N-indazole substituted thiourea derivatives and preparation method and application thereof

A technology of derivatives and thioureas, applied in the field of chemical medicine, to achieve the effect of high antiviral activity and good antioxidant activity

Inactive Publication Date: 2016-07-13
XI AN JIAOTONG UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0006] At present, there are few reports on compounds containing both 1H-indazole ring structure and asymmetric thiourea structure

Method used

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  • N-indazole substituted thiourea derivatives and preparation method and application thereof
  • N-indazole substituted thiourea derivatives and preparation method and application thereof
  • N-indazole substituted thiourea derivatives and preparation method and application thereof

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Embodiment Construction

[0053] The present invention will be further described in detail below in conjunction with specific embodiments, which are explanations of the present invention rather than limitations.

[0054] see figure 1 , the present invention takes 2-pyridinecarboxylic acid 1 as raw material, reacts in thionyl chloride to generate intermediate 2 (4-chloropyridine-2-formyl chloride); intermediate 2 reacts with methylamine solution at low temperature, and undergoes hydrogen oxidation Alkalinization of sodium solution generates intermediate 3 (N-methyl-4-chloropyridine-2-carboxamide); intermediate 3 and p-aminophenol 4 react to generate intermediate 5 [4-(4 -aminophenoxy)-N-methyl-2-pyridinecarboxamide]; intermediate 5 reacts to generate N-methyl-4-(4-isosulfur in the presence of carbon disulfide, triethylamine and ferrous sulfate Cyanate (phenoxy)pyridine-2-carboxamide 6. In addition, 2-methylaniline 7 substituted with nitro in different positions is used as starting material, and glacia...

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Abstract

The invention discloses N-indazole substituted thiourea derivatives and a preparation method and application thereof and belongs to the technical field of chemical medicine.The thiourea derivatives are a series of compounds simultaneously containing the 1H-indazole ring structure and the asymmetrical thiourea structure, and the compounds are not reported in the literature.The bioactivity test result analysis of the thiourea derivatives show that the compounds are good in antioxidant activity, the average scavenging rate is above 80%, the scavenging rate of the compound 12b, the compound 12c, and the compound 12d and the compound 12h is higher than 90%, the scavenging activity IC50 of the compound 12h on DPPH is 0.14mg / mL; part of the target compounds has certain inhibition activity on herpes viruses, vaccinia viruses, reoviruses, Coxsackie viruses, Feline coronary herpes viruses, HIV viruses and the like, and the compound 12c and the compound 12n are high in antivirus activity; the synthesized compounds hopefully have new bioactivity which is not expounded, and a certain material basis is provided for the development of new medicine.

Description

technical field [0001] The invention belongs to the technical field of chemistry and medicine, in particular to N-indazole-N'-[4-[2-(N-methylcarbamoyl)-4-pyridyloxy]phenyl]thiourea derivatives And its preparation method and application. Background technique [0002] N-indazole heterocyclic compounds have a wide range of biological activities, such as pain-related TRPA1 receptor and capsaicin receptor (TRPV1) antagonism, neutrophil elastase inhibitory activity related to lung disease, and intestinal stress syndrome Selective serotonin-4-receptor (5-HT4R) inhibitory activity associated with heart failure, B-Raf kinase inhibitory activity, cMet and Hedgehog pathway inhibitory activity related to tumorigenesis and prognosis, inhibitory activity on kinases, It can mediate tyrosine kinase signaling pathways to regulate or inhibit cell proliferation and neovascularization, such as protein kinase Pim inhibitory activity, cyclin-dependent kinase CDK7 and CDK9 inhibitory activity, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P31/18A61P31/22A61P31/16A61P39/06
CPCC07D401/12
Inventor 孟歌杨涛张解和刘洋石娟郑阿群赵桂兰
Owner XI AN JIAOTONG UNIV
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