23284-84-6Relevant articles and documents
Discovery of 2-oxopiperazine dengue inhibitors by scaffold morphing of a phenotypic high-throughput screening hit
Kounde, Cyrille S.,Yeo, Hui-Quan,Wang, Qing-Yin,Wan, Kah Fei,Dong, Hongping,Karuna, Ratna,Dix, Ina,Wagner, Trixie,Zou, Bin,Simon, Oliver,Bonamy, Ghislain M.C.,Yeung, Bryan K.S.,Yokokawa, Fumiaki
, p. 1385 - 1389 (2017)
A series of 2-oxopiperazine derivatives were designed from the pyrrolopiperazinone cell-based screening hit 4 as a dengue virus inhibitor. Systematic investigation of the structure-activity relationship (SAR) around the piperazinone ring led to the identification of compound (S)-29, which exhibited potent anti-dengue activity in the cell-based assay across all four dengue serotypes with EC50??0.1?μM. Cross-resistant analysis confirmed that the virus NS4B protein remained the target of the new oxopiperazine analogs obtained via scaffold morphing from the HTS hit 4.
Visible-Light-Induced Oxidative α-Alkylation of Glycine Derivatives with Ethers under Metal-Free Conditions
Song, Yang,Zhang, Hao,Guo, Jiabao,Shao, Yifei,Ding, Yuzhou,Zhu, Li,Yao, Xiaoquan
, p. 5914 - 5921 (2021/11/22)
In this work, a visible-light-induced oxidative α-alkylation of glycine derivatives with ethers has been developed in the presence of catalytic Eosin Y. Under the blue light of a 3 W LED, a range of α-etherized glycine derivatives, including α-amino esters, α-amino ketones and α-amino amides, were achieved with good to excellent yields and functional group tolerance with tert-butyl hydroperoxide (TBHP) as oxidant at ambient temperature. The operationally easy procedure provides an economical, metal-free, and mild alternative for the synthesis of the α-etherized glycine derivatives.
Al(OTf)3-Catalyzed Tandem Coupling Reaction between N,N-Disubstituted Aminomalonitriles and Substituted Arenes: a Synthesis of 1-Cyano-bisindolylmethane Analogues≠
Lei, Lin-Sheng,Wang, Bo-Wen,Jin, Da-Ping,Gao, Zhu-Peng,Huan-Liang,Wang, Shao-Hua,Xu, Xue-Tao,Zhang, Kun,Zhang, Xiao-Yun
supporting information, p. 2870 - 2875 (2020/06/17)
A synthesis of 1-cyano-bisindolylmethane analogues via an Al(OTf)3-catalyzed tandem coupling reaction between N,N-disubstituted aminomalonitriles and substituted arenes has been developed. This method not only provides an alternative synthetic strategy for the synthesis of corresponding functional molecules, but also enriches the volume of bisarylmethanes library to facilitate related functional studies. (Figure presented.).