Title : ( Theoretical and Experimental Enzyme Inhibitory Evaluations of New Derivatives of Dipyrimido[4,5-b:5,4-e][1,4]thiazine on Soybean 15-Lipoxygenase )
Authors: azam karimian , Hossein Eshghi , Mehdi Bakavoli , Ali Shiri , mohammad saadatmandzadeh , tayebe asghari shirghan ,
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Abstract
In recent years, the synthesis of fused heterocyclic compounds possessing pyrimidothiazine as central core has been the focus of great interest [1]. It has been recently reported that these compounds show inhibitory effect against 15-lipoxygenase (15-LO). 15-LO has emerged as an attractive target for therapeutic intervention. It implicates in the progression of certain cancers and plays an important role in the progression of Alzheimer disease [2]. In this study, the novel derivatives of tricyclic dipyrimido[4,5-b:5,4-e][1,4]thiazine (3a–f) were synthesized. Then, the inhibitory activity of the synthesized derivatives was studied as the mean of IC50 on soybean 15-LO. Docking of the synthesized compounds by using of GOLD score fitness function was also evaluated. The in vitro evaluation activities and the results of docking process show that compound (3e) (IC50 = 14 μM) has the best results in inhibitory of 15-LO compared with 4-methyl-2-(4-methylpiperazinyl)pyrimido[4,5-b]benzothiazine (4-MMPB, IC50 = 18 μM) as reference [3]. References [1] Gupta, S.; Ajmera,N.; Gautam,N.; Sharma,R.; Gautam,D. C. Chem. Inform. Abstr. 2009, 40: 42, 853-857. [2] Zhao,L.; Funk, C. D. Trends. Cardiovasc. Med. 2004, 14, 191-195. [3] Bakavoli, M.; Nikpour,M.; Rahimizadeh,M.; Saberi,M. R.; Sadeghian,H. Bioorg. Med. Chem. 2007, 15, 2120-2126.
Keywords
, “Dipyrimidothiazines”, “Bioactive heterocycles”, “Docking”, “15-Lipoxygenase”, “Enzyme Inhibition”
@inproceedings{paperid:1043436,
author = {Karimian, Azam and Eshghi, Hossein and Bakavoli, Mehdi and Shiri, Ali and Saadatmandzadeh, Mohammad and Asghari Shirghan, Tayebe},
title = {Theoretical and Experimental Enzyme Inhibitory Evaluations of New Derivatives of Dipyrimido[4,5-b:5,4-e][1,4]thiazine on Soybean 15-Lipoxygenase},
booktitle = {The 22nd Iranian Seminar of Organic Chemistry},
year = {2014},
location = {تبریز, IRAN},
keywords = {“Dipyrimidothiazines”; “Bioactive heterocycles”; “Docking”; “15-Lipoxygenase”; “Enzyme Inhibition”},
}
%0 Conference Proceedings
%T Theoretical and Experimental Enzyme Inhibitory Evaluations of New Derivatives of Dipyrimido[4,5-b:5,4-e][1,4]thiazine on Soybean 15-Lipoxygenase
%A Karimian, Azam
%A Eshghi, Hossein
%A Bakavoli, Mehdi
%A Shiri, Ali
%A Saadatmandzadeh, Mohammad
%A Asghari Shirghan, Tayebe
%J The 22nd Iranian Seminar of Organic Chemistry
%D 2014
