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Dihydrazone Compounds with High Affinity to Aβ Protein and Tau Protein and Their Derivatives and Applications
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A compound, β-protein technology, applied in the field of medical imaging, can solve the problems of slow clearance, low signal-to-noise ratio, poor in vivo stability, and cannot be practically applied, and achieves fast clearance, high specificity, and good pharmacokinetic properties. Effect
Active Publication Date: 2020-06-16
BEIJING NORMAL UNIVERSITY +1
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2-Phenylimidazopyridine derivatives[ 123 I] IMPY (Zhang, Z.P.et al.Journal of Medicinal Chemistry.2003,46:237-243) is the first SPECT imaging agent to enter the clinical stage, but it cannot be practically applied due to its poor stability in vivo
Among these probes [ 18 F]T807 conducted the most in-depth study of AD cases, although [ 18 F]T807 has high selectivity for tau protein, but the latest research found that it has slow clearance in the brain and widespread non-specific binding, resulting in low signal-to-noise ratio
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Embodiment 1
[0029] Embodiment 1: synthetic compound 1
[0030]
[0031] The compound benzaldehyde (212.4mg, 2.0mmol) was dissolved in 10mL ethanol in a 50mL round bottom flask, then hydrazine hydrate (58.9mg, 1.0mmol) was slowly added to the reaction flask, and the reaction was refluxed at 90°C for 10 minutes. After the reaction was completed, , cooled until a yellow solid precipitated, the precipitated product was suction filtered, and washed with 10 mL of ethanol and petroleumether, and the crystalline product obtained by suction filtration was dried to obtain 44.0 mg of compound 1, with a yield of 18.5%, and the structure is as follows : 1 H NMR (400MHz, CDCl 3 )δ8.68 (s, 2H), 7.86 (dd, J=6.5, 3.0Hz, 4H), 7.56–7.35 (m, 6H).
Embodiment 2
[0032] Embodiment 2: synthetic compound 2
[0033]
[0034] Compound 2 was prepared from p-fluorobenzaldehyde according to the method for synthesizing compound 1, and 190.0 mg of a milky white solid was obtained with a yield of 77.8%. The structure is as follows: 1 H NMR (400MHz, CDCl 3 )δ8.62(s,2H),7.90–7.74(m,4H),7.21–7.06(m,4H).
Embodiment 3
[0035] Embodiment 3: synthetic compound 3
[0036]
[0037] Compound 3 was prepared from 4-chlorobenzaldehyde according to the method for synthesizing compound 1, and 131.0 mg of light yellow crystalline solid was obtained with a yield of 47.3%. The structure is as follows: 1 H NMR (400MHz, CDCl 3 )δ8.61(s,2H),7.78(d,J=8.5Hz,4H),7.43(d,J=8.5Hz,4H).
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Abstract
The present invention provides dihydrazone compounds and derivatives thereof with high affinity to Aβ protein and Tau protein, the structure of which is shown in formula (I): this type of compound can be directly used as When used in nuclear medicine imaging, fluorescent probes for junctions need to be labeled with appropriate radioactive isotopes. Such compounds are particularly useful in the diagnosis of neurodegenerative diseases, including Alzheimer's disease, in patients characterized by Aβ plaques and neurofibrillary tangles.
Description
technical field [0001] The invention relates to the technical field of medical imaging, in particular to a dihydrazone compound with high affinity with Aβ protein and Tau protein, its derivatives and applications. Background technique [0002] Alzheimer's disease (AD) is the most common disease in senile dementia, and its clinical manifestations are mainly progressive memory loss and irreversible sensory function impairment. It has become the fourth major disease that seriously threatens the health of the elderly after tumor, heart disease, stroke and diabetes. Neuropathological studies of AD have shown that the deposition of extracellularsenile plaques (SPs), intracellular neurofibrillary tangles (NFTs) and axonal dystrophies (DNs), which mainly occur in the cortex and hippocampus, are important pathological factors in AD. feature. Studies have shown that the deposition of Aβ protein in the brain begins 5-10 years before the onset of AD. After aggregation and deposition,...
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