74189-56-3Relevant 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.
Synthesis and biological evaluation of chalcone-polyamine conjugates as novel vectorized agents in colorectal and prostate cancer chemotherapy
Barette, Caroline,Champavier, Yves,Liagre, Bertrand,Pinon, Aline,Pouget, Christelle,Rioux, Benjamin,Sol, Vincent,Fagnère, Catherine,Gamond, Aurélie,Laurent, Aurélie,Martin, Frédérique
, (2021/06/15)
The aim of this study was to synthesize chalcone-polyamine conjugates in order to enhance bioavailability and selectivity of chalcone core towards cancer cells, using polyamine-based vectors. Indeed, it is well-known that polyamine transport system is upr
Tri-substituted pyrazole derivative and application
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Paragraph 0038-0039; 0043-0045, (2020/02/14)
The invention discloses a tri-substituted pyrazole derivative. Pharmacological research results show that compared with conventional anti-depression medicines, namely fluoxetine and manifarcin, the tri-substituted pyrazole derivative disclosed by the inve