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Discovery and SAR study of piperidine-based derivatives as novel influenza virus inhibitors

A series of piperidine-based derivatives were identified as novel and potent inhibitors of the influenza virus through structural modification of a compound that was selected from a high-throughput screen. Various analogues were synthesized and confirmed as inhibitors. The structure-activity relationship (SAR) studies suggested that the ether linkage between the quinoline and piperidine is critical for the inhibitory activity. The optimized compound tert-butyl 4-(quinolin-4-yloxy)piperidine-1-carboxylate 11e had an excellent inhibitory activity against influenza virus infection from a variety of influenza virus strains, with EC50values as low as 0.05 muM. The selectivity index value (SI = MLD50/EC50) of 11e is over 160 000 based on cytotoxicity, measured by MTT assays of three cell lines. We carried out a time-of-addition experiment to delineate the mechanism of inhibition. The result indicates that 11e interferes with the early to middle stage of influenza virus replication.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Brief introduction of (S)-4-Hydroxydihydrofuran-2(3H)-one

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 7331-52-4, help many people in the next few years.Application In Synthesis of (S)-4-Hydroxydihydrofuran-2(3H)-one

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Characterization of Secondary Metabolites from Various Solvent Extracts of Saffron Floral Waste

Isolation of secondary metabolites from saffron flower waste (stamens), and their identification using chromatographic techniques was carried out. Extraction was carried out with solvents (methanol, ethanol, ethyl acetate, diethylether and hexane) with different polarity. Gas chromatography?mass spectroscopy (GC?MS) technique was used for identification and structure elucidation of secondary metabolites obtained from saffron flower stamens. Chromatogram of ethanol showed higher peak area as compared to other solvents. Ethanol extract showed maximum number of peaks while chromatogram of hexane extract showed minimum number of peaks indicating that polarity of the solvent plays an important role in the extraction process. GC?MS analysis confirmed presence of many important compounds in saffron stamens such as alpha-tocopherol or vitamin E, dibutyl para-cresol, hydroquinone, and certain esters.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Awesome Chemistry Experiments For 15833-61-1

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 15833-61-1 is helpful to your research. Related Products of 15833-61-1

Related Products of 15833-61-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 15833-61-1, molcular formula is C5H10O2, introducing its new discovery.

ISOINDOLONE DERIVATIVES

Provided are compounds of formula (I), wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Properties and Exciting Facts About 3-Hydroxytetrahydrofuran

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 453-20-3, and how the biochemistry of the body works.Recommanded Product: 453-20-3

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 453-20-3, name is 3-Hydroxytetrahydrofuran, introducing its new discovery. Recommanded Product: 453-20-3

Hydrolase enzymes and their use in kinetic resolution

The invention relates to hydrolases and to polynucleotides encoding the hydrolases. In addition, the invention relates to the use of these hydrolase enzymes in kinetic resolution.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

The Absolute Best Science Experiment for (Tetrahydrofuran-3-yl)methanol

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Product Details of 15833-61-1, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 15833-61-1, name is (Tetrahydrofuran-3-yl)methanol. In an article£¬Which mentioned a new discovery about 15833-61-1

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential

Schizophrenia is a serious illness that affects millions of patients and has been associated with N-methyl-D-aspartate receptor (NMDAR) hypofunction. It has been demonstrated that activation of metabotropic glutamate receptor 5 (mGluR5) enhances NMDA receptor function, suggesting the potential utility of mGluR5 positive allosteric modulators (PAMs) in the treatment of schizophrenia. Herein we describe the optimization of an mGluR5 PAM by replacement of a phenyl with aliphatic heterocycles and carbocycles as a strategy to reduce bioactivation in a biaryl acetylene chemotype. Replacement with a difluorocyclobutane followed by further optimization culminated in the identification of compound 32, a low fold shift PAM with reduced bioactivation potential. Compound 32 demonstrated favorable brain uptake and robust efficacy in mouse novel object recognition (NOR) at low doses.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. COA of Formula: C4H6O3. Introducing a new discovery about 7331-52-4, Name is (S)-4-Hydroxydihydrofuran-2(3H)-one

PROCESSES AND HOST CELLS FOR GENOME, PATHWAY, AND BIOMOLECULAR ENGINEERING

The present disclosure provides compositions and methods for genomic engineering.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Awesome and Easy Science Experiments about 4100-80-5

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 4100-80-5, and how the biochemistry of the body works.Electric Literature of 4100-80-5

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Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues

A number of 6-(3,4-dimethoxyphenyl)-4,5-dihydro-2H-pyridazin-3-ones and a novel series of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones were prepared and tested on the cGMP-inhibited phosphodiesterase (PDE3) and cAMP-specific phosphodiesterase (PDE4) enzymes. All tested compounds were found to specifically inhibit PDE4 except for pyridazinone 3b, which showed moderate PDE4 (pIC50 = 6.5) as well as PDE3 (pIC50 = 6.6) inhibitory activity. In both the pyridazinone and phthlazinone series it was found that N-substitution is beneficial for PDE4 inhibition, whereas in the pyridazinone series it also accounts for PDE4 selectivity. In the phthalazinone series, the cis-4a,5,6,7,8,8a-hexahydrophthalazinones and their corresponding 4a,5,8,8a-tetrahydro analogues showed potent PDE4 inhibitory potency (10/11c,d: pIC50 = 7.6-8.4). A molecular modeling study revealed that the cis-fused cyclohexa(e)ne rings occupy a region in space different from that occupied by the other fused (un)saturated hydrocarbon rings applied; we therefore assume that the steric interactions of these rings with the binding site play an important role in enzyme inhibition.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Can You Really Do Chemisty Experiments About 915095-87-3

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915095-87-3, Name is (S)-(2-Chloro-5-iodophenyl)(4-((tetrahydrofuran-3-yl)oxy)phenyl)methanone, belongs to Tetrahydrofurans compound, is a common compound. Computed Properties of C17H14ClIO3In an article, once mentioned the new application about 915095-87-3.

Design, synthesis and anticancer activities of halogenated Phenstatin analogs as microtubule destabilizing agent

A series of halogenated Phenstatin analogs were designed as microtubule destabilizing agent by docking study. It was synthesized within three steps starting from 2-chloro-5-iodobenzoic acid and substituted benzene. All the products were characterized by 1H NMR and 13C NMR spectral analysis, and the stereochemical structure was also confirmed by a single crystal X-ray diffraction crystallographic analysis. The microtubule destabilizing activities were evaluated in vitro with human liver cancer Huh-7 cell line and human lung cancer A549 cell line. Some of the HPAs were achieved IC50 about 5.0 muM against human liver cancer Huh-7 cells. [Figure not available: see fulltext.].

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Properties and Exciting Facts About 3-Methyldihydrofuran-2,5-dione

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 4100-80-5. In my other articles, you can also check out more blogs about 4100-80-5

Electric Literature of 4100-80-5, 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.In a document type is Article, and a compound is mentioned, 4100-80-5, 3-Methyldihydrofuran-2,5-dione, introducing its new discovery.

Fenbufen, a new anti inflammatory analgesic: synthesis and structure activity relationships of analogs

100 analogs of fenbufen were prepared and tested using the carrageenan, polyarthritis, and UV erythema anti inflammatory tests and the 2 phenyl 1,4 benzoquinone writhing and inflamed paw pressure analgesic tests. Only 3 retained the same full spectrum of activity as fenbufen: dl 4 (4 biphenylyl) 4 hydroxybutyric acid, dl 4 (4 biphenylyl) 1,4 butanediol, and 4 biphenylacetic acid. Fenbufen had the same spectrum of activity as aspirin, phenylbutazone, and indomethacin in the 5 tests. In addition, dose response derived potencies show fenbufen more potent than aspirin and at least as potent as phenylbutazone in all 5 tests. Two related compounds were generally similar.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Top Picks: new discover of 3-Methyldihydrofuran-2,5-dione

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Construction of perhydro indol-2-ones by a methoxide catalyzed deacetylation-Michael-aldol cascade

An efficient, stereoselective Michael-aldol cascade for the one-pot construction of the perhydro indol-2-one bicyclic ring system using an acetate protected doubly-activated pyrrole-2-one pro-nucleophile and alpha,beta-unsaturated carbonyl compounds has been developed. Initiated by a methoxide deacetylation in methanol at room temperature, the cascade is easy to perform, stereoselective, efficient and broad in scope to this synthetically relevant structure.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem