Derived chromone having an antihypertensive and analepticheskih activity

 

(57) Abstract:

Usage: in medicine as a means of having an antihypertensive and analepticheskih activity. The inventive product 3-(2-benzimidazolyl)-7-acetoxylation. BF C18H11N2O4so pl. 236 - 238oC. LD > 2620 mg/kg dose of 10 mg/kg increases the duration nematalosa sleep until 103,2 2,3 minutes the compound Obtained reduces blood pressure to the original level after 30 11,2 2,7%, through 60 - 1,3 15,8%. Reagent 1: o-phenylenediamine. Reagent 2: 7-acetylcholin-3-aldehyde. Process conditions: boiled at 160 - 170oC for 90 minutes

The invention relates to chemical-pharmaceutical industry, namely to new biologically active substances on the basis of which can be created drugs with hypotensive and analepticheskih activity.

The claimed creation relates to new derivatives of chromone, namely 3-(2-benzimidazolyl)chromones formula

where R SLA with hypotensive and analepticheskih activity.

Here is the application of a derived chromone, its properties and biological activity not described in literature.

The closest structural giving hypotensive and spasmolytic effect, and isoflavones, 3-erichrome with gipoholesterinemicheskoy activity, as well as heteroanalogs of isoflavones, 3-benzimidazolyl - chroman [2]

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The purpose of the invention to provide new derivatives of chromone having an antihypertensive and analepticheskih activity.

The goal has been achieved by the synthesis of compounds of the formula

which is obtained by condensation of o-phenylenediamine with an appropriate substituted chroman 3-aldehyde.

P R I m e R 1. 3-(2-Benzimidazolyl)-7-acetoxy-chrome.

A mixture of o-phenylenediamine hydrochloride, 7-acetylcholin-3-aldehyde are dissolved in 15 ml of nitrobenzene and heated at 160-170aboutC for 90 min, then from the reaction mixture by cooling rolls sludge, which is separated, washed with diethyl ether and dried. From the mother liquor diethyl ether planted some more product.

Yield: 2.15 g (78%), so pl. 236-238aboutC.

Found, From 67.9; H 3,6; 21,9; 8,8.

Calculated From 67,5; N 3,75; 20; 8,75.

IR spectrum (liquid paraffin) 1650 cm-1(C=0)

1600 cm-1(C=C)

1100 cm-1(With-N) Number of state registration 9931190.

Research hypotensive and analepticheskih activity ASS="ptx2">

Research hypotensive activity was performed according to the method of [3] by studying the effects of compounds on systemic arterial pressure in anesthetized albino rats. Of male rats weighing 210-240 g was narcoticyou with Nembutal at a dose of 40 mg/kg animal body. Blood pressure was recorded using a plastic catheter, which was inserted in the abdominal aorta through the femoral artery. The blood pressure was recorded before and after the introduction of compounds 30 and 60 minutes the effect was recorded in interest to the original level. As reference drug for comparison were selected drugs papaverine hydrochloride in a dose of 10 mg/kg, apressin (1 mg/kg) and Dibazol (10 mg/kg), which was injected intraperitoneally.

Saline in the control series, the benchmark in the standard series and test the connection in the experimental series were injected intraperitoneally warmed to 37aboutC. In each series were used for 6 animals. Doses of the standard and test compounds were selected for effect.

The results of the experiments are statistically processed and presented in table.1.

Research analepticheskih activity was conducted on the model nematalosa sleep [4] it is Known that the and intravenous administration leads to respiratory arrest and sudden decrease in blood pressure.

Standard compounds for comparison were chosen caffeine-sodium benzoate and Dibazol, they were administered at a dose of 10 mg/kg intraperitoneally. It is known that caffeine-sodium benzoate belongs to 2 groups: psychotropic and analepticheskih means.

The experiments were conducted on rats-males weighing 200-230 g were Simultaneously put several series of experiments in each series used in 6 animals. The first series of control (intraperitoneally injected with a saline solution); the second series standard (intraperitoneally injected caffeine-sodium benzoate and/or Dibazol 10 mg/kg, third series experienced) intraperitoneally were administered the test substance at a dose of 10 mg/kg

Saline, standard and investigational compound was administered 30 min prior to injection of Nembutal. Doses of the standard and the analyte was chosen for effect. The results of the experiments are processed statistically, as reflected in the table.2.

Derived chromone formula

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having an antihypertensive and analepticheskih activity.

 

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