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P-aminosalicylic acid azole derivatives and preparation method and application thereof

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

Active Publication Date: 2022-07-05
SOUTHWEST UNIV
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  • 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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  • P-aminosalicylic acid azole derivatives and preparation method and application thereof
  • P-aminosalicylic acid azole derivatives and preparation method and application thereof
  • P-aminosalicylic acid azole derivatives and 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 with reference to the embodiments of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without creative efforts shall fall within 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-tetrazole, 5-methyltetrazole, 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...

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Abstract

The invention discloses p-aminosalicylic acid azole derivatives, a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of the p-aminosalicylic acid azole derivatives is as follows. The antibacterial activity assay results show that the p-aminosalicylic acid azole derivatives of the present invention have good overall inhibitory activity against common pathogens, and the antibacterial activity of some molecules against Pichia pastoris is stronger than or equivalent to the positive drug fluconazole , all the molecules have good inhibitory activity against C. citrus anthracnose, some molecules have comparable or stronger inhibitory activity to the positive control prochloraz, and most of the molecules have good inhibitory effect on C. citrus canker. The anti-tumor cell activity assay results show that the p-aminosalicylic acid azole derivatives of the present invention have inhibitory effects on three tumor cells. The p-aminosalicylic acid azole derivatives of the present invention have potential application prospects in the fields of antibacterial, antifungal, anti-citrus pathogen and antitumor.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to p-aminosalicylic acid azole derivatives and a preparation method and application thereof. Background technique [0002] Para-aminosalicylic acid (PAS) is an antibacterial drug used in the treatment of tuberculosis. It is also used to treat inflammatory bowel disease by inhibiting NF-κB and scavenging free radicals. Mainly used to treat tuberculosis. [0003] PAS amino derivatives are divided into three main categories. The first class is the PAS Schiff base derivatives. The research results show that the synthesized target compounds have lower inhibitory concentrations against Mycobacterium smegmatis and Mycobacterium bovis than PAS; pyrazinamide and Schiff base derivatives of PAS, against H. 37 The inhibitory activity of Rv was stronger than that of PZA (MICs were 3.13 and 6 μg / mL, respectively), and there was a sustained release. The second category is PAS hydrazone...

Claims

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Application Information

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Patent Type & Authority Patents(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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