet

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.

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Cite This Article

OSMANİYE, D., ÖZKAY, Y. (2022). Synthesis and Characterization of New Pyrrole Derivatives, and Investigation of Their Monoamine Oxidase Inhibition Properties and Molecular Docking Studies. Online Türk Sağlık Bilimleri Dergisi, Cilt: 7 - Sayı: 2, 180–187. https://ajindex.com/articles/406160

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References (1)

  1. Hampel H, Berger C, Buch K, Möller HJ. A review of the reversible MAO A inhibitor moclobemide in geriatric patients. Human Psychopharmacology Clin Exp. 1998;13(1):43-51. doi:10.1002/(SICI)1099-1077(199801)13:1 3.0.CO;2-Z El-Halaby LO, El-Husseiny WM, El-Messery SM, Goda FE. Biphenylpiperazine based MAO inhibitors: synthesis, biological evaluation, reversibility and molecular modeling studies. Bioorg Chem. 2021;105216. doi:10.1016/j.bioorg.2021.105216 Shulman KI, Herrmann N, Walker SE. Current place of monoamine oxidase inhibitors in the treatment of depression. CNS Drugs. 2013;27(10):789-797. doi:10.1007/s40263-013-0097-3 Bonnet U. Moclobemide: therapeutic use and clinical studies. CNS Drug Rev. 2003;9(1):97-140. doi:10.1111/j.1527-3458.2003.tb00245.x Li W, Guo B, Tao K, ve ark. Inhibition of SIRT1 in hippocampal CA1 ameliorates PTSD-like behaviors in mice by protections of neuronal plasticity and serotonin homeostasis via NHLH2/MAO-A pathway. Biochem Biophys Res Commun. 2019;518(2):344-350. doi:10.1016/j.bbrc.2019.08.060 Yamali C, Engin FS, Bilginer S, ve ark. Phenothiazine-based chalcones as potential dual-target inhibitors toward cholinesterases (AChE, BuChE) and monoamine oxidases (MAO-A, MAO-B). J Heterocycl Chem. 2021;58(1):161-171. doi:10.1002/jhet.4156 Takao K, Sakatsume T, Kamauchi H, Sugita Y. Syntheses and evaluation of 2-or 3-(N-cyclicamino) chromone derivatives as monoamine oxidase inhibitors. Chem Pharm Bull. 2020;68(11):1082-1089. doi:10.1248/cpb.c20-00579 Salgin-Goksen U, Telli G, Erikci A, ve ark. New 2-pyrazoline and hydrazone derivatives as potent and selective monoamine oxidase A inhibitors. J Med Chem. 2021;64(4):1989-2009. doi:10.1021/acs.jmedchem.0c01504 Aggarwal NN, Dkhar Gatphoh BF, Kumar MV, Ghetia S, Revanasiddappa B. Synthesis, in silico analysis and antidepressant activity of pyrazoline analogs. Thai J Pharm Sci. 2021;45(1). doi:10.3329/dujps.v19i2.50634 Delogu GL, Kumar A, Gatto G, ve ark. Synthesis and in vitro study of nitro-and methoxy-2-phenylbenzofurans as human monoamine oxidase inhibitors. Bioorg Chem. 2021;107:104616. doi:10.1016/j.bioorg.2020.104616 Sağlık BN, Çavuşoğlu BK, Osmaniye D, ve ark. In vitro and in silico evaluation of new thiazole compounds as monoamine oxidase inhibitors. Bioorg Chem. 2019;85:97-108. doi:10.3390/molecules25184342 Can ÖD, Osmaniye D, Özkay ÜD, ve ark. MAO enzymes inhibitory activity of new benzimidazole derivatives including hydrazone and propargyl side chains. Eur J Med Chem. 2017;131:92-