scholarly journals N-[7-Chloro-4-[4-(phenoxymethyl)-1H-1,2,3-triazol-1-yl] quinoline]-acetamide

Molbank ◽  
10.3390/m1213 ◽  
2021 ◽  
Vol 2021 (2) ◽  
pp. M1213
Author(s):  
Paolo Coghi ◽  
Jerome P. L. Ng ◽  
Ali Adnan Nasim ◽  
Vincent Kam Wai Wong

The 1,2,3-triazole is a well-known biologically active pharmacophore constructed by the copper-catalyzed azide–alkyne cycloaddition. We herein reported the synthesis of 4-amino-7-chloro-based [1,2,3]-triazole hybrids via Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition of 4-azido-7-chloroquinoline with an alkyne derivative of acetaminophen. The compound was fully characterized by Fourier-transform infrared (FTIR), proton nuclear magnetic resonance (1H-NMR), carbon-13 nuclear magnetic resonance (13C-NMR), heteronuclear single quantum coherence (HSQC), ultraviolet (UV) and high-resolution mass spectroscopies (HRMS). This compound was screened in vitro with different normal and cancer cell lines. The drug likeness of the compound was also investigated by predicting its pharmacokinetic properties.

1990 ◽  
Vol 36 (2) ◽  
pp. 225-229 ◽  
Author(s):  
K R Copeland ◽  
R W Yatscoff ◽  
R M McKenna

Abstract Eight cyclosporine (CsA) metabolites were isolated from the urine of renal-transplant patients by high-pressure liquid chromatography. Structure and purity of the metabolites were assessed by fast atomic bombardment/mass spectroscopy, by proton nuclear magnetic resonance (NMR), and, when the quantity of metabolites permitted, by 13C-NMR. The immunosuppressive activities (I) of the metabolites were tested in three separate in vitro systems: primary and secondary mixed lymphocyte reactions as well as by a mitogen-stimulated system. The I, as measured by comparing the concentration of each metabolite required for 50% inhibition of incorporation of [3H] thymidine, varied among the assay systems, as did the ranking of I among the test systems. In general, the I of most metabolites in all assay systems were less than 10% of that for CsA. Metabolites with single modifications exhibited the greatest I; e.g., that of M-17 was congruent to 16% of that of CsA (potency ratio 0.16) in a secondary mixed lymphocyte reaction. The significance of these findings in relation to therapeutic monitoring of CsA is discussed.


1985 ◽  
Vol 39 (1) ◽  
pp. 25-30 ◽  
Author(s):  
Danny O. Jacobs ◽  
Scott O. Trerotola ◽  
R.Gregg Settle ◽  
Rolando H. Rolandelli ◽  
Gerald L. Wolf ◽  
...  

2019 ◽  
Vol 10 (35) ◽  
pp. 8135-8142 ◽  
Author(s):  
Masoud Talebi Amiri ◽  
Stefania Bertella ◽  
Ydna M. Questell-Santiago ◽  
Jeremy S. Luterbacher

By using a quantitative HSQC-NMR method to measure chemical functionalities within the structure of isolated lignin samples, lignin's upgradability can be very precisely predicted.


2021 ◽  
Vol 12 (1) ◽  
pp. 56-59
Author(s):  
Mohammed Bahreldin Hussein ◽  
Muna Mahdi Mohammed ◽  
Abdalla Gobara ◽  
Asha Fadllallah Wady ◽  
Awad Salim Ibrahim Holy

Schiff bases are versatile ligands, synthesized via condensation of primary amines with carbonyl compounds. In this study, equimolar amounts of 4-imidazolecarboxaldehyde and thiosemicarbazide were combined and the Schiff base 4-imidazolecarboxaldehyde thiosemicarbazone was prepared as a new bidentate complexing agent. The synthesized ligand was reacted with palladium (II) and platinum (II) ions yielding air-stable complexes. For characterization purpose, infrared spectra, mass spectra, electronic spectra, thermal analysis, proton nuclear magnetic resonance and 13-carbon nuclear magnetic resonance spectra studies were carried out on the obtained complexes and ligand. The characterization data showed that the ligand acts as a bidentate coordinate to the metal ions through azomethine nitrogen and sulfur atoms. An in vitro antimicrobial investigation was also carried out for the free ligand and its metal complexes against four bacteria; Bacillus cereus, Staphylococcus aureus (Gram-positive), Escherichia coli and Salmonella typhimurium (Gram-negative) and one Fungi; Candida albicans, to assess their antimicrobial properties by disc diffusion technique. Antimicrobial activity of the prepared complexes showed higher activity than the free ligand.


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