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Isosteviol derivative as well as preparation method and application thereof
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A technology of isosteviol and its derivatives, which is applied in the field of isosteviol derivatives and its preparation, can solve the problems of high cardiovascular risk and achieve good cardioprotective activity and the effect of protecting death and injury
Active Publication Date: 2021-07-13
GUANGDONG UNIV OF TECH
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Although including statins, angiotensin-converting enzyme inhibitors (ACEIs), beta-blockers (BBs), angiotensin II type 1 receptor blockers (ARBs) and aldosterone receptor blockers (AIRBs) Several groups of cardioprotective drugs, including , have been shown to be effective in reaching hard endpoints, but treatment of hypertension with these drugs reduces mortality by no more than 30%, and the residual cardiovascular risk remains quite high
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Embodiment 1
[0054] This example provides a series of isosteviol derivatives, prepared according to the following two synthetic routes:
[0059] Reaction conditions and reagents: (a) DPPA, Et 3 N, t BuOH, reflux; (b) Acid, DMAP, EDCI, DCM; (c) PDC, DMF.
[0060]
[0061] Specifically, the preparation method of each compound comprises the following steps:
[0062] (1) Synthesis of Compound 2
[0063] Isosteviol (50mg, 0.2mmol), sodiumhydroxide (31.4mg, 0.8mmol) and paraformaldehyde (37.8mg, 1.3mmol) were dissolved in absolute ethanol (2mL), the mixture was stirred at 80°C, and the reaction 5h. The mixture was diluted with ethyl acetate, neutralized with hydrochloric acid (1N), the solution was washed with saturated brine, dried over anhydrous ...
Embodiment 2
[0195] This example is a zebrafish experiment on a series of isosteviol derivatives prepared in the example, and the cardiac activity of the isosteviol derivatives of the present invention is evaluated through the zebrafish experiment.
[0196] (1) Breeding of zebrafish and collection of embryos: buy zebrafish (3-12 months old) from the National ZebrafishResource Center, and raise them in a mobile culture with a photoperiod of 14:10h (light: dark) and a temperature of 28.5±1°C Breeding in the box, feeding with live brine shrimp twice a day; mating of zebrafish (female:male=1:1), collecting embryos, washing with Holt Buffer buffer, and culturing in an incubator (28.5±1°C) for 24h , screened by microscopic examination.
[0197](2) DOX-induced zebrafish embryonic heart failure model for drug screening: 24hpf wild-type zebrafish embryos were allocated to 24-well plates (20 embryos / well), and 1 mL of DOX (100 μM) and various test compounds (5 , 15, 40μM), treated for 72h, observe...
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Abstract
The invention relates to an isosteviol derivative as well as a preparation method and application thereof. The isosteviol derivative disclosed by the invention has a structure as shown in a formula (I) which is described in the specification. In the formula (I), R1 is selected from a hydroxyl group or a carbonyl group; R2 is selected from H, a C1-5 saturated straight-chain alkyl group, a C3-6 saturated cyclic alkyl group, a pyridine ring, a phenyl group, a benzyl / substituted benzyl group, a phenethyl / substituted phenethyl group and phenylpropyl / substituted phenylpropyl group; and R3 is selected from a carboxyl group or primary amine. According to the isosteviol derivative, specific active sites of isosteviol are specifically modified, the obtained derivative has good heart protection activity, and the isosteviol derivative mainly prevents death and damage of myocardial cells by inhibiting excessive generation of active oxygen, recovering the potential of a mitochondrial membrane and maintaining mitochondrial morphology.
Description
technical field [0001] The present invention relates to the fields of drug design and medicinal chemistry, and more specifically relates to an isosteviol derivative and its preparation method and application. Background technique [0002] Cardiovascular disease (CVDs) is the disease with the highest mortality rate in the world. About 17.9 million people die from cardiovascular disease every year, accounting for 31% of the death toll in the world. Cardioprotective drugs can protect the metabolism, structure and function of the heart and blood vessels, and reduce their damage in primary or secondary prevention, and are extremely important in the treatment of patients with cardiovascular disease or high risk of cardiovascular disease. Although including statins, angiotensin-converting enzyme inhibitors (ACEIs), beta-blockers (BBs), angiotensin II type 1 receptor blockers (ARBs) and aldosteronereceptor blockers (AIRBs) Several groups of cardioprotective drugs, including , have...
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