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Synthesis of ring-opened derivatives of triazole-containing quinolinones and their antidepressant and anticonvulsant activities

Based on the potent antidepressant and anticonvulsant activities of the triazole-containing quinolinones reported in our previous work, a series of ring-opened derivatives of them were designed, synthesized in this work. Their antidepressant and anticonvulsant activities were screened using the forced swimming test (FST) and the maximal electroshock seizure test (MES), respectively. The results showed that compounds 4a, 5a, 6c-6e, 6g-6i, and 7 led to significant reductions in the accumulated immobility time in the FST at a dose of 50 mg/kg. Especially compound 7 exhibited higher levels of efficacy than the reference standard fluoxetine in the FST and the tail suspension test. The results of an open field test excluded the possibility of central nervous stimulation of 7, which further confirmed its antidepressant effect. Meanwhile, compounds 6a-6i and 7 showed different degrees of anticonvulsant activity in mice at the doses range from 300 to 30 mg/kg in the MES. Among them, compounds 6e and 7 displayed the ED50 of 38.5 and 32.7 mg/kg in the MES, and TD50 of 254.6 and 245.5 mg/kg, respectively. No one showed neurotoxicity at the dose of 100 mg/kg. The preliminary investigation forward to their mechanism indicated that regulation of GABAergic system might contribute to their anticonvulsive and anti-depressive action.

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Reference of 141-28-6, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 141-28-6, Name is Diethyl adipate, SMILES is CCOC(=O)CCCCC(=O)OCC, belongs to Triazoles compound. In a article, author is Tang, Shengbiao, introduce new discover of the category.

Scandium-catalyzed highly selective N-2-alkylation of benzotriazoles with cyclohexanones

A scandium-catalyzed highly N-2-selective alkylation of benzotriazoles with cyclohexanones has been developed, providing straightforward access to a series of N-2-alkylated benzotriazoles featuring newly formed tetrasubstituted carbon centers in high yields with excellent regioselectivities. The key to the success of this reaction is using Sc(OTf)(3) as the catalyst. Typically, this protocol is also well compatible with 4-aryl-1,2,3-triazoles.

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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 Iida, Tetsuya, once mentioned the application of 141-28-6, Name is Diethyl adipate, molecular formula is C10H18O4, molecular weight is 202.25, MDL number is MFCD00009215, category is Triazoles. Now introduce a scientific discovery about this category, Recommanded Product: 141-28-6.

Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders

Lysine demethylase 5 C (KDM5C) controls epigenetic gene expression and is attracting great interest in the field of chemical epigenetics. KDM5C has emerged as a therapeutic target for anti-prostate cancer agents, and recently we identified triazole 1 as an inhibitor of KDM5C. Compound 1 exhibited highly potent KDM5C-inhibitory activity in in vitro enzyme assays, but did not show strong anticancer effects. Therefore, a different approach is needed for the development of anticancer agents targeting KDM5C. Here, we attempted to identify KDM5C degraders by focusing on a protein-knockdown strategy. Compound 3 b, which was designed based on compound 1, degraded KDM5C and inhibited the growth of prostate cancer PC-3 cells more strongly than compound 1. These findings suggest that KDM5C degraders are more effective as anticancer agents than compounds that only inhibit the catalytic activity of KDM5C.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 141-28-6, Name is Diethyl adipate, SMILES is CCOC(=O)CCCCC(=O)OCC, in an article , author is Gomez-Martinez, Melania, once mentioned of 141-28-6, Product Details of 141-28-6.

N,N-Dialkylhydrazones as Versatile Umpolung Reagents in Enantioselective Anion-Binding Catalysis

An enantioselective anion-binding organocatalytic approach with versatile N,N-dialkylhydrazones (DAHs) as polarity-reversed (umpolung) nucleophiles is presented. For the application of this concept, a highly ordered hydrogen-bond (HB) network between a carefully selected CF3-substituted triazole-based multidentate HB-donor catalyst, the ionic substrate and the hydrazone in a supramolecular chiral ion-pair complex was envisioned. The formation of such a network was further supported by both experimental and computational studies, which showed the crucial role of the anion as a template unit. The asymmetric Reissert-type reaction of quinolines as a model test reaction chemoselectively delivered highly enantiomerically enriched hydrazones (up 95:5 e.r.) that could be further derivatized to value-added compounds with up to three stereocenters.

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 141-28-6 is helpful to your research. Category: Triazoles.

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, 141-28-6, Name is Diethyl adipate, SMILES is CCOC(=O)CCCCC(=O)OCC, belongs to Triazoles compound. In a document, author is El-Helw, Eman A. E., introduce the new discover, Category: Triazoles.

Evaluation of some new heterocycles bearing 2-oxoquinolyl moiety as immunomodulator against highly pathogenic avian influenza virus (H5N8)

The hydrazide obtained from furan-2(3H)-one integrated with a quinolin-2(1H)-one core reported previously by our research group was utilized as a building block synthon to obtain some pyrrolone, pyridazinone, oxadiazole, and triazole derivatives through treating with some carbon electrophilic reagents, for example, chloroacetyl chloride, benzoyl chloride, acetic anhydride, carbon disulfide, 3,4-dimethoxybenzaldehyde, and 2-oxoquinolin-3-carbaldehyde to achieve the target heterocycles. The newly synthesized compounds were evaluated as immunomodulator against highly pathogenic avian influenza virus (H5N8). The compounds 1, 11, and 17 displayed the highest potency (100% protection).

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 141-28-6 is helpful to your research. Category: Triazoles.

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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. 141-28-6, Name is Diethyl adipate, molecular formula is C10H18O4, belongs to Triazoles compound, is a common compound. In a patnet, author is Song, Han Byul, once mentioned the new application about 141-28-6, SDS of cas: 141-28-6.

Effects of Network Structures on the Tensile Toughness of Copper-Catalyzed Azide-Alkyne Cycloaddition (CuAAC)-Based Photopolymers

In the present study, photoinitiated copper-catalyzed azide-alkyne cycloaddition (CuAAC) polymerization was utilized to form structurally diverse glassy polymer networks. Systematic alterations in the monomer backbone rigidity (e.g., cyclic or aliphatic groups with a different length of the backbone) and the reactive functional group density (e.g., tetra-, tri-, di-, and monofunctional azide and alkyne monomers) were used to provide readily tailorable network structures with cross-link densities (estimated from the rubbery modulus) varying by a factor of over 20. All eight of the resultant networks exhibited glass transition temperatures (T-g(s)) between 50 and 80 degrees C with the tensile toughness ranging from 28 to 61 MJ m(-3). A nearly linear dependence of yield stress and elongation at break (broadly defined as strength and ductility, respectively) on the T-g and rubbery modulus was established in these triazole networks. When a flexible dialkyne monomer (five carbon spacing between alkynes) was incorporated into a network composed of a tri-alkyne and di-azide monomer, the elongation at break was improved from 166 to 300%, while the yield stress was reduced from 36 to 23 MPa. Additionally, the polymer ductility was also varied by incorporating monofunctional azides as chain ends into the network-replacing a sterically hindered stiff mono-azide with a more flexible mono-azide increased the elongation at break from 24 to 185% and the tensile toughness from 6 to 28 MJ m(-3).

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 141-28-6 is helpful to your research. Computed Properties of C10H18O4.

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 141-28-6, Name is Diethyl adipate, SMILES is CCOC(=O)CCCCC(=O)OCC, belongs to Triazoles compound. In a document, author is Yang, Chen, introduce the new discover, Computed Properties of C10H18O4.

Investigating the Stabilizing Forces of Pentazolate Salts

Pentazolate (cyclo-N-5(-)) salts are actively pursued energetic nitrogen-rich compounds due to their potential as propellants and explosives. An in-depth understanding of the stabilizing forces between cyclo-N-5(-) anions and cations is important for designing cyclo-N-5(-) salts and achieving cyclo-N-5(-) salt conversions. Herein, the metathetical syntheses of cyclo-N-5(-) salts (compounds 1-4) containing heterocyclic amino-based cations 3,6-diguanidino-1,2,4,5-tetrazine, 1-guanyl-1,2,4-triazolium, 3,7-diamino-7H-[1,2,4]triazolo[4,3-b][1,2,4]triazol-2-ium, and 3,6,7-triamino-7H-[1,2,4]triazolo[4,3-b][1,2,4]triazol-2-ium are reported. In addition, an energetic cocrystal (compound 5) composed of compound 4 with 3,6,7-triamino-7H-[1,2,4]triazolo[4,3-b][1,2,4]triazole was synthesized using cocrystallization techniques. Crystal structures were investigated through geometrical and Hirshfeld analyses and theoretical calculations to reveal the contributions of hydrogen-bonding and pi-stacking interactions in stabilizing the pentazolate salts. Compounds 1-3 are stabilized by strong hydrogen-bonding interactions and weak pi-stacking interactions. The it-stacking interactions (cation-anion pi(+)-pi(-) contacts) are stronger in 4 and have an important role in promoting the stability of the salt. The binding energy of this pi-stacking interaction (-82.4 kcal mol(-1)) slightly surpasses that of the robust N6-H6A center dot center dot center dot N1 interaction (-75.1 kcal mol(-1)). For cocrystal 5, the spatial arrangement of its structural framework differs from that of its precursor, compound 4. The molecular stabilization energy, which increases from -75.1 to -94.3 kcal mol(-1) during the conversion of 4-5, primarily arises from strong pi-stacking interactions. Further observations indicate that cocrystal 5 has better thermal stability and detonation performance than 4, which establishes noncovalent modification via cocrystallization as an efficient method for forming multicomponent crystal systems and highlights the ability of coformers to modify energetic performance.

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Related Products of 141-28-6, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 141-28-6.

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Investigation of Corrosion Inhibition Property of Triazole-Based Schiff Bases on Maraging Steel in Acid Mixtures

Triazole-based Schiff bases, 4-{[4-(dimethylamino)benzylidene]amino}-5-methyl-4H-1,2,4-triazole-3-thiol [DBAMTT] and 5-methyl-4-[(thiophene-2-ylmethylidene)amino]-4H-1,2,4-triazole-thiol [MTATT], were studied for their corrosion inhibitory action on maraging steel in the temperature range 30-45 degrees C in a 2:1 mixture of HCl and H2SO4. Both the inhibition efficiencies increased with temperature rise as well as the concentration of inhibitors. The anti-corrosion potential of these molecules was further validated by kinetic and thermodynamic analyses. Both DBAMTT and MTATT demonstrated inhibitory action of a mixed form by chemisorption on the metal surface obeying Langmuir isotherm adsorption. SEM-EDX analysis was conducted to confirm inhibitor adsorption onto the labeling steel surface. Experimental data indicated better corrosion inhibition property of MTATT over DBAMTT, whereas theoretical studies predict DBAMTT as a better inhibitor over MTATT. This may be due to the difference in the conditions of both studies: experimental studies carried out in acid solutions and theoretical studies in the gas phase. Different quantum chemical parameters were assessed using DFT calculations using the B3LYP/6-311++(d, p) basis set to gain insight into the relationship between the molecular structure and the efficiency of corrosion inhibition.

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One-pot three-component condensation for the synthesis of 2,4,6-triarylpyridines and evaluation of their antimicrobial activity

A new series of 2,4,6-triarylpyridines are synthesised through one-pot three-component condensation of triazole pyrazolyl aldehydes and acetophenones with ammonium acetate in moderate to good yields. The structures of the synthesised compounds are confirmed by spectral methods viz. IR, H-1 NMR, C-13 NMR and mass spectral analysis. All these scaffolds are evaluated for their in vitro antimicrobial activity and found to exhibit promising antimicrobial potency.

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Acryloyl isothiocyanate skeleton as a precursor for synthesis of some novel pyrimidine, triazole, triazepine, thiadiazolopyrimidine and acylthiourea derivatives as antioxidant agents

The reactions of 2-cyano-3-pyrazolylpropenoyl isothiocyanate derivative 2 with some mono- and bidentate nucleophiles namely, dodecan-1-amine, 6-aminothiouracil, hydrazine, phenylhydrazine, phenylurea, semicarbazide, and thiosemicarbazide, in addition to some derivatives of hydrazides, have been investigated to obtain some valuable heterocyclic skeletons gathering with a pyrazole core, viz. pyrimidine, triazole, triazepine, thiadiazolopyrimidine as well as acylthiourea derivatives. Hydrazinolysis of 2 was found to provide a mixture of thiosemicarbazide, diheterylazine, and triazepine derivatives. Treatment of 2 with phenylhydrazine was mainly dependent on the reaction conditions to produce a mixture of pyrimidinethione and triazole derivatives at room temperature or the triazepine derivative at heating conditions. The antioxidant activity screening of these compounds disclosed that pyrimidinethione derivatives 9 and 13 exhibited the most potency.

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