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Updated: Jun 30, 2025

A Platform of Anti-biofilm Assays Suited to the Exploration of Natural Compound Libraries
Published on: December 27, 2016
Discovery of Dehydroabietylamine Derivatives as Antibacterial and Antifungal Agents
Shu-Guang Zhang1, Yu-Qiang Wan1, Wei-Hua Zhang1
1Jiangsu Key Laboratory of Pesticide, College of Sciences, Nanjing Agricultural University, Nanjing 210095, People's Republic of China.
Abstract:
A diverse array of biologically active derivatives was derived by modifying the chemically active sites of dehydroabietylamine. Herein, we describe the synthesis of a new series of C-19-arylated dehydroabietylamine derivatives using a palladium-catalyzed C(sp3)-H activation reaction. Five analogues (3b, 3d, 3h, 3n, and 4a) exhibited antibacterial activity against Escherichia coli. Compound 4a exhibited strong inhibitory activity against DNA Topo II and Topo IV. Molecular docking modeling indicated that it can bind effectively to the target through interactions with amino acid residues. The synthesized compounds were tested in vitro for their antifungal activity against six common phytopathogenic fungi. The mechanism of action of compound 4c against Rhizoctorzia solani was investigated, revealing that it disrupts the morphology of the mycelium and enhances cell membrane permeability.
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