Guiqing Xu

Design, synthesis and antifungal activity of novel paeonol derivatives linked with 1,2,3-triazole moiety by the click reaction

For obtaining novel bioactive compounds with significant antifungal activities, a series of novel paeonol derivatives linked with a 1,2,3-triazole moiety have been designed and synthesised by a click reaction under mild conditions using Cu(OAc)2·H2O/sodium ascorbate as a catalyst. The antifungal activities of all the target compounds were evaluated in vitro against two plant pathogenic fungi, Colletotrichum capsici and Rhizoctonia cerealis. Preliminary results indicated that 1-(4-methoxy-2-{[1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl]-methoxy}phenyl)ethanone showed the best antifungal activities against C. capsici, while 1-(2-{[1-(2-fuorophenyl)-1H-1,2,3-triazol-4-yl]methoxy}-4-methoxyphenyl)ethanone and 1-(4-methoxy-2-{[1-(o-tolyl)-1H-1,2,3-triazol-4-yl]methoxy}phenyl)ethanone were found to have better antifungal activities against the tested two fungi. All the synthesised compounds have been determined by IR, HR MS and NMR spectra.

Design, synthesis, and antifungal evaluation of novel 1,4-disubstituted 1,2,3-triazoles containing indole framework

Abstract In order to find novel bioactive compounds with significant antifungal activities, a series of novel 1,4-disubstituted 1,2,3-triazoles containing an indole ring via CuCl2/Zn-catalyzed Huisgen cycloaddition were designed, synthesized, and characterized. Antifungal activity against colletotrichum capsici and cotton physalospora pathogens of all the prepared compounds was evaluated, and the test results indicated that these compounds, especially 4g and 4h, showed significant inhibitory effects for fungi. All the synthesized compounds have been characterized by IR, NMR, and high-resolution mass spectra experiments. The preliminary structure activity relationship is also discussed in this paper.

Synthesis, Characterization and Antifungal Evaluation of Novel 2H-1,4-Benzoxazin-3(4H)-one Derivatives Linked with a 1,2,3-Triazole Moiety

In order to obtain novel bioactive compounds with significant antifungal activities, a series of 2H-1,4-benzoxazin-3(4H)-one analogs linked with a 1,2,3-triazole moiety have been designed and synthesized via click reactions in a one-pot process at room temperature using CuCl as the catalyst. Their antifungal activities were tested against two plant-pathogenic fungi, Rhizoctonia cerealis (RC) and Colletotrichum capsici (CC). Statistical analysis showed that among the tested compounds in particular compound 3a exhibits a significant growth inhibitory activity against both RC and CC. All the synthesized compounds have been characterized by IR, HRMS and NMR experiments. Graphical Abstract Synthesis, Characterization and Antifungal Evaluation of Novel 2H-1,4-Benzoxazin-3(4H)-one Derivatives Linked with a 1,2,3-Triazole Moiety

An Efficient Synthesis of 1,4-Disubstituted Triazoles in Water via CuCl2/Zn-Catalyzed Huisgen Cycloaddition

An efficient method for the synthesis of 1,4-disubstituted triazoles in water at room temperature has been developed using CuCl2/Zn as a catalyst system. Under the optimized conditions, a novel series of 1,4-disubstituted 1,2,3-triazoles were synthesized. Graphical Abstract An Efficient Synthesis of 1,4-Disubstituted Triazoles in Water via CuCl2/Zn-Catalyzed Huisgen Cycloaddition

Synthesis of paeonol derivatives linked with 1,2,3-triazole moiety by 1,3-dipolar huisgen-cylcoaddition reaction

Paeonol is a major phenolic component isolated from Moutan Cortex, a traditional Chinese medicine. An efficient synthesis of paeonol derivatives linked to a 1,2,3-triazole moiety using a 1,3-dipolar Huisgen-cycloaddition reaction is described. The paeonol derivatives are regioselectively obtained in good yields under mild conditions using Cu(OAc)2·H2O/sodium ascorbate as a catalyst system, and t-BuOH/H2O (1:1, v/v) as a co-solvent.