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Synthesis of Thiazolone Derivatives As Novel Soybean 15-Lox Inhibitors Publisher



Mahdavi M1 ; Saeedi M2, 3 ; Nadri H4 ; Eghtedari M5 ; Gholizadeh S1 ; Hariri R3 ; Akbarzadeh T3, 6
Authors
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Authors Affiliations
  1. 1. School of Pharmacy, International Campus (TUMS-IC), Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
  5. 5. Faculty of Chemistry, University of Mazandaran, Babolsar, Iran
  6. 6. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O. Box: 14155-6451, Tehran, Iran

Source: Letters in Organic Chemistry Published:2017


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. © 2017 Bentham Science Publishers.