Archives for Chemistry Experiments of Methyl 4-bromobenzo[b]thiophene-2-carboxylate

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Spirolactam-based acetyl-CoA carboxylase inhibitors: Toward improved metabolic stability of a chromanone lead structure

Acetyl-CoA carboxylase (ACC) catalyzes the rate-determining step in de novo lipogenesis and plays a crucial role in the regulation of fatty acid oxidation. Alterations in lipid metabolism are believed to contribute to insulin resistance; thus inhibition of ACC offers a promising option for intervention in type 2 diabetes mellitus. Herein we disclose a series of ACC inhibitors based on a spirocyclic pyrazololactam core. The lactam series has improved chemical and metabolic stability relative to our previously reported pyrazoloketone series, while retaining potent inhibition of ACC1 and ACC2. Optimization of the pyrazole and amide substituents led to quinoline amide 21, which was advanced to preclinical development.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

New explortion of 6-Chlorobenzo[b]thiophene-2-carboxylic acid

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Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor

The blood coagulation enzyme factor Xa (FXa) is a particularly promising target for anticoagulant therapy, and identification of oral small-molecule inhibitors of FXa remains a research focus. On the basis of the X-ray crystal structure of FXa and its inhibitor rivaroxaban, we designed and synthesized a series of conformationally restricted mimics containing a novel [6,6,5] tricyclic fused oxazolidinone scaffold. Intensive structure-activity relationship (SAR) and structure-pharmacokinetic relationship (SPR) studies on this new series led to the discovery of compound 11a: a highly potent, selective, direct, and orally bioavailable FXa inhibitor with excellent in vivo antithrombotic efficacy and preferable pharmacokinetic profiles. Druggability evaluation of compound 11a was undertaken and elicited positive outcomes. All results indicate that compound 11a is a promising drug candidate for the prevention and treatment of thromboembolic diseases in venous and arterial systems.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Awesome and Easy Science Experiments about 7-Fluorobenzo[b]thiophene

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USE OF HISTONE DEACETYLASE INHIBITORS FOR THE CARE OF PHILADELPHIA-NEGATIVE MYELOPROLIFERATIVE SYNDROMES

The use of substances capable of inhibiting one or more enzymes of the histone deacetylase family (histone deacetylase inhibitors) for the therapeutic treatment of Philadelphia-negative myeloproliferative syndromes (polyeythemia vera, essential thrombocythemia or idiopathic myelotibrosis) is described. The dosage of the above-mentioned substances is significantly lower than that normally used for the care of other tumour syndromes and may be from 10 to 150 mg/day/patient.

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Benzothiophene – Wikipedia,
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Brief introduction of 22913-24-2

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Related Products of 22913-24-2, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 22913-24-2, Name is Methyl benzo[b]thiophene-2-carboxylate, molecular formula is C10H8O2S. In a Article£¬once mentioned of 22913-24-2

Benzo[b]thiophene-2-carboxamide derivatives as potent urotensin-II receptor antagonists

Members of a series of benzo[b]thiophene-2-carboxamide derivatives, possessing an N-(1-(3-bromo-4-(piperidin-4-yloxy)benzyl)piperidin-4-yl) group, were synthesized and evaluated as urotensin-II receptor antagonists. The results show that these substances have potent UT binding affinities. Observations made in a systematic SAR investigation of the effects of a variety of substituents (R1and R2) at the 5- and 6-positions in the benzo[b]thiophene-2-carboxamide moiety on UT binding affinities led to identification of the 5-cyano analog 7f as a highly potent UT antagonist with an IC50value of 25?nM. Despite having a good metabolic stability, 7f is a potent inhibitor of CYP isozyme and displays an unsuitable PK profile.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

A new application about 6-Methylbenzo[b]thiophene

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Application of directed metalation in synthesis. Part 4: Expedient synthesis of substituted benzo[b]thiophene and naphthothiophene

A short, simple and inexpensive synthesis of several diversely substituted benzo[b]thiophenes and one naphthothiophene is described. The method involves introduction of methylsulfanyl group ortho- to the amide function of readily available N,N-diethylamides of aryl carboxylic acid by directed metalation. Thioindoxyls, obtained in high yields through side-chain deprotonation and cyclisation in one pot, are reduced to benzo[b]thiophene or napthothiophene.

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Extended knowledge of 17402-83-4

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Towards the development of an in vivo chemical probe for cyclin G associated kinase (GAK)

SGC-GAK-1 (1) is a potent, selective, cell-active chemical probe for cyclin G-associated kinase (GAK). However, 1 was rapidly metabolized in mouse liver microsomes by cytochrome P450-mediated oxidation, displaying rapid clearance in liver microsomes and in mice, which limited its utility in in vivo studies. Chemical modifications of 1 that improved metabolic stability, generally resulted in decreased GAK potency. The best analog in terms of GAK activity in cells was 6-bromo-N-(1H-indazol-6-yl)quinolin-4-amine (35) (IC50 = 1.4 muM), showing improved stability in liver microsomes while still maintaining a narrow spectrum activity across the kinome. As an alternative to scaold modifications we also explored the use of the broad-spectrum cytochrome P450 inhibitor 1-aminobenzotriazole (ABT) to decrease intrinsic clearance of aminoquinoline GAK inhibitors. Taken together, these approaches point towards the development of an in vivo chemical probe for the dark kinase GAK.

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Benzothiophene – Wikipedia,
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Extended knowledge of Benzo[b]thiophen-5-ol

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BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES

The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

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Benzothiophene – Wikipedia,
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Archives for Chemistry Experiments of 4923-87-9

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Nickel-catalyzed cyanation of aryl halides and triflates using acetonitrile: Via C-CN bond cleavage assisted by 1,4-bis(trimethylsilyl)-2,3,5,6-tetramethyl-1,4-dihydropyrazine

We developed a non-toxic cyanation reaction of various aryl halides and triflates in acetonitrile using a catalyst system of [Ni(MeCN)6](BF4)2, 1,10-phenanthroline, and 1,4-bis(trimethylsilyl)-2,3,5,6-tetramethyl-1,4-dihydropyrazine (Si-Me4-DHP). Si-Me4-DHP was found to function as a reductant for generating nickel(0) species and a silylation reagent to achieve the catalytic cyanation via C-CN bond cleavage.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

The Absolute Best Science Experiment for 63675-74-1

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. name: 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 63675-74-1, name is 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene. In an article£¬Which mentioned a new discovery about 63675-74-1

Diarylvinyl sulfoxides

The present invention is directed to new diarylvinyl sulfoxides.

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Benzothiophene | C8H6S – PubChem

 

Awesome and Easy Science Experiments about 5-Bromobenzothiophene

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Pyruvate enolate arylation and alkylation: OBO ester protected pyruvates as useful reagents in organic synthesis

A protected pyruvate equivalent is described that allows arylation and arylation/alkylation reactions to be performed at the methyl group. Utilization of the OBO derivative of the pyruvate ester allowed the application of palladium catalyzed arylation reactions together with subsequent alkylation, under basic conditions. Moreover, the OBO protecting group could be easily removed in one step to provide access to a wide range of substituted pyruvate derivatives.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem