Novel Pyrimidine Derivatives Bearing a 1,3,4-Thiadiazole Skeleton: Design, Synthesis, and Antifungal Activity

被引:12
作者
Pan, Nianjuan [1 ]
Liu, Chunyi [1 ]
Wu, Ruirui [1 ]
Fei, Qiang [1 ]
Wu, Wenneng [1 ]
机构
[1] Guiyang Univ, Food & Pharmaceut Engn Inst, Guiyang, Peoples R China
来源
FRONTIERS IN CHEMISTRY | 2022年 / 10卷
关键词
4-thiadiazole; pyrimidine; design; synthesis; antifungal activity; BIOLOGICAL-ACTIVITY; DISCOVERY; WILT;
D O I
10.3389/fchem.2022.922813
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In this study, twenty novel pyrimidine derivatives bearing a 1,3,4-thiadiazole skeleton were designed and synthesized. Then their antifungal activity against Botrytis cinereal (B. cinereal), Botryosphaeria dothidea (B. dothidea), and Phomopsis sp. were determined using the poison plate technique. Biological test results showed that compound 6h revealed lower EC50 values (25.9 and 50.8 mu g/ml) on Phompsis sp. than those of pyrimethanil (32.1 and 62.8 mu g/ml).
引用
收藏
页数:5
相关论文
共 50 条
  • [31] New 1,3,4-Thiadiazole Derivatives: Synthesis, Characterization, and Antimicrobial Activity
    Abo-Bakr, Ahmed M.
    Hashem, Heba E.
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2019, 56 (03) : 1038 - 1047
  • [32] Novel 1,3,4-Thiadiazole-2-yl-pyrimidine Derivatives In Vitro and the Etymology of Antifungal Activity
    Andrews, B.
    Sudarsan, S.
    Durairaj, A. Leo Michael
    RUSSIAN JOURNAL OF ORGANIC CHEMISTRY, 2024, 60 (SUPPL1) : S22 - S27
  • [33] Synthesis and Biological Activity of Acylthiourea Derivatives Contain 1,2,3-thiadiazole and 1,3,4-thiadiazole
    Yang, Ming-Yan
    Zhao, Wen
    Sun, Zhao-Hui
    Tan, Cheng-Xia
    Weng, Jian-Quan
    Liu, Xing-Hai
    LETTERS IN DRUG DESIGN & DISCOVERY, 2015, 12 (04) : 314 - 318
  • [34] New 1,3,4-Thiadiazole Derivatives with Anticancer Activity
    Janowska, Sara
    Khylyuk, Dmytro
    Bielawska, Anna
    Szymanowska, Anna
    Gornowicz, Agnieszka
    Bielawski, Krzysztof
    Noworol, Jaroslaw
    Mandziuk, Slawomir
    Wujec, Monika
    MOLECULES, 2022, 27 (06):
  • [35] Synthesis and antitumor activity evaluation in vitro of 4-aminoquinazoline derivatives containing 1,3,4-thiadiazole
    Si, Xiaojie
    Dai, Honglin
    Gao, Chao
    Wang, Hao
    Chi, Lingling
    Wang, Zhangjie
    Liu, Limin
    Zhang, Luye
    Li, Erdong
    Zheng, Jiaxin
    Wang, Yaoyao
    Ke, Yu
    Liu, Hongmin
    Zhang, Qiurong
    MEDICINAL CHEMISTRY RESEARCH, 2022, 31 (08) : 1384 - 1392
  • [36] Synthesis and Evaluation of Biological Activity of Homodrimane Sesquiterpenoids Bearing 1,3,4-Oxadiazole or 1,3,4-Thiadiazole Units
    Lungu, Lidia
    Ciocarlan, Alexandru
    Smigon, Crina
    Ozer, Ilker
    Shova, Sergiu
    Gutu, Iacob
    Vornicu, Nicoleta
    Mangalagiu, Ionel
    D'Ambrosio, Michele
    Aricu, Aculina
    CHEMISTRY OF HETEROCYCLIC COMPOUNDS, 2020, 56 (05) : 578 - 585
  • [37] Synthesis and cytotoxic evaluation of new colchicine derivatives bearing 1,3,4-thiadiazole moieties
    Shen, Li-Hong
    Li, Hong-Yu
    Shang, Hui-Xia
    Tian, Shu-Ting
    Lai, Yi-Sheng
    Liu, Li-Jie
    CHINESE CHEMICAL LETTERS, 2013, 24 (04) : 299 - 302
  • [38] Synthesis and Antiviral Activity of Novel 1,4-Pentadien-3-one Derivatives Containing a 1,3,4-Thiadiazole Moiety
    Yu, Lu
    Gan, Xiuhai
    Zhou, Dagui
    He, Fangcheng
    Zeng, Song
    Hu, Deyu
    MOLECULES, 2017, 22 (04):
  • [39] Synthesis and Bioactivities of Novel Galactoside Derivatives Containing 1,3,4-Thiadiazole Moiety
    Shu, Yafei
    Chen, Meihang
    Lu, Daowang
    Zhou, Zengyan
    Yu, Jianhong
    Hu, Xiaoling
    Yang, Jiaqin
    Li, Aiqin
    Liu, Jianglong
    Luo, Hairong
    FRONTIERS IN CHEMISTRY, 2022, 10
  • [40] Synthesis and in vitro antitumor activity of 1,3,4-thiadiazole derivatives based on benzisoselenazolone
    Zhao, Jie
    Chen, Bao Quan
    Shi, Yan Ping
    Liu, Yu Ming
    Zhao, Hai Chuan
    Cheng, Ji
    CHINESE CHEMICAL LETTERS, 2012, 23 (07) : 817 - 819