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Guava dialdehyde heterosource terpene piperazinyl and tetrazolium derivative composition for preparing anti-rhinitis drug

A composition and technology for rhinitis, which are applied in directions such as drug combinations, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve problems such as poor curative effect and ineffectiveness of rhinitis, and achieve good anti-rhinitis effect.

Inactive Publication Date: 2018-06-08
CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, antihistamine drugs such as terfenadine or antiallergic drugs such as tranilast and ketotifen are mainly used in the treatment of rhinitis. These drugs have poor or ineffective effects on chronicity and recurrent rhinitis

Method used

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  • Guava dialdehyde heterosource terpene piperazinyl and tetrazolium derivative composition for preparing anti-rhinitis drug
  • Guava dialdehyde heterosource terpene piperazinyl and tetrazolium derivative composition for preparing anti-rhinitis drug
  • Guava dialdehyde heterosource terpene piperazinyl and tetrazolium derivative composition for preparing anti-rhinitis drug

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Experimental program
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Effect test

Embodiment 1

[0012] Embodiment 1 A kind of preparation of guava dialdehyde heteroterpene

[0013] A preparation method of guava dialdehyde heteroterpenoids (I) refers to the literature published by Meng Shao et al. (MengShao et al., 2010. 12 (2010) 5040–5043) method.

[0014]

Embodiment 2

[0015] Embodiment 2 Synthesis of O-bromoethyl derivative (II) of a guava dialdehyde heteroterpene

[0016] Compound I (474 ​​mg, 1.00 mmol) was dissolved in 20 mL of benzene, tetrabutylammonium bromide (TBAB) (0.16 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 12 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine three times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (5...

Embodiment 3

[0021] Embodiment 3 Synthesis of O-(piperazinyl) ethyl derivative (III) of guava dialdehyde heteroterpene

[0022] Compound II (344mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 4h. After the reaction, the reaction solution was poured into ice water, extracted three times with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of compound ...

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Abstract

The invention discloses a guava dialdehyde heterosource terpene piperazinyl and tetrazolium derivative composition for preparing an anti-rhinitis drug and relates to the field of organic synthesis andpharmaceutical chemistry, in particular to a piperazinyl and 1H-Tetraazole derivative composition of guava dialdehyde heterosource terpene as well as a preparation method and application thereof to the preparation of an anti-rhinitis drug. The invention discloses a piperazinyl and 1H-Tetraazole derivative composition of guava dialdehyde heterosource terpene and a preparation method thereof. Pharmacological experiments show that the piperazinyl and 1H-Tetraazole derivative composition of the guava dialdehyde heterosource terpene has an anti-rhinitis effect and has the value of developing the anti-rhinitis drug.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Rhinitis is a common and frequently-occurring disease in clinical practice. The occurrence of rhinitis is mainly related to allergic reactions and belongs to the category of immune inflammation. At present, antihistamine drugs such as terfenadine or antiallergic drugs such as tranilast and ketotifen are mainly used for the treatment of rhinitis, and these drugs have poor or ineffective effects on chronicity and recurrent rhinitis. Therefore, small molecular compounds with clear components, quality control, safety and high efficiency have potential value in the development of drugs for rhinitis treatment. [0003] It is most important to find compounds or lead compounds from natural products and obtain their derivatives through structural modification, so as to o...

Claims

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Application Information

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IPC IPC(8): C07D313/06C07D405/14A61K31/496A61K31/41A61P11/02A61P37/08
CPCC07D313/06A61K31/41A61K31/496C07D405/14A61K2300/00
Inventor 华子春李媛媛
Owner CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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