82857-82-7Relevant articles and documents
Quorum sensing and nf-κb inhibition of synthetic coumaperine derivatives from piper nigrum
Baruch, Yifat,Gopas, Jacob,Kadosh, Yael,Kumar, Rajendran Saravana,Kushmaro, Ariel,Muthuraman, Subramani,Yaniv, Karin
supporting information, (2021/05/28)
Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections.
Preparation method of ilepcimide
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Paragraph 0050; 0052-0053; 0054; 0056-0057; 0058; 0060-0061, (2021/10/11)
The invention provides a preparation method of ilepcimide. The preparation method comprises the following step: in the presence of a catalyst, reacting raw materials containing 4-bromo-1, 2-methylenedioxybenzene, an acrylate compound and piperidine to obtain the ilepcimide. The preparation method disclosed by the invention is good in selectivity, reduces side reactions, increases the conversion rate and yield of the product, reduces the use of toxic and irritant raw materials, saves the treatment cost of three wastes, is a green and environment-friendly process, and is suitable for industrial production, and the molar yield is 76% or above, and the purity is 99% or above.
Piperine derivative as well as preparation method and application thereof
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Paragraph 0142; 0255-0256; 0260-0262, (2020/05/08)
The invention provides a piperine derivative as well as a preparation method and an application thereof. The piperine derivative is a compound shown as a formula (I), or a salt thereof, or a stereoisomer thereof, or a hydrate thereof. The compound provided by the invention can effectively protect nerve cells and improve the survival rate of the nerve cells, so that the compound provided by the invention can effectively treat neurodegenerative diseases and can be used for preparing medicines for treating the neurodegenerative diseases.