N-Alkillenmiş Tetrazol Türevi Bileşiklerin Absorpsiyon, Dağılım, Metabolizma ve Atılım (ADME) Özelliklerinin Araştırılması

Year 2019, , 384 - 394, 30.11.2019

Hamdi Özkan

https://doi.org/10.29233/sdufeffd.631009

Cited By: 2

Abstract

Tetrazoller heterosiklik
bileşiklerdir. Tetrazol halkası içeren
bileşikler, antiviral, antibakteriyel, antifungal, antialerjik, antiülser,
antikonvülsan, antiinflamatuar, antitüberküloz gibi farmakolojik
etkinliklerinden dolayı ilaç sentezinde sıklıkla kullanılır. Tetrazol türevi
bir ilaç olan Losartan yüksek tansiyon, Tomelukast astım tedavisinde
kullanılır. Bu çalışmada, aromatik
halkalar içeren N-alkillenmiş
tetrazol türevleri sentezlendi. Sentezlenen bileşiklerin yapıları spektroskopik
yöntemlerle aydınlatıldı. Aynı zamanda, sentezlenen moleküllerin ADME (absorpsiyon,
dağılım, metabolizma ve atılım) özellikleri in
silico olarak incelendi. Teorik olarak, bileşik 4a, 4b ve 4c'nin ince bağırsağından absorpsiyon
yüzdeleri hesaplandı ve sırasıyla 93,95, 93,95 ve 90,77 gibi çok yüksek
değerler bulundu. Tetrazol halkasını içeren bu bileşikler, merkezi sinir
sistemini etkileyecek moleküller için önemli bir özellik olan kan beyin
bariyerini kolayca geçerler. Bu nedenle, bu bileşiklerin antidepresan ilaçların
sentezi için iyi adaylar oldukları söylenebilir.

Keywords

Heterosiklik Bileşik, Tetrazol, ADME, Farmakokinetik

Thanks

Çalışma sürecinde verdikleri desteklerden dolayı Prof. Dr. Yılmaz Yıldırır, Prof. Dr. Ali Dişli, Doç. Dr. Şevki Adem ve Batuhan Yetim’e teşekkürlerimi sunarım.

N-Alkylated Tetrazole Derivative Compounds and Investigation of Absorption, Distribution, Metabolism and Excretion (ADME) Properties

Abstract

Tetrazoles
are heterocyclic compounds. The compounds containing the tetrazole ring are
frequently used in drug synthesis due to their pharmacological activities such
as antiviral, antibacterial, antifungal, antiallergic, antiulcer,
anticonvulsant, anti-inflammatory, antituberculosis. Tetrazole derivated drug
Losartan is used to treat high blood pressure, Tomelukast asthma. In this
study, N-alkylated tetrazole
derivatives containing substituted aromatic rings were synthesized. The
structures of the synthesized compounds were determined by spectroscopic
methods. At the same time, ADME (absorption, distribution, metabolism and
excretion) properties of the synthesized molecules were investigated as silico. Theoretically, the percentages
of absorption from the small intestine of compounds 4a, 4b and 4c were calculated and very high values
were found, such as 93.95, 93.95 and 90.77, respectively. These compounds
containing the tetrazole ring easily cross the blood brain barrier, which is an
important property for molecules that will affect the central nervous system.
Therefore, it can be said that these compounds are good candidates for the
synthesis of antidepressant drugs.

Keywords

Heterocyclic Compounds, Tetrazole, ADME, Pharmacokinetic

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