853994-91-9Relevant academic research and scientific papers
Generation, optimization and characterization of novel anti-prion compounds
Altieri, Andrea,Biasini, Emiliano,Biggi, Silvia,Ishibashi, Daisuke,Kurkin, Alexander V.,Nishida, Noriyuki,Sivtzev, Semen I.,Spiridonov, Evgeny A.
, (2020/09/09)
Prions are misfolded proteins involved in neurodegenerative diseases of high interest in veterinary and public health. In this work, we report the chemical space exploration around the anti-prion compound BB 0300674 in order to gain an understanding of its Structure Activity Relationships (SARs). A series of 43 novel analogues, based on four different chemical clusters, were synthetized and tested against PrPSc and mutant PrP toxicity assays. From this biological screening, two compounds (59 and 65) emerged with a 10-fold improvement in anti-prion activity compared with the initial lead compound, presenting at the same time interesting cell viability.
Efficient synthesis of substituted 3-iodofurans by electrophilic cyclization of propargylic oxirane derivatives
Xie, Yong-Xin,Liu, Xue-Yuan,Wu, Lu-Yong,Han, Yao,Zhao, Lian-Biao,Fan, Ming-Jin,Liang, Yong-Min
experimental part, p. 1013 - 1018 (2009/04/11)
The electrophilic cyclization of various propargylic oxirane compounds and I2 offers an efficient and straightforward route to highly substituted iodofurans under mild reaction conditions. Further functionalization has demonstrated that the iod
