Study on synthesis and antifungal activities of galloyl piperazine derivatives
10.12206/j.issn.1006-0111.201908127
- VernacularTitle:没食子酰哌嗪类化合物的合成及抗真菌作用研究
- Author:
Hanxuan WANG
1
,
2
;
Jiaxiao DONG
2
;
Ying MA
3
;
Yue GAO
4
;
Yongsheng JIN
4
Author Information
1. School of Pharmacy, Naval Medical University, Shanghai 200433, China
2. Department of Drug and Equipment, the 72nd Group Army Hospital of PLA, Huzhou 313000，China.
3. Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in University of Shandong, Yantai 264005, China.
4. School of Pharmacy, Naval Medical University, Shanghai 200433, China.
- Keywords:
gallic acid;
antifungals;
synergy;
synthesis
- From:
Journal of Pharmaceutical Practice
2020;38(6):506-508
- CountryChina
- 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.
