Journal of Pharmaceutical Practice 2020;38(6):506-508

doi:10.12206/j.issn.1006-0111.201908127

Study on synthesis and antifungal activities of galloyl piperazine derivatives

Hanxuan WANG 1 ; Jiaxiao DONG 2 ; Ying MA 3 ; Yue GAO 4 ; Yongsheng JIN 4

Affiliations

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Keywords

gallic acid; antifungals; synergy; synthesis

Country

China

Language

Chinese

Abstract

Objective To design, synthesize and measure antifungal activities of galloyl piperazine derivatives. Methods Trimethoxyl gallic acid was used as starting material, reacted with piperazine in the presence of PyBOP/DIEA to afford the intermediates. The target compounds were obtained through the reaction with corresponding acids after deprotection gave. The antifungal activities of the target compounds were evaluated by FLC-resistant Candida albican isolated according to the CLSI recommended method. Results 11 target compounds were synthesized and six of them showed more potent antifungal activities than gallic acid. Conclusion Galloyl piperazine derivatives could enhance antifungal activities. Galloyl moiety was an important pharmacophore, which could improve antifungal activities with the introduction of cinnamic acid and 2,3-dichlorobenzoic acid.