P-aminosalicylic acid fluoroquinolone derivative as well as intermediate, preparation method and application thereof

A technology of fluoroquinolone acid and aminosalicyl, which is applied in the field of drug synthesis, can solve the problems of complex differentiation of citrus canker sore strains, accelerated drug resistance, and high incidence of disease

Active Publication Date: 2021-01-01
SOUTHWEST UNIVERSITY
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  • Abstract
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  • Claims
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Problems solved by technology

The citrus canker fungus has complex differentiation, high incidence, rapid spread, and wide host range. Therefore, the prevention and treatment of citrus disease has always been a worldwide problem. At present, there is no method to cure it.
During production, Bordea...

Method used

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  • P-aminosalicylic acid fluoroquinolone derivative as well as intermediate, preparation method and application thereof
  • P-aminosalicylic acid fluoroquinolone derivative as well as intermediate, preparation method and application thereof
  • P-aminosalicylic acid fluoroquinolone derivative as well as intermediate, preparation method and application thereof

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Embodiment Construction

[0049] 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.

[0050] 1. Main reagents and instruments

[0051] p-aminosalicylic acid, chloroacetyl chloride, dichloromethane, N,N-dimethylformamide, gatifloxacin, clinfloxacin, ciprofloxacin, baloxacin, sarafloxacin, moxifloxacin, Enoxacin (>95%); norfloxacin, ofloxacin, lomefloxacin, concentrated sulfuric acid, methanol, sodium bicarbonate, potassium carbonate, absolute ethanol (AR); the remaining reagents are commercially pure Or analyze the pure product.

[0052] NMR (AV-600, 600MHz, T...

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Abstract

The invention discloses a p-aminosalicylic acid fluoroquinolone derivative and an intermediate, a preparation method and application thereof, and belongs to the technical field of drug synthesis. Thestructural formula of the p-aminosalicylic acid fluoroquinolone derivative is shown in the specification. In-vitro activity determination results show that part of fluoroquinolone aminosalicylate derivatives (compounds for short) and intermediates have inhibition effects on mycobacterium smegmatis; the compounds and intermediates have good inhibition activity on common pathogenic bacteria as a whole; most compounds and intermediates have better antibacterial activity on pichia pastoris as a whole; part of the compounds have good inhibitory activity on citrus canker pathogens. The p-aminosalicylic acid fluoroquinolone derivative and the intermediate thereof have potential application prospects in the fields of tuberculosis resistance, bacteria resistance, fungus resistance and citrus pathogen resistance.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to p-aminosalicylic acid fluoroquinolone derivatives and intermediates, preparation methods and applications thereof. Background technique [0002] Para-aminosalicylic acid (PAS), which has long been used in the treatment of tuberculosis, has also been used in the treatment of inflammatory bowel disease. PAS amino derivatives can be divided into three categories. The first category is PAS Schiff base derivatives. The results of the study show that the synthesized target compound has 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, respectively). The second category is PAS hydrazone derivatives. Isoniazid (INH) and PAS were reacted to prepare compounds containing hydrazone groups. The experimental results showed that the average ratio of th...

Claims

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Application Information

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IPC IPC(8): C07D215/56C07D401/04C07D471/04C07C229/64A61P31/04A61P31/10A61P31/06A01N43/90A01N43/60A01P3/00
CPCC07D215/56C07D401/04C07D471/04C07C229/64A61P31/04A61P31/10A61P31/06A01N43/90A01N43/60
Inventor 杨大成任艳会范莉潘建芳唐雪梅谢建平胡军华周围徐兴然许峻旗吴玉珠李洋岳琪佳孙青羽
Owner SOUTHWEST UNIVERSITY
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