7527-65-3Relevant articles and documents
Bithiazole Inhibitors of Phosphatidylinositol 4-Kinase (PI4KIIIβ) as Broad-Spectrum Antivirals Blocking the Replication of SARS-CoV-2, Zika Virus, and Human Rhinoviruses
Grazia Martina, Maria,Vicenti, Ilaria,Bauer, Lisa,Crespan, Emmanuele,Rango, Enrico,Boccuto, Adele,Olivieri, Noemi,Incerti, Matteo,Zwaagstra, Marleen,Allodi, Marika,Bertoni, Simona,Dreassi, Elena,Zazzi, Maurizio,van Kuppeveld, Frank J. M.,Maga, Giovanni,Radi, Marco
supporting information, p. 3548 - 3552 (2021/09/09)
Over half a century since the description of the first antiviral drug, “old” re-emerging viruses and “new” emerging viruses still represent a serious threat to global health. Their high mutation rate and rapid selection of resistance toward common antiviral drugs, together with the increasing number of co-infections, make the war against viruses quite challenging. Herein we report a host-targeted approach, based on the inhibition of the lipid kinase PI4KIIIβ, as a promising strategy for inhibiting the replication of multiple viruses hijacking this protein. We show that bithiazole inhibitors of PI4KIIIβ block the replication of human rhinoviruses (hRV), Zika virus (ZIKV) and SARS-CoV-2 at low micromolar and sub-micromolar concentrations. However, while the anti-hRV/ZIKV activity can be directly linked to PI4KIIIβ inhibition, the role of PI4KIIIβ in SARS-CoV-2 entry/replication is debated.
IDO INHIBITORS
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Paragraph 0623; 0930, (2016/10/27)
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Preparation of Vicinal N-Alkylamino Alcohols via Acylation-Rearrangement of Nitrones Followed by Hydride Reduction
Coates, Robert M.,Cummins, Clark H.
, p. 1383 - 1389 (2007/10/02)
Acylation-rearrangement of N-tert-butyl and N-cyclohexyl nitrones of cyclohexanecarboxaldehyde (1), n-butyraldehyde, isobutyraldehyde, 3-cyclohexenecarboxaldehyde, and α-methylpropionaldehyde gave α-pivaloyloxy imines, which underwent reduction with lithi