1484-85-1Relevant articles and documents
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Reeve,Eareckson
, p. 3299 (1950)
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Erne,Ramirez
, p. 912,915 (1950)
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Structure–activity relationship and biological evaluation of berberine derivatives as PCSK9 down-regulating agents
Fan, Tian-Yun,Yang, Yu-Xin,Zeng, Qing-Xuan,Wang, Xue-Lei,Wei, Wei,Guo, Xi-Xi,Zhao, Li-Ping,Song, Dan-Qing,Wang, Yan-Xiang,Wang, Li,Hong, Bin
, (2021/06/01)
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secreted protein and its deficiency markedly enhanced the survival rate of patient with cardiovascular diseases (CVDs). Forty berberine (BBR) derivatives were synthesized and evaluated for their activities on down-regulating the transcription of PCSK9 in HepG2 cells, taking BBR as the lead. Structure–activity relationship (SAR) analysis revealed that 2,3-dimethoxy moiety might be beneficial for activity. Among them, 9k displayed the most potent activity with IC50 value of 9.5 ± 0.5 μM, better than that of BBR. Also, it significantly decreased PCSK9 protein level at cellular level, as well as in the liver and serum of mice in vivo. Furthermore, 9k markedly increased LDLR expression and LDL-C clearance via down-regulating PCSK9 protein. The mechanism of action of 9k is targeting HNF1α and/or Sp1 cluster modulation upstream of PCSK9, a different one from BBR. Therefore, 9k might have the potential to be a novel PCSK9 transcriptional inhibitor for the treatment of atherosclerosis, worthy for further investigation.
A synthetic preparation method for small carbags hydrochloric acid
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Paragraph 0200-0202, (2021/12/08)
The present invention belongs to the field of organic chemistry, relates to a method of synthesizing berberine hydrochloride, comprising: S1: with 5-halo-o-quinoastearaldehyde and piperine ethylamine to obtain N- [2-(3,4-dimethoxyphenyl-5-yl) ethyl] -1- (5-halo-2,3-dimethoxybenzyl) methylimide; S2: to obtain 2- (3,4-diimoxyphenyl) -N- (5-bromo-2,3-dimethoxybenzyl) ethylamine; S3: to obtain 2-(3,4-dimethoxyphenyl) -N- (5-bromo-2 S4: to obtain 12-halogenated berberine derivative; S5: to obtain berberine. The present invention is free from the application of the by-product o-vanillin synthesis of o-resveratal raw material constraints, synthesis of 5- substitute o-resveratal and piperine ethylamine, and the use of the two preparation of berberine hydrochloride, with raw materials readily available, mild reaction conditions, easy to operate, high chemical yield, low cost and other advantages.
Method for preparing homopiperonyl amine by taking pyrocatechol as raw material
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Paragraph 0010; 0013; 0014; 0015, (2019/05/02)
A method for preparing homopiperonyl amine by taking pyrocatechol as the raw material relates to medicine preparing methods. The method comprises, firstly, taking the pyrocatechol with a purity degreeof 99 w% as the raw material, dimethyl sulfoxide as solvent and potassium carbonate as acid-binding agent to have methylenenation reaction with dichloromethane at 130 DEG C to obtain benzodioxole; secondly, taking ethyl acetate as solvent to perform one-step addition reaction on the benzodioxole and home-made 2-chlorethamin at 65 DEG C and with existence of catalysts to obtain homopiperonyl amine, and performing alkali neutralization; thirdly, evaporating the ethyl acetate from the reaction liquid, cooling down the reaction liquid for crystallization, and vacuumizing, filtering and drying crystals; fourthly, recrystallizing the initial product in absolute ethyl alcohol to obtain the finished homopiperonyl amine. The method for preparing the homopiperonyl amine by taking pyrocatechol as the raw material is simple in process, reduces the cost, avoids application of toxic cyanides and achieves green and sustainable processes as well as significant economic and social benefits.