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Application of thiazolopyranone analogues in preparation of anti-inflammatory medicines

A technology of anti-inflammatory drugs and analogs, applied in the directions of anti-inflammatory agents, drug combinations, antipyretics, etc., can solve the problems of inability to increase polar excretion, lack of fatty chains, and difficult to metabolize, and achieve the effect of significant anti-inflammatory activity

Active Publication Date: 2019-04-26
LANZHOU UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the polycyclic conjugated structure of such drugs is often difficult to metabolize due to the lack of fatty chains, that is, the first-phase biotransformation process requires excessive oxidation to generate a large amount of reactive oxygen species (ROS), or consumes excess glutathione to produce toxicity
In addition, the multi-conjugated ring structure of existing NSAIDs drugs may make them unable to effectively excrete through the second phase biotransformation to increase polarity, so that they accumulate in the body and exhibit toxicity

Method used

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  • Application of thiazolopyranone analogues in preparation of anti-inflammatory medicines
  • Application of thiazolopyranone analogues in preparation of anti-inflammatory medicines
  • Application of thiazolopyranone analogues in preparation of anti-inflammatory medicines

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Embodiment Construction

[0037] The synthesis and anti-inflammatory activity of the thiazolopyrone analogs of the present invention will be described in detail below in conjunction with specific examples. It should be understood that these examples are used to illustrate the present invention and not to limit the scope of the present invention.

[0038] 1. Structure and synthesis of thiazolopyrone analogs

[0039] In Examples 1-23, the structures of thiazolopyrone analogues are as follows:

[0040]

[0041] According to different configurations, the synthesis method of the above-mentioned chiral thiazolopyrone analogs can be selected, and according to different compounds, attention should be paid to the selection of the corresponding 5-enthiazolone substrate during the synthesis process. In Examples 1-23, the configurations and NMR characterizations of the thiazolopyrone analogs are shown in Table 1.

[0042]Table 1 Configuration and NMR characterization of thiazolopyrone analogues in Examples 1-...

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Abstract

The invention provides new medical application of thiazolopyranone analogues, in particular relates to application of the thiazolopyranone analogues in preparation of anti-inflammatory medicines. Theinflammation is aseptic inflammation. A general structural formula of the thiazolopyranone analogues is described in the description; the thiazolopyranone analogues are free from significant cytotoxicity and can effectively inhibit the release of nitric oxide from macrophage RAW264.7 induced by LPS; an experiment for detecting nitric oxide (NO) release by using a Griess method, an ELISA assay of PGE2, a Western Blot experiment and Xylene-induced mouse ear swelling experiments prove that the thiazolopyranone analogues can inhibit the production of NO and PGE2, and reduces the expression of iNOSand COX-2 by inhibiting MAPK (ERK, JNK and p38) signaling pathways. Therefore, the thiazolopyranone compounds can be used as active substances for the preparation of the anti-inflammatory medicines.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry and relates to the application of thiazolopyrone analogs in the preparation of anti-inflammatory drugs. Background technique [0002] Inflammation is a basic pathological process that the body produces in response to the damage of inflammatory factors, mainly in the defense response. Prostaglandins (PGs) and leukotrienes (LTs) are the most important inflammatory mediators produced by the metabolism of arachidonic acid (AA) in inflammation-related processes, involved in rheumatism, rheumatoid arthritis, pain, asthma, atherosclerosis Occurrence and treatment of sclerosis, stroke, Alzheimer's disease, cancer and other indications. In the metabolic network of AA, cyclooxygenase (COX) is the key enzyme for the release of prostaglandin PG, among which cyclooxygenase-1 (COX-1) is closely related to the synthesis of physiological PGs, and COX-2 is mostly induced , is associated with the gene...

Claims

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Application Information

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IPC IPC(8): A61K31/429A61P29/00A61P1/16
CPCA61K31/429A61P1/16A61P29/00
Inventor 王锐林利田婷李太晗
Owner LANZHOU UNIVERSITY
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