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Compound 1,10-N-decylene lycorine dibromo salt, pharmaceutical composition and application thereof in medicine

A technology of decylene double stones and compounds, which is applied in the field of medicine and can solve problems such as compounds that have not been seen

Inactive Publication Date: 2012-10-24
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there are no reports on the compound 1,10-N-decylenebislycorine dibromide and its pharmacological effects in the prior art

Method used

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  • Compound 1,10-N-decylene lycorine dibromo salt, pharmaceutical composition and application thereof in medicine
  • Compound 1,10-N-decylene lycorine dibromo salt, pharmaceutical composition and application thereof in medicine
  • Compound 1,10-N-decylene lycorine dibromo salt, pharmaceutical composition and application thereof in medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Compound 1, the preparation of 10-N-decylene bislycorine dibromide, namely compound 1:

[0028] Take lycorine (144 mg, 0.5 mmol), add 1 mL of dry DMF, 1,10-dibromodecane (75 mg, 0.25 mmol). After mixing, stir at 100 oC for 6-12 h under nitrogen protection. The solvent in the reaction system was evaporated to dryness, using gel LH-20 chromatographic column chromatography, methanol or water as the eluent, to obtain compound 1, 10-N-decylidene dilycorine dibromide, compound 1 (131 mg , 0.125 mmol, 60% yield).

[0029] Compound 1, 10-N-decyl dilycorine dibromide salt is compound 1, light yellow solid; 1 H NMR (CD 3 OD, 500 MHz) δ 7.11 (s, 2H), 7.08 (s, 2H), 6.05 (s, 4H), 5.80 (s, 2H), 4.90 (d, J = 14.0 Hz, 2H), 4.61 (br. s, 2H), 4.26 (br. s, 2H), 4.27 (d, J = 14.0 Hz, 2H), 3.90 (d, J = 10.0 Hz, 2H), 3.63 (m, 2H), 2.87-3.25 (m , 10H), 1.77 (m, 4H), 1.30 (m, 12H); ESIMS m / z: 357 [M] 2+ , 793 [M+Br] + .

[0030] Compound 1, the structural formula of compound 1, 10-N-de...

Embodiment 2

[0035] Determination of the cholinesterase inhibitory activity of compound 1, 10-N-decyldilycorine dibromide of the present invention, that is, compound 1:

[0036] For the assay method of human acetylcholinesterase (hAChE) and butyrylcholinesterase (hBChE) inhibitory activity, see Ellman et al [Ellman GL, Courtney KD, Andres V, Jr., Feather-Stone RM: A new and rapid colorimetric determination of acetylcholinesterase activity. Biochemical pharmacology 1961, 7:88-95.], the activity results of compound 1 are shown in Table 1.

[0037] Table 1 Inhibitory effect of compound 1 prepared in Example 1 on human acetylcholinesterase (hAChE) and butyrylcholinesterase (hBChE)

[0038]

[0039] a Mean ± SD; n = 3

Embodiment 3

[0041] Tablet: Compound 1 obtained in Example 1 10 mg, lactose 180 mg, starch 55 mg, magnesium stearate 5 mg;

[0042]Preparation method: mix compound 1 obtained in Example 1 with lactose and starch, wet it evenly with water, sieve the wet mixture and dry it, then sieve it, add magnesium stearate, and press the mixture into tablets, each weighing 250 mg, the compound content is 10 mg.

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Abstract

The invention relates to a compound 1, 10-N-decylene lycorine dibromo salt showed by the structural formula (1), a pharmaceutical composition of the compound, application of the compound in the preparation of medicines for treatment of Alzheimer's diseases (senile dementia) and in the preparation of a dual inhibitor of acetylcholinesterase and butyrylcholinesterase, and preparation methods of the compound and the pharmaceutical composition.

Description

Technical field: [0001] The invention relates to the field of medicine, in particular to the compound 1,10-N-decylbislycorine dibromide and its pharmaceutical composition, their preparation method, and their preparation and treatment of Alzheimer's disease (senile dementia) And the application in the preparation of dual inhibitors of acetylcholinesterase and butyrylcholinesterase. Background technique: [0002] Alzheimer's disease (AD), also known as senile dementia, is a degenerative disease of the central nervous system. It brings a heavy burden to patients, families and society. AD is a common disease of the elderly. It often occurs after the age of 60. The incidence rate is about 6.9% for those over 65 years old, and it can be as high as 50% for those over 85 years old. [0003] According to the currently accepted "cholinergic deficiency theory", the loss of the neurotransmitter-acetylcholine (ACh) in the brain of Alzheimer's patients is the key cause of AD. Acetylcho...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61K31/4745A61P25/28
Inventor 王跃虎龙春林罗吉凤
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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