Category: 10500-57-9

Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter. 10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, SMILES is C1=CC=NC2=C1CCCC2, belongs to quinoxaline compound. In a document, author is Silveira, Flavia F., introduce the new discover, COA of Formula: C9H11N.

Comparative study between the anti-P. falciparum activity of triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives and the identification of new PfDHODH inhibitors

In this work, we designed and synthesized 35 new triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives as P. falciparum inhibitors (3D7 strain). Thirty compounds exhibited anti-P. falciparum activity, with IC50 values ranging from 0.030 to 9.1 mu M. The [1,2,4] triazolo[1,5-a]pyrimidine derivatives were more potent than the pyrazolo[1,5-a]pyrimidine and quinoline analogues. Compounds 20, 21, 23 and 24 were the most potent inhibitors, with IC50 values in the range of 0.030-0.086 mu M and were equipotent to chloroquine. In addition, the compounds were selective, showing no cytotoxic activity against the human hepatoma cell line HepG2. All [1,2,4]triazolo[1,5-a]pyrimidine derivatives inhibited PfDHODH activity in the low micromolar to low nanomolar range (IC50 values of 0.08-1.3 mu M) and did not show significant inhibition against the HsDHODH homologue (0-30% at 50 mu M). Molecular docking studies indicated the binding mode of [1,2,4]triazolo[1,5-a]pyrimidine derivatives to PfDHODH, and the highest interaction affinities for the PfDHODH enzyme were in agreement with the in vitro experimental evaluation. Thus, the most active compounds against P. falciparum parasites 20 (R = CF3, R-1 = F; IC50 = 0.086 mu M), 21 (R = CF3; R-1 = CH3; IC50 = 0.032 mu M), 23, (R = CF3, R-1 = CF3; IC50 = 0.030 mu M) and 24 (R = CF3, 2-naphthyl; IC50 = 0.050 mu M) and the most active inhibitor against PfDHODH 19 (R = CF3, R-1 = Cl; IC50 = 0.08 mu M – PfDHODH) stood out as new lead compounds for antimalarial drug discovery. Their potent in vitro activity against P. falciparum and the selective inhibition of the PfDHODH enzyme strongly suggest that this is the mechanism of action underlying this series of new [1,2,4]triazolo[1,5-a]pyrimidine derivatives. (c) 2020 Elsevier Masson SAS. All rights reserved.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 10500-57-9, in my other articles. COA of Formula: C9H11N.

Reference:
Quinoline – Wikipedia,
,Quinoline | C9H7N – PubChem

In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. The reactant in an enzyme-catalyzed reaction is called a substrate. 10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, molecular formula is , belongs to quinoxaline compound. In a document, author is Hagras, Mohamed, Safety of 5,6,7,8-Tetrahydroquinoline.

Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation

Discovering of new anticancer agents with potential activity against tubulin polymerisation is still a promising approach. Colchicine binding site inhibitors are the most relevant anti-tubulin polymerisation agents. Thus, new quinoline derivatives have been designed and synthesised to possess the same essential pharmacophoric features of colchicine binding site inhibitors. The synthesised compounds were tested in vitro against a panel of three human cancer cell lines (HepG-2, HCT-116, and MCF-7) using colchicine as a positive control. Comparing to colchicine (IC50 = 7.40, 9.32, and 10.41 mu M against HepG-2, HCT-116, and MCF-7, respectively), compounds 20, 21, 22, 23, 24, 25, 26, and 28 exhibited superior cytotoxic activities with IC50 values ranging from 1.78 to 9.19 mu M. In order to sightsee the proposed mechanism of anti-proliferative activity, the most active members were further evaluated in vitro for their inhibitory activities against tubulin polymerisation. Compounds 21 and 32 exhibited the highest tubulin polymerisation inhibitory effect with IC50 values of 9.11 and 10.5 nM, respectively. Such members showed activities higher than that of colchicine (IC50 = 10.6 nM) and CA-4 (IC50 = 13.2 nM). The impact of the most promising compound 25 on cell cycle distribution was assessed. The results revealed that compound 25 can arrest the cell cycle at G2/M phase. Annexin V and PI double staining assay was carried out to explore the apoptotic effect of the synthesised compounds. Compound 25 induced apoptotic effect on HepG-2 thirteen times more than the control cells. To examine the binding pattern of the target compounds against the tubulin heterodimers active site, molecular docking studies were carried out.

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Related Products of 10500-57-9, Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, SMILES is C1=CC=NC2=C1CCCC2, belongs to quinoxaline compound. In a article, author is Melis, Diana R., introduce new discover of the category.

Subcellular Localisation of a Quinoline-Containing Fluorescent Cyclometallated Ir-III Complex in Plasmodium falciparum

A fluorescent analogue of a previously synthesised N,N-chelated Ir-III complex was prepared by coordination of the organic ligand to an extrinsic bis(2-phenylpyridine)iridium(III) fluorophore. This cyclometallated Ir-III complex in itself displays good, micromolar activity against the chloroquine-sensitive NF54 strain of Plasmodium falciparum. Live-cell confocal microscopy found negligible localisation of the fluorescent complex within the digestive vacuole of the parasite. This eliminated the haem detoxification pathway as a potential mechanism of action. Similarly, no localisation of the complex within the parasitic nucleus was found, thus suggesting that this complex probably does not interfere with the DNA replication process. A substantial saturation of fluorescence from the complex was found near phospholipid structures such as the plasma and nuclear membranes but not in neutral lipid bodies. This indicates that an association with these membranes, or organelles such as the endoplasmic reticulum or branched mitochondrion, could be essential to the efficacies of these types of antimalarial compounds.

Related Products of 10500-57-9, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 10500-57-9 is helpful to your research.

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Quinoline – Wikipedia,
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Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, new energy materials, nano-ceramics, nano-hybrid composite materials, preparation and modification of special coatings. , Name: 5,6,7,8-Tetrahydroquinoline, 10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, molecular formula is C9H11N, belongs to quinoxaline compound. In a document, author is Kwak, Sang Woo, introduce the new discover.

Synthesis and Photophysical Properties of a Series of Dimeric Indium Quinolinates

A novel class of quinolinol-based dimeric indium complexes (1-6) was synthesized and characterized using H-1 and C-13(H-1) NMR spectroscopy and elemental analysis. Compounds 1-6 exhibited typical low-energy absorption bands assignable to quinolinol-centered pi-pi* charge transfer (CT) transition. The emission spectra of 1-6 exhibited slight bathochromic shifts with increasing solvent polarity (p-xylene < tetrahydrofuran (THF) < dichloromethane (DCM)). The emission bands also showed a gradual redshift, with an increase in the electron-donating effect of substituents at the C5 position of the quinoline groups. The absolute emission quantum yields (phi(PL)) of compounds 1 (11.2% in THF and 17.2% in film) and 4 (17.8% in THF and 36.2% in film) with methyl substituents at the C5 position of the quinoline moieties were higher than those of the indium complexes with other substituents. We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 10500-57-9. The above is the message from the blog manager. Name: 5,6,7,8-Tetrahydroquinoline.

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Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Basavanna, Vrushabendra, once mentioned the application of 10500-57-9, Category: quinolines-derivatives, Name is 5,6,7,8-Tetrahydroquinoline, molecular formula is C9H11N, molecular weight is 133.19, MDL number is MFCD00006734, category is quinoxaline. Now introduce a scientific discovery about this category.

Quinolinyl-pyrazoles: synthesis and pharmacological evolution in the recent decennial

In the recent decade, the study on N-heterocycles has dramatically increased due to its versatility in many significant fields and because of its distinctive battle which is associated with the bioassay and its interaction with the cells. These novel heterocycles are designed and synthesized by chemists through new strategies on par with the reported methods. Subsequently, the synthesized molecules were screened for their efficacy against the typical drugs in the market. In this article, recently unveiled pharmacologically important quinoline allied pyrazoles have been reviewed. Moreover, this review gives a bird’s-eye view of different methods adopted for synthesis in addition to the conventional approaches and also detailed study of the bioactive quinolinyl-pyrazole heterocycle when compared with standard drug-associated/having efficient molecule. We believe that this review will inspire synthetic as well as medicinal chemists who are in quest of less toxic and more potent quinolinyl-pyrazoles for the treatment of various health threats. [GRAPHICS] .

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Quinoline – Wikipedia,
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Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. COA of Formula: C9H11N,10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, SMILES is C1=CC=NC2=C1CCCC2, belongs to quinoxaline compound. In a document, author is Qin, Jing-Can, introduce the new discover.

Design and synthesis of a solvent-dependent fluorescent probe for dual selective detection of Mg2+ ion and Zn2+ ion

A solvent-dependent fluorescent probe QC for the dual detection of Mg2+ ion and Zn2+ ion has been constructed based on a Schiff base compound, in which 8-hydroxyquinoline served as not only a fluorophore but also a recognition group. Among the various tested metal ions, this probe exhibited high sensitivity and good selectivity toward Mg2+ ion in acetonitrile and Zn2+ ion in EtOH-H2O (9:1, v/v), respectively. With the treatment of Mg2+ ion or Zn2+ ion, 1:2 complex was formed between QC and Mg2+ ion, which inhibited the PET processes caused by the lone pair electrons from the nitrogen atom of the -C = N group and the nitrogen atom of quinoline moiety, resulting in the fluorescence enhancement for Mg2+ ion. Whereas a 1:1 complex was formed between QC and Zn2+ ion, which inhibited the PET process only caused by the lone pair electrons from the nitrogen atom of the -C = N group, resulting in the fluorescence enhancement at a shorter wavelength. The detection limit was calculated as low as 6.28 x 10(-8) M for Mg2+ ion and 2.36 x 10(-7) M for Zn2+ ion. DFT analysis further supported this concept to design the probe.

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Quinoline – Wikipedia,
,Quinoline | C9H7N – PubChem

Electric Literature of 10500-57-9, Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, SMILES is C1=CC=NC2=C1CCCC2, belongs to quinoxaline compound. In a article, author is Rao, Ramdas Nishanth, introduce new discover of the category.

An expeditious microwave assisted one-pot sequential route to pyrido fused imidazo[4,5-c] quinolines in green media

An expeditious microwave assisted one-pot sequential route to synthesize pyrido fused imidazo[4,5-c]quinolines via the Pictet-Spengler cyclization strategy has been developed. In this study, substituted 2-amino pyridines are condensed with 2-bromo-2 ‘-nitroacetophenone to generate imidazo[1,2-a]pyridines with nitro group functionality at C-2 position. Reduction of nitro group to its amine congener in green media followed by the Pictet-Spengler cyclization strategy with substituted aldehydes led to the formation of new C-C and C-N bonds in a one-pot sequential manner. The cyclization proceeds through the CO(carbonyl)-C(H) cleavage of the aldehyde group via oxidative cross-coupling, transamination, cyclization and aromatization steps. Low cost reagents and a green solvent were used to facilitate the architecturally beautiful pyrido fused imidazo[4,5-c]quinoline scaffolds in high yields. The key features of this synthetic protocol are the use of microwave-assisted mild reaction conditions, one-pot sequential pathway, broad substrate scope and green media, which make it feasible for the synthesis of fused polyheterocycles. Moreover, the synthetic manipulation proceeded well with heteroaromatic and aliphatic aldehydes also in good yields.

Electric Literature of 10500-57-9, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 10500-57-9 is helpful to your research.

Reference:
Quinoline – Wikipedia,
,Quinoline | C9H7N – PubChem

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Mehndiratta, Samir, once mentioned the application of 10500-57-9, SDS of cas: 10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, molecular formula is C9H11N, molecular weight is 133.19, MDL number is MFCD00006734, category is quinoxaline. Now introduce a scientific discovery about this category.

Effect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms

A series of 3-subsituted quinolinehydroxamic acids has been synthesised and evaluated for their effect on human lung cancer cell line (A549), human colorectal cancer cell line (HCT116) and HDAC isoforms 1, 2, 6, and 8. The results indicated that substitution at C3 of quinoline is favoured for HDAC6 selectivity. Two compounds (25 and 26) were also found to be potent anti-proliferative compounds with IC50 values ranging from 1.29 to 2.13 mu M against A549 and HCT116 cells. These compounds displayed remarkable selectivity for HDAC6 over other HDAC isoforms with nanomolar IC50 values. Western blot analysis revealed that compounds of this series activate apoptotic caspase pathway as indicated by cleavage of caspase 3, 8, and 9 and also increase phosphorylated H2AX thus inducing DNA double strand fragmentation in a concentration dependent manner. Flow cytometric analysis also displayed a dose dependent increase of cell population in sub G1 phase.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 10500-57-9 help many people in the next few years. SDS of cas: 10500-57-9.

Reference:
Quinoline – Wikipedia,
,Quinoline | C9H7N – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. Name: 5,6,7,8-Tetrahydroquinoline,10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, SMILES is C1=CC=NC2=C1CCCC2, belongs to quinoxaline compound. In a document, author is Kitagawa, Osamu, introduce the new discover.

Chiral Pd-Catalyzed Enantioselective Syntheses of Various N-C Axially Chiral Compounds and Their Synthetic Applications

Biaryl atropisomers are key structural components in chiral ligands, chiral functional materials, natural products, and bioactive compounds, and their asymmetric syntheses have been reported by many groups. In contrast, although the scientific community has long been aware of atropisomers due to rotational restriction around N-C bonds, they have attracted scant attention and have remained an unexplored research area. In particular, their catalytic asymmetric synthesis and the synthetic applications were unknown until recently. This Account describes studies conducted by our group on the catalytic enantioselective syntheses of N-C axially chiral compounds and their applications in asymmetric reactions. In the presence of a chiral Pd catalyst, the reactions of achiral secondary ortho-tert-butylanilides with 4-iodonitrobenzene proceeded in a highly enantioselective manner (up to 96% ee), affording N-C axially chiral N-arylated ortho-tert-butylanilides in good yields. The application of the present chiral Pd-catalyzed N-arylation reaction to an intramolecular version gave N-C axially chiral lactams with high optical purity (up to 98% ee). These reactions were the first highly enantioselective syntheses of N-C axially chiral compounds with a chiral catalyst. Since the publication of these reactions, N-C axially chiral compounds have been widely accepted as new target molecules for catalytic asymmetric reactions. Furthermore, chiral-Pd-catalyzed intramolecular N-arylations were applied to the enantioselective syntheses of N-C axially chiral quinoline-4-one and phenanthridin-6-one derivatives. We also succeeded in the enantioselective syntheses of various N-C axially chiral compounds using other chiral Pd-catalyzed reactions. That is, optically active N-C axially chiral N-(2-tert-butylphenyl)indoles, 3-(2-bromophenyl)quinazolin-4-ones, and N-(2-tert-butylphenypsulfonamides were obtained through chiral Pd-catalyzed 5-endo-hydroaminocyclization, monohydrodebromination (reductive asymmetric desymmetrization), and Tsuji-Trost N-allylation, respectively. The study of the catalytic asymmetric synthesis of axially chiral indoles has contributed to the development of not only N-C axially chiral chemistry but also the chemistry of axially chiral indoles. Subsequently, the catalytic asymmetric syntheses of various indole derivatives bearing a C-C chiral axis as well as an N-C chiral axis have been reported by many groups. Moreover, axially chiral quinazlolin-4-one derivatives, which were obtained through chiral Pd-catalyzed asymmetric desymmetrization, are pharmaceutically attractive compounds; for example, 2-methyl-3-(2-bromophenyl)quinazolin-4-one product is a mebroqualone possessing GABA agonist activity. Most of the N-C axially chiral products have satisfactory rotational stability for synthetic applications, and their synthetic utility was also demonstrated through application to chiral enolate chemistry. That is, the reaction of various alkyl halides with the enolate prepared from the optically active anilide, lactam, and quinazolinone products proceeded with high diastereoselectivity by asymmetric induction due to the N-C axial chirality. At the present time, N-C axially chiral chemistry has become a popular research area, especially in synthetic organic chemistry, and original papers on the catalytic asymmetric syntheses of various N-C axially chiral compounds and their synthetic applications have been published.

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Quinoline – Wikipedia,
,Quinoline | C9H7N – PubChem

Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. 10500-57-9, Name is 5,6,7,8-Tetrahydroquinoline, molecular formula is C9H11N. In an article, author is Vinoth, Nangagoundan,once mentioned of 10500-57-9, HPLC of Formula: C9H11N.

Expedient Synthesis and Antibacterial Activity of Tetrahydro-1 ‘ H-spiro[indoline-3,4 ‘-quinoline]-3 ‘-carbonitrile Derivatives Using Piperidine as Catalyst

A convenient synthesis of 2 ‘-amino-7 ‘,7 ‘-dimethyl-2,5 ‘-dioxo-1 ‘-(phenylamino)-5 ‘,6 ‘,7 ‘,8 ‘-tetrahydro-1 ‘ H-spiro[indoline-3,4 ‘-quinoline]-3 ‘-carbonitrile derivatives has been designed using different substituted isatins, various 5,5-dimethyl-3-(2-phenylhydrazinyl)cyclohex-2-enones (arylhydrazones of dimedone) and malononitrile in ethanol with piperidine as catalyst at room temperature. The structures of the synthesized compounds have been elucidated by various spectroscopic techniques. The selected compounds have also been evaluated for their antibacterial activities against human pathogenic bacteria.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 10500-57-9. HPLC of Formula: C9H11N.

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Quinoline – Wikipedia,
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