Rhynchophylline analog and its application in the preparation of antihypertensive drugs
A technology for anti-hypertension and high blood pressure, which is applied to the structure of rhynchophylline analogues of the extract of Uncaria uncaria in traditional Chinese medicine, and the preparation of anti-hypertensive drugs. It can solve the problems of low safety and speed up, and achieve significant anti-hypertension blood pressure effect
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Embodiment 1
[0029] Example 1 Preparation of rhynchophylline analogues of formula (1) structure
[0030] 1. Preparation of N-tert-butyloxycarbonyl-S-propargyl-cysteine (SPRC-Boc)
[0031]
[0032] Take S-propargyl-cysteine (1.59g, 10mmol) and dissolve in the mixed solution (50ml / 50ml) of tetrahydrofuran and water, add (Boc) 2 O (3.27g, 15mmol) and triethylamine (2.79ml, 20mmol), stirred at room temperature for 12 hours, TLC monitored the reaction, potassium permanganate chromogen developed color, after the reaction was complete, the tetrahydrofuran was decompressed, and then the remaining reaction solution Diethyl ether was extracted three times, the aqueous layer was adjusted to Ph=2 with 1N HCl, extracted three times with ethyl acetate, the organic phase was combined, and the organic phase was washed with anhydrous Na 2 SO 4 Dry, filter and spin dry to obtain a brown oily substance that is directly used as a reaction material;
[0033] 2. Preparation of compound (2)
[0034] ...
Embodiment 2
[0040] Embodiment 2 pharmacological action experiment
[0041] The rhynchophylline analog shown in structure (1) reduces the blood pressure and the heart rate level experiment of SHR rat:
[0042] Thirty-two 16-week-old inbred SHR rats were divided into four groups, 8 in each group, administered according to the following scheme, and the changes in blood pressure of the rats within 1 hour after administration were recorded:
[0043](1) SHR control group: SHR rats were given ethanol solution (400 microliters per kilogram of body weight) through the tail vein;
[0044] (2) 5mg / kg group: SHR rats were given ethanol solution of rhynchophylline analogues as shown in the above structure (1) through the tail vein (400 microliters per kilogram of body weight, containing 5 mg of analogues per 400 microliters) ;
[0045] (3) 10mg / kg group: SHR rats were given the ethanol solution of rhynchophylline analogues as shown in the above structure (1) through the tail vein (400 microliters pe...
Embodiment 3
[0049] Example 3 In Vitro Vascular Ring Experiment
[0050] The SD rats were anesthetized by intraperitoneal injection of chloral hydrate (20 mg / kg) and killed by neck dislocation. The thorax was cut open, and the complete thoracic aorta was taken out and placed in PSS nutrient solution with oxygen to strip the connective tissue and fat outside the blood vessel. The blood vessel was made into a 3mm vascular ring, which was placed in 37-degree oxygenated PSS nutrient solution, and connected to the tension transducer of the SUMC-PC biological signal processor (Shanghai Jialong Jiaoyi Factory) through a stainless steel triangle hook. Record the vasoconstriction tension, stimulate the blood vessels with norepinephrine and relax them with acetylcholine to prove the integrity of the vascular endothelium, then wash and change the fluid, stimulate the vasoconstriction with phenylephrine to reach a plateau, then add Y482 in order from low to high concentration, and draw the volume Effe...
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