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Hypotensively active compound and preparation method thereof

A compound and high blood pressure technology, applied in the field of antihypertensive compounds and their preparation, can solve problems affecting the selection of antihypertensive drugs, and achieve the effect of good development and application prospects and wide application

Inactive Publication Date: 2016-05-25
青岛友诚高新技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In actual clinical use, the patient's cardiovascular risk factors, target organ damage, complications, complications, antihypertensive efficacy, adverse reactions, etc. will all affect the choice of antihypertensive drugs

Method used

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  • Hypotensively active compound and preparation method thereof
  • Hypotensively active compound and preparation method thereof
  • Hypotensively active compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Dissolve 4.47g (15mmol) of compound A in 50mL of toluene in a 100mL round bottom flask, then add 2mmol DMF and 20mmol benzoyl chloride, and then react while stirring at 40°C for 2 hours. Then add 100mL toluene, wash with distilled water 100mL×3 times, dry over anhydrous sodium sulfate, concentrate the organic phase under reduced pressure, and finally use silica gel column chromatography for purification, the eluent is petroleum ether / ethyl acetate=2:1, Obtain oily compound B, ESI-MS, m / e=402.11 ([M+NH 4 ] + ).

[0025] Dissolve 15mmol of compound B in 50mL of toluene, then add 20mmol of triethylamine, then add 20mmol of thionyl chloride dropwise at 10°C under the protection of nitrogen, stir while adding, naturally rise to room temperature after 20 minutes, and continue to stir for 0.5 Hour. The reaction solution was washed with saturated brine 100mL×3 times, dried over anhydrous sodium sulfate, and the organic phase was concentrated under reduced pressure, and final...

Embodiment 2

[0032] The maximum tolerance test of the formula I compound of the present invention:

[0033] Get 40 mice with a body weight of 20 ± 2g, half male and half male, orally administered at 0.8mg / 20g such as a suspension with a concentration of 100mg / ml of the compound of formula I, and continuously observe the death of the animal within 30 days. As a result, within 30 days , all animals had normal feeding activity, no deaths, no LD detected 50 , considered non-toxic.

Embodiment 3

[0035] The test of the pharmacological activity of the compound described in formula I of the present invention:

[0036] 1. Radioimmunoassay of cGMP:

[0037] Take 40 healthy Wistar rats with a body weight of 180-220g, half male and half male, and divide them into two groups at random. , to detect the normal value of rat cGMP and the cGMP of myocardial tissue, the results are as follows: see Table 1.

[0038] Table 1 is as the impact of formula I compound on blood plasma and myocardial cGMP

[0039]

[0040]

[0041] Compared with the control group, P<0.001.

[0042] 2. Acute antihypertensive effect

[0043] 45 healthy Wistar rats, both male and female, weighing 180-220 g, were randomly divided into three groups (15 rats / group). The first group: intraperitoneal injection of normal saline; the second group: intraperitoneal injection of the compound of formula I; the third group: intraperitoneal injection of nitroglycerin as a positive control. 500μg / kg was used in e...

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PUM

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Abstract

The invention discloses a hypotensively active compound as well as a preparation method and application thereof. Pharmacological experiments show that the compound according to formula I has hypotensive activity, is useful in treating cardiovascular diseases and is basically free of effects upon various human organics. Therefore, the compound of the invention is useful in the preparation of hypotensive drugs, has a promising development and application prospect and is widely applicable to clinical and medical researches.

Description

technical field [0001] The invention relates to the field of drugs related to hypertension. In particular, the present invention relates to compounds with hypotensive activity and methods for their preparation. Background technique [0002] Hypertension is a chronic disease characterized by continuous elevation of arterial blood pressure, which often causes lesions in heart, brain, kidney and other important organs with corresponding consequences. The blood pressure of a normal person fluctuates within a certain range with changes in the internal and external environment. In the whole population, the blood pressure level gradually increases with age, especially the systolic blood pressure, but the diastolic blood pressure shows a downward trend after the age of 50, and the pulse pressure also increases accordingly. In recent years, people have deepened their understanding of the role of multiple risk factors for cardiovascular disease and the protection of heart, brain, an...

Claims

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Application Information

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IPC IPC(8): C07C235/34C07C231/02A61K31/24A61P9/12
CPCC07C235/34C07C67/14C07C67/287C07C231/02
Inventor 不公告发明人
Owner 青岛友诚高新技术有限公司
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