Abstract
Background: Thiazole derivatives are known as important sulfur containing heterocycles which are present in a wide range of biologically active natural products.
Methods: A series of thiazolone derivatives were synthesized and evaluated for their soybean 15-LOX inhibitory activity. The title compounds were prepared by the reaction of 2-arylthiazol-4(5H)-ones and different aromatic aldehydes. All compounds were characterized and evaluated against soybean 15-LOX. Results: Among the synthesized thiazolone derivatives, 5-(4-methoxybenzylidene)-2-((2-methoxyphenyl) amino)thiazol-4(5H)-one (3l) was found to be the most active compound comparing with quercetin as the reference drug. Conclusion: It seems that prepared thiazolones having methoxy groups both on aryl and aminoaryl moieties can be considered for further drug discovery research.Keywords: Heterocycles, inhibitory activity, 15-LOX, synthesis, thiazolones.
Graphical Abstract
Letters in Organic Chemistry
Title:Synthesis of Thiazolone Derivatives as Novel Soybean 15-LOX Inhibitors
Volume: 14 Issue: 3
Author(s): Mohammad Mahdavi, Mina Saeedi, Hamid Nadri, Mohammad Eghtedari, Sama Gholizadeh, Roshanak Hariri and Tahmineh Akbarzadeh*
Affiliation:
- Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences P.O. Box: 14155-6451, Tehran,Iran
Keywords: Heterocycles, inhibitory activity, 15-LOX, synthesis, thiazolones.
Abstract: Background: Thiazole derivatives are known as important sulfur containing heterocycles which are present in a wide range of biologically active natural products.
Methods: A series of thiazolone derivatives were synthesized and evaluated for their soybean 15-LOX inhibitory activity. The title compounds were prepared by the reaction of 2-arylthiazol-4(5H)-ones and different aromatic aldehydes. All compounds were characterized and evaluated against soybean 15-LOX. Results: Among the synthesized thiazolone derivatives, 5-(4-methoxybenzylidene)-2-((2-methoxyphenyl) amino)thiazol-4(5H)-one (3l) was found to be the most active compound comparing with quercetin as the reference drug. Conclusion: It seems that prepared thiazolones having methoxy groups both on aryl and aminoaryl moieties can be considered for further drug discovery research.Export Options
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Cite this article as:
Mahdavi Mohammad, Saeedi Mina, Nadri Hamid, Eghtedari Mohammad, Gholizadeh Sama, Hariri Roshanak and Akbarzadeh Tahmineh*, Synthesis of Thiazolone Derivatives as Novel Soybean 15-LOX Inhibitors, Letters in Organic Chemistry 2017; 14 (3) . https://dx.doi.org/10.2174/1570178614666170227143902
DOI https://dx.doi.org/10.2174/1570178614666170227143902 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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