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Application of substituted o-hydroxybenzophenone compound or pharmaceutically acceptable salt thereof to preparation of drug for treating neurodegenerative disease
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A technology for neurodegenerative diseases and o-hydroxybenzophenone, which is applied in the application field of substituting o-hydroxybenzophenone compounds in the preparation of drugs for the treatment of neurodegenerative diseases, and can solve the problems that AChE inhibitory activity needs to be improved
Active Publication Date: 2018-09-25
ZHEJIANG ACAD OF MEDICAL SCI
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In the Chinese patent application 201710170290.8, our laboratory has disclosed that metal ions and acetylcholinesterase are used as targets, starting from the special mode of action of rivastigmine and AChE catalytic triad, combined with the metal chelating fragment of acetophenone, using "Fusion method" design, synthesis and pharmacological activity screening resulted in a series of promising anti-senile dementia compounds, which showed good metal ionchelation ability and Aβ aggregation inhibitory ability in in vitro activity screening, but their AChE inhibition Activity needs to be improved
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Embodiment 1
[0084] Example 1: (4-tert-butyl-piperazin-1-yl)-phenyl-methanone (2-1)
[0085]
[0086] Dissolve 1.5g (8.06mmol) of N-Boc piperazine in 20ml of dichloromethane, then add 1.68ml (9.68mmol) of DIPEA, then slowly add 1.03ml (8.82mmol) of benzoyl chloride at 0°C. Then the temperature was raised to room temperature 25°C, and the reaction was stirred for 2h. After the reaction, it was diluted with 30 ml of dichloromethane, and washed with 50 ml of 1M sodiumhydroxide solution. It was dried over anhydroussodiumsulfate, filtered, and evaporated under reduced pressure to obtain 1.487 g of a yellow solid. 1 H-NMR (δ, CDCl 3):7.37-7.41(m,5H,ArH),3.73(m,2H,piperazine),3.38(m,2H,piperazine),2.94(m,2H,piperazine),2.81(m,2H,piperazine),1.47 (s,9H,-C(CH 3 ) 3 ).
Embodiment 2
[0087] Example 2 (4-tert-butyl-piperazin-1-yl)-(4-chloro-phenyl)-methanone (2-2)
[0090] Example 3 (4-tert-butyl-piperazin-1-yl)-(4-nitro-phenyl)-methanone (2-3)
[0091]
[0092] Operation is with embodiment 1. 1 H-NMR (δ, CDCl 3 ):8.31(t,1H,J=2.0Hz ArH),8.29(t,1H,J=2.0Hz,ArH),7.59(t,1H,J=2.0Hz,ArH),7.57(t,1H,J =2.0Hz ArH),3.77(m,2H,piperazine),3.55(m,2H,piperazine),3.41(m,2H,piperazine),3.35(m,2H,piperazine),1.47(s,9H,-C (CH 3 ) 3 ).
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Abstract
The invention discloses application of a substituted o-hydroxybenzophenone compound or a pharmaceutically acceptable salt thereof to preparation of a drug for treating a neurodegenerative disease. Thestructure of the compound is shown in a formula I; in the formula I, a structural formula of R1 is shown in the description, and the structural formula of R2 is independently -NR8R9 or a five-membered ring, a six-membered ring or a seven-membered ring containing -N; R3 is independently selected from H, hydroxy, amido, C1-C10 alkyl, C1-C10 alkenyl, aryl, or C1-C10 halo-alkyl, C1-C4 oxa-alkyl, C1-C4 aza-alkyl or halogen. The compound has acetylcholineesterase inhibitory activity, and a hydrolysate thereof has a metalionchelation effect, so the compound can treat from multiple targets, is suitable for preparing the drug for treating the neurodegenerative diseases, is especially suitable treating Alzheimer's disease or Parkinson's disease, and has a good application prospect of the neurodegenerative diseases. (The formula I is shown in the description.).
Description
technical field [0001] The invention relates to the field of derivatives of o-hydroxybenzophenone, in particular to the application of a substituted o-hydroxybenzophenone compound in the preparation of drugs for treating neurodegenerative diseases. Background technique [0002] At present, the problem of population aging in my country is becoming more and more serious. The "2011 Statistical Bulletin on the Development of China's Aging Career" shows that by the end of 2011, the number of people aged 60 and above in the country has reached 185 million, and has entered an aging society. Among them, dementia and other degenerative diseases are common and frequently-occurring diseases of the elderly. The incidence rate of people over 65 years old is 8%, 20% over 75 years old, and as high as 40% over 85 years old. [0003] Currently, the main marketed drugs for the treatment of senile dementia are five acetylcholinesterase (AChE) inhibitors and one N-methyl-D-aspartic acid (NMDA) ...
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