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SUBSTITUTED PHENOXY-AMINOPROPANOLS

Substituted phenoxy-aminopropanols of the formula STR1 wherein R is a branched-chain alkyl of 3 or 4 carbon atoms, R 1 is hydrogen, halogen or lower alkyl and R 2 and R 3, independently, are hydrogen, halogen, lower alkyl, lower alkoxy or lower alkylthio, and pharmaceutically acceptable acid addition salts thereof, are described. A process for their preparation, as well as pharmaceutical preparations containing them are also described. The compounds of formula I and their salts possess cardioselective beta-adrenergic blocking activity and antihypertensive activity.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extracurricular laboratory:new discovery of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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SHMT INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Cinnamamides, novel liver X receptor antagonists that inhibit ligand-induced lipogenesis and fatty liver

Liver X receptor (LXR) is a member of the nuclear receptor superfamily, and it regulates various biologic processes, including de novo lipogenesis, cholesterol metabolism, and inflammation. Selective inhibition of LXR may aid the treatment of nonalcoholic 1fatty liver diseases. In the present study, we evaluated the effects of three cinnamamide derivatives on ligand-induced LXRalpha activation and explored whether these derivatives could attenuate steatosis in mice. N-(4-trifluoromethylphenyl) 3,4-dimethoxycinnamamide (TFCA) decreased the luciferase activity in LXRE-tk-Luc-transfected cells and also suppressed ligand-induced lipid accumulation and expression of the lipogenic genes in murine hepatocytes. Furthermore, it significantly attenuated hepatic 1neutral lipid accumulation in a ligand-induced fatty liver mouse 1system. Modeling study indicated that TFCA inhibited activation of the LXRalpha ligand-binding domain by hydrogen bonding to Arg305 in the H5 region of that domain. It regulated the transcriptional control exerted by LXRalpha by influencing coregulator exchange; this process involves dissociation of the thyroid hormone receptor-associated proteins (TRAP)/DRIP coactivator and recruitment of the nuclear receptor corepressor. These results show that TFCA has the potential to attenuate ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRalpha in the liver.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Reference of 2879-20-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, molecular formula is C10H10O3. In a Article£¬once mentioned of 2879-20-1

A simple procedure for the synthesis of 3-(substituted-sulfanyl)-4-hydroxy-6-substituted-pyran-2-ones

A series of 3-(substituted sulfanyl)-4-hydroxy-6-substituted-pyran-2-ones were synthesized for Human immunodeficiency virus-1 protease inhibition. These compounds were synthesized in a simple and convergent fashion to allow us a rapid preparation of many structurally diversified analogues. Thus the condensation of trimethylsilyl enol ethers of corresponding ketones, with 2-(S-substituted)propane-1,3-dioates afforded the corresponding pyrones in 24-70% isolated yields.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis, characterization and biological screening of some new sulfonamides derivatives of 1,4-benzodioxane-6-amine

In the present study, a series of N-substituted derivatives of 1,4-benzodioxane-6-amine have been synthesized. The reaction of 1,4-benzodioxane-6-amine (1) with various alkyl/aryl sulfonyl chlorides (2a-k) yielded N-alkyl/aryl sulfonamides (3a-k), which further on treatment with benzyl chloride (4) in the presence of sodium hydride furnished into N-benzylated sulfonamides (6a-k) while the reaction of 3a-k with ethyl iodide (5 ) yielded N-ethylated sulfonamides 7a-k. These derivatives were characterized by IR, 1H-NMR and EI-MS and then screened against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and lipoxygenase (LOX) enzymes and were found to be good inhibitors of lipoxygenase only. The interaction between inhibitors and target enzymes were computationally observed which correlates with the experimental results.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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PROLYL HYDROXYLASE ANTAGONISTS

This invention relates to certain 2-[(quinolin-3-yl)carbonyl]aminoacetic acid derivatives of formula (I), where the various groups are defined herein, and which are useful in treating anemia

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extracurricular laboratory:new discovery of 10288-72-9

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URACIL NUCLEOTIDE ANALOGUES, THEIR PREPARATION METHOD AND USE THEREOF

The invention relates to uracil nucleotide analogues, their preparation method and use thereof. Specifically, the invention provides the uracil nucleotide analogues with the formula (I), their stereoisomers and pharmaceutical acceptable salts, the preparation method and use. These compounds are RNA-dependent RNA viral replication inhibitors, and can be used as HCV NS5B polymerase inhibitors, HCV replication inhibitors as well as for the treatment of hepatitis C infection in mammals. They have broad application prospects and are expected to develop a new generation of antiviral drugs.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Pentafluorobenzenesulfonamides and analogs

The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents. The compositions include compounds of the general formula I: STR1

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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N-Bromosuccinimide as an efficient catalyst for the synthesis of indolo[2,3-b]quinolines

The use of N-bromosuccinimide as a catalyst promoted the synthesis of polycyclic indolo[2,3-b]quinoline derivatives in good to high yields in the reactions of various aryl amines with indole-3-carbaldehyde at room temperature under mild conditions.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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FUNGAL HYDROXYLATION OF ETHYL BENZENE AND DERIVATIVES

The fungus Mortierella isabellina converts ethyl benzene and a number of para-substituted derivatives to the corresponding optically active 1-phenylethanols with enantiomeric excesses between 5 and 40percent.Hydrogen removal from the substrate preceeds product formation and is stereochemically independent of it.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem