JOURNAL OF HETEROCYCLIC CHEMISTRY
·
2017
·Vol. 55
·期 1
·351-359
·
IF 0.893
Xiong-Wei Liu,Jun Yang,Guan-Lian Wang,Yi Gong,Ting-Ting Feng,Xiong-Li Liu,Yu Cao,Ying Zhou,Wei-Cheng Yuan
Described herein is a facile and efficient methodology toward the synthesis of novel convolutamydine A-incorporated β -ionone scaffold 3 from an Aldol addition event of β -ionone to isatins via enamine Et 2 NH catalysis. Products featuring a quaternary carbon center were smoothly obtained in good yields (up to 96% yield). This protocol also represents the first construction of ionone skeleton-fused oxindole molecules, thus leading to new knowledge in the fields of both molecular complexity and diversity-oriented synthesis and the lead compound discovery. Furthermore, their biological activities against human leukemia cells K562 have been preliminarily demonstrated by in vitro assays. The results demonstrated that most of these compounds obtained by this protocol showed comparable with or even much better than the positive control of Cisplatin.
研究领域:
有机化学
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药物化学
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
RUSSIAN JOURNAL OF GENERAL CHEMISTRY
·
2025
·Vol. 95
·期 3
·644-653
·
IF 0.8
Wang J.,Zhou Y.,Wu X.,Zhou X.,Sun Y.,Wu W.,Wang X.
Discovering super-efficient herbicides with novel structures is one of the effective ways to solve the increasingly severe weed resistance problem and meet ecological requirements. In this work, a series of novel bromo- p -hydroxybenzamides were designed based on the molecular hybridization strategy, and rapidly synthesized by one-step amidation reaction, and then characterized by 1 H NMR, 13 C NMR and HRMS. The herbicidal activity assay indicated that most of the target compounds exhibited good-to-excellent inhibition effects on seed germination of two model plants. At a concentration of 100 mg/L, the inhibition rate of 3,5-dibromo- N -(4-bromo-3-chlorophenyl)- p -hydroxybenzamide reached up to 98 and 96% on the roots and stalks of the monocotyledonous barnyard grass ( E. crus-galli ), respectively. 3,5-Dibromo- N -(2-bromophenyl)- p -hydroxybenzamide showed excellent inhibitory activity on the roots and stalks of dicotyledonous rape ( B. napus ) at 100 mg/L, with an inhibitory rate of more than 90%. Furthermore, the concentration was reduced to 1 mg/L, the inhibitory rate of 3,5-dibromo- N -(2-bromophenyl)- p -hydroxybenzamide on the roots of B. napus was still as high as 90%. This work provides a novel molecular scaffold for the development and research of new super-efficient herbicides.
研究领域:
农药化学
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植物生理学
✓ 已验证
DOI
高影响因子
Food Chemistry-X
·
2024
·
IF 6.5
Min He,Jinfeng Zhang,Na Li,Lu Chen,Yan He,Zhiyun Peng,Guangcheng Wang
Thirteen kojic acid-coumarin derivatives were synthesized using the principle of molecular hybridization, and their structures were characterized by 1 H NMR, 13 C NMR, and HRMS. In vitro enzyme inhibition experiments showed that all newly synthesized derivatives have excellent inhibition of tyrosinase (TYR) activity. As a mixed inhibitor, compound 6f has the strongest activity, with an IC 50 value of 0.88 ± 0.10 µM. Multispectral experiments have confirmed that the mode of action of compound 6f on TYR was static quenching. In addition, compound 6f formed a new complex with TYR, which increased the hydrophobicity of the enzyme microenvironment, reduced the content of the α-helix in the enzyme, and changed the secondary structure. The experimental results showed that compound 6f effectively inhibited the browning of lotus root slices and had low cytotoxicity. Therefore, compound 6f is believed to have great development potential as a TYR inhibitor in the food industry.
研究领域:
食品科学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MICROBIOLOGICAL METHODS
·
2025
·
IF 1.9
Juan Du,Ziqi Huang,Zongshuang Li,Limin Wang,Quanfeng Zhang,Yurui Dai,Yanhong Bai
Total bacterial counts (TBC) and coliforms bacteria have been used as the index of microbial quality and fecal contamination for foods, the detection of them is involved in microbiological criteria of most countries to guarantee food safety. In this study, a gold nanoparticle (AuNPs) based colorimetric assay for rapid detection of TBC and coliform bacteria was developed by using the molecular hybridization approach. Thiol modified primers SH-27F and SH- lacZ F were designed and conjugated with AuNPs, which was acted as both hybridization probe and signal probe, and salt induced aggregation of AuNPs was indicator of the hybridization and detection. Escherichia coli was studied as model strain in this study. The result showed that under the optimal conditions, the limit of detection for TBC and coliforms bacteria were 10 2 CFU/mL and 10 1 CFU/mL by visual detection, and 10 1 CFU/mL by UV–vis spectrum analysis, a smart phone application named ColorPicker was used for the quantitative analysis of the colorimetric assay. The colour signal had good linear relationship of E. coli concentration in the range of 10 1 –10 4 CFU/mL. The detection is rapid, simple and sensitive, without the needing of culture enrichment and precious equipment, has good application potential for the on-site detection of TBC and coliforms bacteria. In addition, the proposed strategy provides a direction for the design of highly sensitive colorimetric signal probes for other pathogenic microorganisms.
研究领域:
微生物学
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食品安全
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生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）