357177-90-3Relevant academic research and scientific papers
Biomimetic Total Synthesis of Dysoxylum Alkaloids
Puerto Galvis, Carlos E.,Kouznetsov, Vladimir V.
, p. 15294 - 15308 (2019/11/29)
A five-step total synthesis of Dysoxylum alkaloids has been achieved using a biomimetic approach from zanthoxylamide protoalkaloids. The synthesis featured a direct amidation and a Bischler-Napieralski reaction to form the dihydroisoquinoline ring, which
Design, synthesis of N-phenethyl cinnamide derivatives and their biological activities for the treatment of Alzheimer's disease: Antioxidant, beta-amyloid disaggregating and rescue effects on memory loss
Chai, Tian,Zhao, Xiao-Bo,Wang, Wei-Feng,Qiang, Yin,Zhang, Xiao-Yun,Yang, Jun-Li
, (2018/10/26)
Gx-50 is a bioactive compound for the treatment of Alzheimer's disease (AD) found in Sichuan pepper (Zanthoxylum bungeanum). In order to find a stronger anti-AD lead compound, 20 gx-50 (1-20) analogs have been designed and synthesized, and their molecular structures were determined based on nuclear magnetic resonance (NMR) and mass spectrometry (MS) analysis, as well as comparison with literature data. Compounds 1-20 were evaluated for their anti-AD potential by using DPPH radical scavenging assay for considering their anti-oxidant activity, thioflavin T (ThT) fluorescence assay for considering the inhibitory or disaggregate potency of Ab, and transgenic Drosophila model assay for evaluating their rescue effect on memory loss. Finally, compound 13 was determined as a promising anti-AD candidate.
Column chromatography-free solution-phase synthesis of a natural piper-amide-like compound library
Kiim, Sumin,Lim, Chaemin,Lee, Sukjin,Lee, Seokwoo,Cho, Hyunkyung,Lee, Joo-Youn,Shim, Dong Sup,Park, Hee Dong,Kim, Sanghee
, p. 208 - 215 (2013/05/22)
We have achieved an efficient solution-phase parallel synthesis of a library of natural piper-amide-like compounds from the bifunctional β-phosphono-N-hydroxy-succinimidyl ester intermediate. The primary important feature in our study is the construction of natural-product-like molecules through the adaptation of sophisticated organic reactions that create water-soluble byproducts for a chromatography-free purification. This simple and efficient method rapidly provides a combinatorial library of high yield and purity. The library was evaluated against GPCR targets to demonstrate its potential use as a tool for drug discovery and in chemical biology.
