Synthesis of Thiazolone Derivatives as Novel Soybean 15-LOX Inhibitors

Page: [186 - 191] Pages: 6

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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