95124-20-2Relevant academic research and scientific papers
Schiff base Cu(I) catalyst for aerobic oxidation of primary alcohols
Lagerspets, Emi,Lagerblom, Kalle,Heli?vaara, Eeva,Hiltunen, Otto-Matti,Moslova, Karina,Nieger, Martin,Repo, Timo
, p. 75 - 79 (2019/02/25)
We report here new copper(I)-Schiff base complexes for the selective oxidation of primary alcohols to aldehydes under ambient conditions (with 2,2,6,6-tetramethylpiperdine-N-oxyl (TEMPO), N-methylimidazole (NMI), ambient air, acetonitril and RT). Particularly, the copper(I) complex bearing N-(4-fluorophenyl)-1-(furan-2-yl)methanimine (L2) showed high activity in the series and gave near- quantitative yields in the oxidations of benzyl alcohol (99% yield in 1 h) and 1-octanol (96% yield in 24 h). Based on the X-ray structure determination, the complex has a square pyramidal coordination accomplished by two L2 ligands and bromide as a counter anion. The oxidation reactions were monitored with UV–vis and in situ ATR-IR spectroscopy to study the changes in the catalytic structure and to elucidate the catalytic properties and the mechanistic details. Accordingly, detachment of one of the L2 ligands from the complexes is related to the oxidation activity.
Discovery of Indole Derivatives as Novel and Potent Dengue Virus Inhibitors
Bardiot, Dorothée,Koukni, Mohamed,Smets, Wim,Carlens, Gunter,McNaughton, Michael,Kaptein, Suzanne,Dallmeier, Kai,Chaltin, Patrick,Neyts, Johan,Marchand, Arnaud
, p. 8390 - 8401 (2018/09/25)
3-Acyl-indole derivative 1 was identified as a novel dengue virus (DENV) inhibitor from a DENV serotype 2 (DENV-2) phenotypic antiviral screen. Extensive SAR studies led to the discovery of new derivatives with improved DENV-2 potency as well as activity in nanomolar to micromolar range against the other DENV serotypes. In addition to the potency, physicochemical properties and metabolic stability in rat and human microsomes were improved during the optimization process. Chiral separation of the racemic mixtures showed a clear preference for one of the two enantiomers. Furthermore, rat pharmacokinetics of two compounds will be discussed in more detail, demonstrating the potential of this new series of pan-serotype-DENV inhibitors.
Dimethyl (2-Furyl)-N-(2-Methoxyphenyl)Aminomethylphosphonate Induces Apoptosis in Esophageal Squamous Cancer Cells. Structure Versus Activity of its Selected Analogs
Klimczak, Anna Agnieszka,Matusiak, Agnieszka,Lewkowski, Jaroslaw,Bitner, Jan,Szemraj, Janusz,Kontek, Renata
, p. 1088 - 1099 (2015/08/04)
Cytotoxicities of several new aminophosphonic compounds bearing 2-furyl moiety 2b-d and 3a-c on KYSE 30, 150, and 270 esophageal cancer cell lines are reported here. The qualitative study on correlations between the structure and cytotoxic activity of fur
Synthesis of new N-arylamino(2-furyl)methylphosphonic acid diesters, and in vitro evaluation of their cytotoxicity against esophageal cancer cells
Klimczak, Anna Agnieszka,Kuropatwa, Agnieszka,Lewkowski, Jaroslaw,Szemraj, Janusz
, p. 852 - 860 (2013/04/23)
N-Furfurylideneanilines and N-arylamino(2-furyl)methylphosphonates with tolyl and anisyl moieties were synthesized by the addition of phosphites to azomethine bond of corresponding Schiff bases and their NMR spectroscopic properties were investigated. The
VIRAL REPLICATION INHIBITORS
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Page/Page column 129; 140, (2013/04/13)
The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.
STUDIES IN THE FURAN SERIES. 22. N-ARYLFURFURYL- AND N-ARYL-5-METHYLFURFURYLAMINES AND THEIR N-ALLYL DERIVATIVES.
Klepo,Jakopcic
, p. 235 - 237 (2007/10/02)
The compounds, where aryl is a meta- or para-substituted chlorophenyl, methoxyphenyl, or methylphenyl group, were prepared by reduction of corresponding azomethines. Their allylation with allyl iodide or allyl bromide yielded tertiary N-arylfurfurylamines
