Application of compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and pharmaceutically acceptable salt thereof in preparing non-steroidal anti-inflammatory and analgesic medicines

A benzenesulfonyloxybenzoxazolone, non-steroidal anti-inflammatory technology, applied in the field of new compound uses, can solve the problem of no relevant reports on the pharmacological effect of anti-inflammatory and analgesic activity, and achieve the effect of low price

Inactive Publication Date: 2012-01-11
SHANXI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no relevant report on the anti-inflammatory and analgesic activity pharmacological effects of compound 4-o-toluenesulfonyloxybenzoxazolone and its pharmaceutically acceptable salts at home and abroad.

Method used

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  • Application of compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and pharmaceutically acceptable salt thereof in preparing non-steroidal anti-inflammatory and analgesic medicines
  • Application of compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and pharmaceutically acceptable salt thereof in preparing non-steroidal anti-inflammatory and analgesic medicines
  • Application of compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and pharmaceutically acceptable salt thereof in preparing non-steroidal anti-inflammatory and analgesic medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] 1. Effect of compound MBB on pain threshold of hot plate in mice

[0015] 1.1 Experimental steps:

[0016] Kunming mice were placed in a water bath with a water temperature of 55°C, and the mice kicked or licked due to heat stimulation.

[0017] Response to rear foot or limb movement, which is used as an indicator of pain response. Select 48 female mice (choose the mouse that licks the feet within 5 seconds and 30 seconds on the hot plate, and the unqualified ones are eliminated), and they are randomly divided into 4 groups, 12 in each group, which are respectively physiological saline control group, the invention The compound MBB administration group (suspension prepared with 0.5% sodium carboxymethylcellulose) and the positive control group (chlorzoxazone) were intragastrically administered to rats (see Table 1 for intragastric administration dosage). Afterwards, the time from when the mouse was placed on the hot metal plate to when the pain response occurred was re...

Embodiment 2

[0032] 1. The effect of compound MBB on the writhing response of mice induced by acetic acid

[0033] 1.1 Experimental steps:

[0034] Kunming strain mice, weighing 20±2g, were randomly divided into normal saline control group, MBB administration group of the compound of the present invention and positive control group (chlorzoxazone). Each group was intragastrically administered once a day (see Table 3 for intragastric administration dosage) for 3 consecutive days. One hour after the last administration, each mouse was intraperitoneally injected with 0.2ml of 0.6% acetic acid, and then observed the torsion caused by acetic acid within 15 minutes. Body times.

[0035] 1.2 Calculation and statistical analysis of experimental results (Table 3):

[0036] Inhibition rate (%) = (writhing times of blank control group - writhing times of drug administration group) / writhing times of blank control group × 100%.

[0037] Table 3 The effect of compound MBB on the number of times of ...

Embodiment 3

[0085] 1. Effect of compound MBB on carrageenan-induced toe swelling in rats

[0086] 1.1 Experimental steps:

[0087] Take 40 rats, half male and half female, weighing 160-180g, and randomly divide them into five groups according to body weight, 8 rats in each group, respectively: solvent control group (i.e. model group); MBB effect group (including three doses) and Positive control group (chlorzoxazone). Rats in each group were given 0.5% sodium carboxymethylcellulose, compound MBB and positive drug every day. The animals were gavaged once a day (see Table 9 for the gavage dose) for 3 consecutive days. One hour after the last administration, the diameter of the normal toe of the left hind limb of the rats in each group was accurately measured with a vernier caliper. Make a mark around the ankle joint of the hindlimb, and then subcutaneously inject 0.15ml of 1% carrageen suspension in the toes of the left hindlimb of the rat to cause inflammation. Subsequently, eve...

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Abstract

The invention discloses medicinal usage of the compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and pharmaceutically acceptable salts thereof, specifically application of the compound and the pharmaceutically acceptable salts thereof in preparing non-steroidal anti-inflammatory and analgesic medicines. According to analgesic and anti-inflammatory tests on mice, after normal administration, the mice have obviously enhanced ability in fighting pain; compared to similar medicines, the compound and the pharmaceutically acceptable salts thereof have a more obvious analgesic effect, have a good inhibition effect on inflammation reactions of animals caused by various factors, and have hypotoxicity according to results of toxicity tests. In a word, the compound 4-o-methyl-benzenesulfonyl-2(3H)-benzoxazolone and the pharmaceutically acceptable salts thereof have the characteristics of good anti-inflammatory and analgesic activity and hypotoxicity, can be industrially synthesized, are cheap, and can be used individually or jointly with other pharmaceutically acceptable pharmaceutic adjuvants to prepare non-steroidal anti-inflammatory and analgesic medicines, thereby providing a novel means and method for clinical treatment of diseases caused by inflammatory pains and opening up a new direction for clinical administration.

Description

technical field [0001] The invention belongs to the field of completely new compound applications, and specifically relates to the application of the compound 4-o-toluenesulfonyloxybenzoxazolone and its pharmaceutically acceptable salts in the preparation of non-steroidal anti-inflammatory and analgesic drugs. Background technique [0002] The research on non-steroidal anti-inflammatory analgesic drugs is a research hotspot in the field of drug research. These drugs have anti-inflammatory, anti-rheumatic, analgesic, antipyretic and anti-coagulant effects, and are widely used clinically for osteoarthritis, Relief of rheumatoid arthritis, multiple fevers, and various pain symptoms. There are many kinds of non-steroidal anti-inflammatory analgesic drugs, mainly divided into six categories: pyrazolidinedione, anthranilic acid, aryl alkanoic acid, aryl propionic acid, 1,2-benzothiazine (Oxicam class) and other classes (mainly including COX-2 inhibitors). Most of these drugs hav...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/423A61P29/00
Inventor 李青山唐莉马云龙梁泰刚韩玲革
Owner SHANXI MEDICAL UNIV
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