22nd Iranian Seminar of Organic Chemistry , 2014-10-19

Title : ( Biological Evaluation and Docking Studies of 3,5-Bis ((5-bromo-6-methyl-2-taminopyrimidin-4-yl)thio)-4H-1,2,4-triazol-4-aminesas 15- Lipoxygenase Inhibitors )

Authors: tayebe asghari shirghan , Mehdi Bakavoli , Hossein Eshghi , satar saberi , azam karimian , F. Hadizadeh , M. Ghandadi ,

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Triazoles and their derivatives play important roles in medicinal fields [1]. More over pyrimidine derivatives are highly effective as hypnotic drugs, antitumor, antibacterial agents and in cancer detection. Recently, 15-lipoxygenase (15-LO) has emerged as an attractive target for therapeutic intervention [2]. Keeping this in mind, and in continuation of our recent studies [3] on the enzyme inhibitory activity of heterocyclic compounds against soybean 15LO, we consideredthe synthesis,biological evaluation and molecular docking studiesof new derivatives of 3,5-bis((5-bromo-6-methyl-2-t-aminopyrimidin-4-yl)thio)-4H-1,2,4-triazol-4amines 4a-g and their cyclized products pyrimidotriazolothiadiazines 5a-gas 15-LO inhibitors.Thein vitro evaluation activities and the results of docking process show that compounds 4d (NR 2 =1-methylpiperazine) and 4f (NR 2 =1-ethylpiperazine)have the best IC of 15-LO inhibition (IC 50 50 = 9 and 12 µM, respectively)compared with 4-methyl-2-(4methylpiperazinyl)pyrimido[4,5-b]benzothiazine (IC 50 = 18 µM) as reference [3].

Keywords

, 15-Lipoxygenase (15-LO)”,
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@inproceedings{paperid:1043069,
author = {Asghari Shirghan, Tayebe and Bakavoli, Mehdi and Eshghi, Hossein and Saberi, Satar and Karimian, Azam and F. Hadizadeh and M. Ghandadi},
title = {Biological Evaluation and Docking Studies of 3,5-Bis ((5-bromo-6-methyl-2-taminopyrimidin-4-yl)thio)-4H-1,2,4-triazol-4-aminesas 15- Lipoxygenase Inhibitors},
booktitle = {22nd Iranian Seminar of Organic Chemistry},
year = {2014},
location = {تبریز, IRAN},
keywords = {15-Lipoxygenase (15-LO)”; “Inhibitors”;“Docking”},
}

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%0 Conference Proceedings
%T Biological Evaluation and Docking Studies of 3,5-Bis ((5-bromo-6-methyl-2-taminopyrimidin-4-yl)thio)-4H-1,2,4-triazol-4-aminesas 15- Lipoxygenase Inhibitors
%A Asghari Shirghan, Tayebe
%A Bakavoli, Mehdi
%A Eshghi, Hossein
%A Saberi, Satar
%A Karimian, Azam
%A F. Hadizadeh
%A M. Ghandadi
%J 22nd Iranian Seminar of Organic Chemistry
%D 2014

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