121817-65-0Relevant articles and documents
Synthesis of zanthoxylamide protoalkaloids and their in silico ADME-Tox screening and in vivo toxicity assessment in zebrafish embryos
Puerto Galvis, Carlos E.,Kouznetsov, Vladimir V.
, p. 291 - 299 (2018/11/24)
Inspired by the simple and attractive structure of zanthoxylamide protoalkaloids: armatamide, rubecenamide, lemairamin, rubemamine and zanthosine; isolated from plants of the genus Zanthoxylum. We report the synthesis of a series of 29 substituted N-pheny
N-Caffeoylphenalkylamide derivatives as bacterial efflux pump inhibitors
Michalet, Serge,Cartier, Gilbert,David, Bruno,Mariotte, Anne-Marie,Dijoux-franca, Marie-Genevieve,Kaatz, Glenn W.,Stavri, Michael,Gibbons, Simon
, p. 1755 - 1758 (2007/10/03)
As part of an ongoing project to identify plant natural products as efflux pump inhibitors (EPIs), bioassay-guided fractionation of the methanolic extract of Mirabilis jalapa Linn. (Nyctaginaceae) led to the isolation of an active polyphenolic amide: N-trans-feruloyl 4′-O-methyldopamine. This compound showed moderate activity as an EPI against multidrug-resistant (MDR) Staphylococcus aureus overexpressing the multidrug efflux transporter NorA, causing an 8-fold reduction of norfloxacin MIC at 292 μM (100 μg/mL). This prompted us to synthesize derivatives in order to provide structure-activity relationships and to access more potent inhibitors. Among the synthetic compounds, some were more active than the natural compound and N-trans-3,4-O-dimethylcaffeoyl tryptamine showed potentiation of norfloxacin in MDR S. aureus comparable to that of the standard reserpine.
