scholarly journals Deprotometalation-Iodolysis and Direct Iodination of 1-Arylated 7-Azaindoles: Reactivity Studies and Molecule Properties

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6314
Author(s):  
Mohamed Yacine Ameur Ameur Messaoud ◽  
Ghenia Bentabed-Ababsa ◽  
Ziad Fajloun ◽  
Monzer Hamze ◽  
Yury S. Halauko ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Bond Formation ◽  
Biological Properties ◽  
Crystallographic Data ◽  
Atomic Charges ◽  
Pka Values

Five protocols were first compared for the copper-catalyzed C-N bond formation between 7-azaindole and aryl/heteroaryl iodides/bromides. The 1-arylated 7-azaindoles thus obtained were subjected to deprotometalation-iodolysis sequences using lithium 2,2,6,6-tetramethylpiperidide as the base and the corresponding zinc diamide as an in situ trap. The reactivity of the substrate was discussed in light of the calculated atomic charges and the pKa values. The behavior of the 1-arylated 7-azaindoles in direct iodination was then studied, and the results explained by considering the HOMO orbital coefficients and the atomic charges. Finally, some of the iodides generated, generally original, were involved in the N-arylation of indole. While crystallographic data were collected for fifteen of the synthesized compounds, biological properties (antimicrobial, antifungal and antioxidant activity) were evaluated for others.

Improvement in mechanical, physical and biological properties of eucalyptus and pine woods by raw pine resin in situ polymerization

2021 ◽  
Vol 166 ◽  
pp. 113495
Author(s):  
Andrey Pereira Acosta ◽  
Kelvin Techera Barbosa ◽  
Sandro Campos Amico ◽  
André Luiz Missio ◽  
Rafael de Avila Delucis ◽  
...  
Keyword(s):  
In Situ Polymerization ◽  
Biological Properties ◽  
Pine Resin

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

ChemInform Abstract: C-C Bond Formation via C-H Bond Activation Using an in situ Generated Ruthenium Catalyst.

ChemInform ◽  
2009 ◽  
Vol 40 (44) ◽  
Author(s):  
Remi Martinez ◽  
Marc-Olivier Simon ◽  
Reynald Chevalier ◽  
Cyrielle Pautigny ◽  
Jean-Pierre Genet ◽  
...  
Keyword(s):  
Bond Activation ◽  
Bond Formation ◽  
Ruthenium Catalyst

Expression of a novel FGF in the Xenopus embryo. A new candidate inducing factor for mesoderm formation and anteroposterior specification

Development ◽  
1992 ◽  
Vol 114 (3) ◽  
pp. 711-720 ◽  
Author(s):  
H.V. Isaacs ◽  
D. Tannahill ◽  
J.M. Slack
Keyword(s):  
Specific Activity ◽  
Biological Properties ◽  
The Body ◽  
Mesoderm Induction ◽  
Gastrula Stage ◽  
Blastula Stage ◽  
Mesoderm Formation ◽  
Low Levels

We have cloned and sequenced a new member of the fibroblast growth factor family from Xenopus laevis embryo cDNA. It is most closely related to both mammalian kFGF (FGF-4) and FGF-6 but as it is not clear whether it is a true homologue of either of these genes we provisionally refer to it as XeFGF (Xenopus embryonic FGF). Two sequences were obtained, differing by 11% in derived amino acid sequence, which probably represent pseudotetraploid variants. Both the sequence and the behaviour of in vitro translated protein indicates that, unlike bFGF (FGF-2), XeFGF is a secreted molecule. Recombinant XeFGF protein has mesoderm-inducing activity with a specific activity similar to bFGF. XeFGF mRNA is expressed maternally and zygotically with a peak during the gastrula stage. Both probe protection and in situ hybridization showed that the zygotic expression is concentrated in the posterior of the body axis and later in the tailbud. Later domains of expression were found near the midbrain/hindbrain boundary and at low levels in the myotomes. Because of its biological properties and expression pattern, XeFGF is a good candidate for an inducing factor with possible roles both in mesoderm induction at the blastula stage and in the formation of the anteroposterior axis at the gastrula stage.

Aktywność biologiczna ekstraktów z propolisu

2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Magdalena Woźniak ◽  
Anna Kwiatkowska ◽  
Elżbieta Hołderna-Kędzia ◽  
Katarzyna Sosnowska ◽  
Lucyna Mrówczyńska ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Biological Activity ◽  
Phenolic Compounds ◽  
Propylene Glycol ◽  
Ethyl Alcohol ◽  
Antiradical Activity ◽  
Colorimetric Method ◽  
Biological Properties ◽  
Bioactive Substances ◽  
Dpph Test

Introduction. Propolis, also known as bee glue, is a resinous material collected by honeybees with numerous biological properties, including antibacterial, antifungal, antioxidant and anticancer effects. Due to its health-promoting properties, propolis is a component of many products, including dietary supplements, cosmetics and healthy food. Aim. The aim of the study was to determine the antibacterial, antifungal and antioxidant activity of propolis extracts, as well as to compare the biological activity of propolis extracts, depending on the solvent used – ethyl alcohol or propylene glycol. Material and methods. Two propolis extracts were used in the research – the first was prepared in ethyl alcohol, and the second in propylene glycol. The antimicrobial activity of the examined extracts was determined against S. aureus, E. coli and C. albicans. The antioxidant activity was determined on the basis of the evaluation of their antiradical activity in the DPPH· test and Fe2+ chelating activity. Moreover, the total content of phenolic compounds and flavonoids in the tested extracts was determined using the colorimetric method. Results. The tested propolis extracts, regardless of the solvent used (ethyl alcohol or propylene glycol), showed high antibacterial (against S. aureus), antifungal (against C. albicans) and antioxidant (antiradical activity in the DPPH· test and ferrous iron chelating potency in the ferrozine test) activity. Moreover, both tested extracts were characterized by a high and similar content of bioactive compounds – phenolic compounds and flavonoids. Conclusions. The results of the conducted tests showed that the solvent used did not affect determined biological activity and the content of bioactive substances in the tested propolis extracts.

In Situ Formation of Cationic π-Allylpalladium Precatalysts in Alcoholic Solvents: Application to C–N Bond Formation

ACS Catalysis ◽  
2021 ◽  
pp. 560-567
Author(s):  
Philippe Steinsoultz ◽  
Aurélien Bailly ◽  
Patrick Wagner ◽  
Estefania Oliva ◽  
Martine Schmitt ◽  
...  
Keyword(s):  
Bond Formation ◽  
In Situ Formation

scholarly journals Engineering the mechanical and biological properties of nanofibrous vascular grafts for in situ vascular tissue engineering

2017 ◽  
Vol 9 (3) ◽  
pp. 035007 ◽  
Author(s):  
Jeffrey J D Henry ◽  
Jian Yu ◽  
Aijun Wang ◽  
Randall Lee ◽  
Jun Fang ◽  
...  
Keyword(s):  
Tissue Engineering ◽  
Vascular Tissue ◽  
Vascular Grafts ◽  
Biological Properties ◽  
Vascular Tissue Engineering

A kinetic study of mechanochemical halogen bond formation by in situ31P solid-state NMR spectroscopy

2017 ◽  
Vol 53 (71) ◽  
pp. 9930-9933 ◽  
Author(s):  
Yijue Xu ◽  
Lysiane Champion ◽  
Bulat Gabidullin ◽  
David L. Bryce
Keyword(s):  
Activation Energy ◽  
Solid State ◽  
Nmr Spectroscopy ◽  
Kinetic Study ◽  
Solid State Nmr ◽  
Halogen Bond ◽  
Bond Formation ◽  
Nmr Studies ◽  
Solid State Nmr Spectroscopy

In situ 31P solid-state NMR studies of mechanochemical halogen bond formation provide insights into the cocrystallisation process and an estimate of the activation energy.

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