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Application of N-[2-[3-(1-piperazine methyl) imidazo [2, 1-B] thiazole-6-yl] phenyl]-2-quinoxaline formamide in preparation of medicament for prevention and treatment of high blood pressure

A kind of technology of quinoxaline carboxamide and methyl group, applied in N-[2-[3-(1-piperazinylmethyl) imidazo[2,1-B]thiazol-6-yl]phenyl The application field of ]-2-quinoxalinecarboxamide in the preparation of drugs for preventing and treating hypertension can solve the problem of no research report on the therapeutic effect of hypertension, and achieve the purpose of reducing the blood pressure of the tail artery of rats, reducing the pulse wave speed, and preventing and treating hypertension. Effect

Inactive Publication Date: 2013-04-10
NANJING CHILDRENS HOSPITAL AFFILIATED TO NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] It has been reported in the literature that N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxaline carboxamide can enhance skeletal muscle, The oxidative metabolic process in the liver and brown adipose tissue and promotes its fat consumption can be used to treat obesity, type 2 diabetes and insulin resistance under high-fat diet, but its therapeutic effect on hypertension has not been reported

Method used

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  • Application of N-[2-[3-(1-piperazine methyl) imidazo [2, 1-B] thiazole-6-yl] phenyl]-2-quinoxaline formamide in preparation of medicament for prevention and treatment of high blood pressure
  • Application of N-[2-[3-(1-piperazine methyl) imidazo [2, 1-B] thiazole-6-yl] phenyl]-2-quinoxaline formamide in preparation of medicament for prevention and treatment of high blood pressure
  • Application of N-[2-[3-(1-piperazine methyl) imidazo [2, 1-B] thiazole-6-yl] phenyl]-2-quinoxaline formamide in preparation of medicament for prevention and treatment of high blood pressure

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Embodiment 1

[0019] Example 1: Acetic acid removal by N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide Antihypertensive effect of oxycorticosterone-salt in hypertensive rats

[0020] 1. Experimental method

[0021] 1. Animal model preparation and experimental grouping: establishment and grouping of animal models: 13-week-old SD rats (220-250g), anesthetized by intraperitoneal injection of pentobarbital (40mg / Kg BW), median abdominal incision, separation and ligation of the left After the lateral renal artery, renal vein and ureter were removed, left nephrectomy was performed, and the abdominal cavity was closed layer by layer, and the postoperative recovery was 1 week. In the experiment, 23 surviving rats after left nephrectomy were randomly divided into 3 groups, control group (n=7): drinking tap water; model group (n=8) and N-[2-[3-(1-piperidine) Azinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide (SRT1720) treatment group (n...

Embodiment 2

[0043] Example 2 N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide for high spontaneity Antihypertensive effect in blood pressure rats

[0044] 1. Experimental method

[0045] 1. Grouping of experimental animals: 16 male spontaneously hypertensive rats (SHR) (16 weeks old, body weight 280-320 g) were randomly divided into 2 groups with 8 rats in each group, namely SHR control group and N-[2 -[3-(1-Piperazinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide treatment group. Eight healthy male Wistar-Kyoto (WKY) rats of the same age and weight were used as the normotensive control group. The N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide treatment group was given 100 mg·Kg -1 ·d -1 , gavage, SHR control group and WKY normotensive control group were given the same amount of distilled water by gavage at the same time every day, once a day, for 8 consecutive weeks.

[0046] 2. Me...

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Abstract

The invention discloses an application of N-[2-[3-(1- piperazine methyl) imidazo [2, 1-B] thiazole-6-base] phenyl]-2-quinoxaline formamide in preparation of a medicament for prevention and treatment of high blood pressure. The experiment research proves that the N-[2-[3-(1- piperazine methyl) imidazo [2, 1-B] thiazole-6-yl] phenyl]-2-quinoxaline formamide can greatly reduce the tail arterial blood pressure, central aortic systolic blood pressure, central aortic diastolic blood pressure, center average arterial pressure and pulse wave velocity of hypertension rats, can improve the artery elastic function, and can reduce the middle thickness of aorta and the vessel wall collagen fiber, increases the blood vessel diameter, and has a favorable effect of prevention and treatment of high blood pressure; and even no significant adverse reactions appear in the experiment process, the medicament is expected to be developed into a new generation safe and effective medicament for prevention and treatment of high blood pressure.

Description

technical field [0001] The present invention relates to N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide compounds, in particular to N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-B]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide in the preparation of drugs for preventing and treating hypertension of new clinical uses. Background technique [0002] Hypertension is the most common chronic disease and has become a major public health problem worldwide. According to a study by WHO in 2004, the number of deaths caused by hypertension worldwide is 7.5 million every year, and the loss of disability-adjusted life years caused by hypertension ranks fifth. In the past few decades, the prevalence of hypertension in my country has been increasing rapidly, especially since the reform and opening up, with the changes in people's lifestyles and the acceleration of the aging process, the prevalence of hypertension has accelerated. The estimated number of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/498A61P9/12
Inventor 张爱华黄松明
Owner NANJING CHILDRENS HOSPITAL AFFILIATED TO NANJING MEDICAL UNIV
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