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含取代吡啶基的新型吡唑肟化合物的设计、合成及生物活性

Design, Synthesis, and Biological Activities of Novel Pyrazole Oxime Compounds Containing a Substituted Pyridyl Moiety.

作者信息

Chen Cuili, Chen Jia, Gu Haiying, Bao Ning, Dai Hong

机构信息

College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, China.

School of Public Health, Nantong University, Nantong 226019, China.

出版信息

Molecules. 2017 May 25;22(6):878. doi: 10.3390/molecules22060878.

DOI:10.3390/molecules22060878
PMID:28587083
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6152754/
Abstract

In this paper, in order to find novel biologically active pyrazole oximes, a series of pyrazole oxime compounds bearing a substituted pyridyl unit were prepared. Bioassays showed that some target compounds were found to have good acaricidal activity against at a concentration of 500 μg/mL, compound especially displayed potent acaricidal activity against when the concentration was reduced to 100 μg/mL. Interestingly, most target compounds possessed excellent insecticidal activities against at 500 μg/mL. Moreover, some compounds were active against and at 500 μg/mL. Additionally, compounds , , , , , , , , , and displayed significant antiproliferative activities against HepG2 cells with IC values of 1.53-17.27 μM, better than that of the control 5-fluorouracil (IC = 35.67 μM).

摘要

在本文中，为了寻找新型生物活性吡唑肟，制备了一系列带有取代吡啶基单元的吡唑肟化合物。生物活性测试表明，一些目标化合物在浓度为500μg/mL时对[具体螨类名称未给出]具有良好的杀螨活性，尤其是化合物[具体化合物名称未给出]，当浓度降至100μg/mL时，对[具体螨类名称未给出]表现出强效杀螨活性。有趣的是，大多数目标化合物在500μg/mL时对[具体昆虫名称未给出]具有优异的杀虫活性。此外，一些化合物在500μg/mL时对[具体生物名称未给出]和[具体生物名称未给出]具有活性。另外，化合物[具体化合物名称未给出]对HepG2细胞表现出显著的抗增殖活性，IC值为1.53 - 17.27μM，优于对照5-氟尿嘧啶（IC = 35.67μM）。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57f6/6152754/0d80ad5dbdb0/molecules-22-00878-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57f6/6152754/afb14fa5e5d3/molecules-22-00878-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57f6/6152754/8edcce662066/molecules-22-00878-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57f6/6152754/0d80ad5dbdb0/molecules-22-00878-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57f6/6152754/afb14fa5e5d3/molecules-22-00878-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57f6/6152754/8edcce662066/molecules-22-00878-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/57f6/6152754/0d80ad5dbdb0/molecules-22-00878-sch001.jpg

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本文引用的文献

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Synthesis and bioactivities of novel pyrazole oxime derivatives containing a 1,2,3-thiadiazole moiety.含1,2,3-噻二唑部分的新型吡唑肟衍生物的合成及生物活性
Bioorg Med Chem Lett. 2016 Sep 15;26(18):4504-4507. doi: 10.1016/j.bmcl.2016.07.068. Epub 2016 Jul 29.
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Synthesis and Bioactivities of Novel Pyrazole Oxime Derivatives Containing a 5-Trifluoromethylpyridyl Moiety.
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Molecules. 2016 Feb 27;21(3):276. doi: 10.3390/molecules21030276.
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Microwave assistant synthesis, antifungal activity and DFT theoretical study of some novel 1,2,4-triazole derivatives containing pyridine moiety.微波辅助合成、含吡啶基的新型 1,2,4-三唑衍生物的抑菌活性及 DFT 理论研究。
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Benzylidene 2-aminoimidazolones derivatives: synthesis and in vitro evaluation of anti-tumor carcinoma activity.亚苄基-2-氨基咪唑酮衍生物：合成及其抗肿瘤活性的体外评价
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