57999-46-9Relevant articles and documents
Design, synthesis and biological evaluation of 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles as inhibitors of ebola virus infection
Bessières, Maxime,Plebanek, El?bieta,Chatterjee, Payel,Shrivastava-Ranjan, Punya,Flint, Mike,Spiropoulou, Christina F.,Warszycki, Dawid,Bojarski, Andrzej J.,Roy, Vincent,Agrofoglio, Luigi A.
, (2021/02/06)
Novel 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles were designed and synthesized as Ebola virus inhibitors. The proposed structures of the new prepared benzimidazole-piperidine hybrids were confirmed based on their spectral data and CHN analyses. The target compounds were screened in vitro for their anti-Ebola activity. Among tested molecules, compounds 26a (EC50=0.93 μM, SI = 10) and 25a (EC50=0.64 μM, SI = 20) were as potent as and more selective than Toremifene reference drug (EC50 = 0.38 μM, SI = 7) against cell line. Data suggests that the mechanism by which 25a and 26a block EBOV infection is through the inhibition of viral entry at the level of NPC1. Furthermore, a docking study revealed that several of the NPC1 amino acids that participate in binding to GP are involved in the binding of the most active compounds 25a and 26a. Finally, in silico ADME prediction indicates that 26a is an idealy drug-like candidate. Our results could enable the development of small molecule drug capable of inhibiting Ebola virus, especially at the viral entry step.
IVB group-containing bimetallic complex catalyst as well as preparation method and application thereof
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Paragraph 0111; 0113; 0122-0125, (2020/11/23)
The invention provides an IVB group-containing bimetallic complex catalyst as well as a preparation method and application of the catalyst. The IVB group-containing bimetallic complex has a structuralexpression shown in the specification. The IVB group-co
Metal complex, preparation method and application thereof
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Paragraph 0125; 0136-0140, (2020/10/20)
The invention provides a metal complex, a preparation method and application thereof. The metal complex has the following structural expression shown as the specification. The invention has the technical advantages that: the invention puts forward the O,