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Para-aminosalicylic acid azole derivative as well as preparation method and application thereof

A technology of aminosalicylic acid azoles and derivatives, applied in the field of drug synthesis, can solve problems such as no biological activity, and achieve the effect of good antibacterial activity

Active Publication Date: 2020-12-04
SOUTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are no reports on the derivatives linked to PAS and azoles and their biological activities

Method used

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  • Para-aminosalicylic acid azole derivative as well as preparation method and application thereof
  • Para-aminosalicylic acid azole derivative as well as preparation method and application thereof
  • Para-aminosalicylic acid azole derivative as well as preparation method and application thereof

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Embodiment Construction

[0047] The technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Obviously, the described embodiments are only some of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0048] 1. Main reagents and instruments

[0049] p-aminosalicylic acid, chloroacetyl chloride, dichloromethane, N,N-dimethylformamide, imidazole, 2-methylimidazole, 4-methylimidazole, pyrazole, benzimidazole, 1,2,4 -Triazole, 2,4-dimethylpyrazole, 1H-tetrazolium, 5-methyltetrazolium, 4,6-dimethyl-2-mercaptopyrimidine, 1-methyl-5-mercapto Tetrazolium, 1-phenyl-5-mercaptotetrazolium, 2-mercapto-5-methyl-1,3,4-thiadiazole; concentrated sulfuric acid, methanol, sodium bicarbonate...

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Abstract

The invention discloses a para-aminosalicylic acid azole derivative as well as a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of the para-aminosalicylic acid azole derivative is shown in the specifications. An antibacterial activity determination result shows that the para-aminosalicylic acid azole derivative disclosed bythe invention has good inhibition activity on common pathogenic bacteria as a whole, and the antibacterial activity of part of molecules on pichia pastoris is stronger than or equal to that of a positive drug, fluconazole; all the molecules have good inhibitory activity on colletotrichum gloeosporioides, part of the molecules have the inhibitory activity equal to or higher than that of positive control prochloraz, and most of the molecules have a good inhibitory effect on citrus canker pathogens. An anti-tumor cell activity determination result shows that the para-aminosalicylic acid azole derivative disclosed by the invention has an inhibition effect on the three kinds of tumor cells. The para-aminosalicylic acid azole derivative disclosed by the invention has a potential application prospect in the fields of bacterium resistance, fungus resistance, citrus pathogen resistance and tumor resistance.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to p-aminosalicylic acid azole derivatives and their preparation methods and applications. Background technique [0002] Para-aminosalicylic acid (PAS) is an antibacterial drug used to treat tuberculosis. It is also used to treat inflammatory bowel disease by inhibiting NF-κB and scavenging free radicals. Mainly used in the treatment of tuberculosis. [0003] PAS amino derivatives are divided into three categories. The first category is PAS Schiff base derivatives. The results of the study showed that the synthesized target compounds had lower inhibitory concentrations to Mycobacterium smegmatis and Mycobacterium bovis than PAS; 37 The inhibitory activity of Rv was stronger than that of PZA (MICs were 3.13 and 6 μg / mL), and there was a sustained release. The second category is PAS hydrazone derivatives, reacting INH with PAS to prepare compounds containing hydrazone grou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/56C07D235/06C07D231/12C07D249/08C07D257/04C07D239/38C07D285/125C07D285/135C07D263/58C07D277/74A61P31/04A61P31/10A61P35/00A01N43/50A01N43/56A01N43/52A01N43/653A01N43/713A01N43/54A01N43/824A01N43/76A01N43/78A01P3/00A01P1/00
CPCC07D233/56C07D235/06C07D231/12C07D249/08C07D257/04C07D239/38C07D285/125C07D285/135C07D263/58C07D277/74A61P31/04A61P31/10A61P35/00A01N43/50A01N43/56A01N43/52A01N43/653A01N43/713A01N43/54A01N43/82A01N43/76A01N43/78Y02A50/30
Inventor 杨大成潘建芳范莉唐雪梅任艳会徐兴然胡军华周围徐志刚吴玉珠李洋韩海燕
Owner SOUTHWEST UNIV
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