Application of aromatic alkanoyl tetrahydro-β-carboline and its derivatives in the treatment of metabolic diseases
A technology of aryl alkanoyl tetrahydro and derivatives, which can be used in metabolic diseases, medical preparations containing active ingredients, drug combinations, etc., and can solve the problem of unclear molecular mechanism of compounds, unsatisfactory physical and chemical properties of compounds, and restrictions on the development of compounds To improve pharmacokinetic properties, excellent therapeutic effects, and changes in physical and chemical properties
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Embodiment 1
[0107] Embodiment one: the preparation of each compound
Embodiment 1-1
[0108] Example 1-1, Synthesis of N-phenylacetyl-(6-trifluoromethyl)-1,3,4,9-tetrahydro-1H-β-carboline (NTC001)
[0109] Take 4-trifluoromethylphenylhydrazine hydrochloride (425mg, 2mmol) in 14mL alcohol and water (volume ratio is 5 / 1), slowly add 4-chlorobutyraldehyde dimethyl acetal (367mg, 2.2 mmol), then warming and reflux for 5-18 hours. Complete, remove most of the solvent under reduced pressure, then adjust the pH value of the solution to 12, extract three times with ethyl acetate, combine the organic phases, dry with anhydrous sodium sulfate, and distill off the solvent under reduced pressure to obtain the intermediate 5-trifluoroform Tritryptamine (crude product 464 mg).
[0110] 5-Trifluoromethyltryptamine (464mg, 2.0mmol) was dissolved in 3mL of glacial acetic acid, and 37% formaldehyde solution (45μL, 0.60mmol) was added dropwise under the protection of nitrogen to complete the addition and react overnight. Most of the acetic acid was evaporated under reduced pres...
Embodiment 2-52
[0112] Preparation of NTC002-52 carboline compounds shown in Example 2-52 and Table 1 (see reference below for specific process)
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[0118] Embodiment 1: The compound of the present invention is to the treatment of type 2 diabetic mice
[0119] (1) Establishment of type 2 diabetes mouse model
[0120] Purchase 6-week-old ICR mice, observe them in the animal center for one week, feed them with high-fat diet (ResearchDiets company, 60% fat) for 3 weeks, weigh the mice every week, remove the mice with no significant increase in body weight after three weeks, and become obese The mice were intraperitoneally injected with 2% STZ citric acid solution at a dose of 85mg / kg, fed with high-fat feed continuously, and the blood glucose of the mice was measured two hours after the meal after three weeks, and those with a blood glucose value higher than 11.1mM were considered to be type 2 diabetes Mice, mice whose blood sugar level ...
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