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Application of the Mannich reaction in the structural modification of natural products
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Miao-Xia Pu, Hong-Yan Guo, Zhe-Shan Quan, Xiaoting Li, Qing-Kun Shen
Obovatol, a novel lignan bearing a diphenyl ether skeleton, exhibits a wide range of biological activities, including antifungal76, anti-tumor77, anti-inflammatory78, anxiolytic79, anti-platelet80, and anti-AD activities81. The biological activity of obovatol can be significantly improved by introducing active groups at the ortho position of the phenolic hydroxyl group82. Yang et al.83 designed and synthesised a series of C-4-aminomethylated derivatives of obovatol as lead compounds through the Mannich reaction. Inhibition of spore germination and mycelial growth by these derivatives has been investigated against several phytopathogenic fungi.