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SUBSTITUENT EFFECTS ON THE GAS PHASE BASICITIES OF ACETOPHENONES

The gas phase basicities of m- and p-substituted acetophenones have been determined by the ion cyclotron resonance (ICR) eqiulibrium constant method.The application of the LArSR Eq. to these substituent effects provides a rho=12.2 and an r+=0.76 with excellent precision.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2086O – PubChem

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2-Hydroxymethyl-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl] -1-benzenesulfonamide (DRF-4367): An orally active COX-2 inhibitor identified through pharmacophoric modulation

Analogs of 1,5-diarylpyrazoles with a novel pharmacophore at N1 were designed, synthesized and evaluated for the in-vitro cyclooxygenase (COX-1/COX-2) inhibitory activity. The variations at/around position-4 of the C-5 phenyl ring in conjunction with a CF3 and CHF2 groups at C-3 exhibited a high degree of potency and selectivity index (SI) for COX-2 inhibition. The in-vivo evaluation of these potent compounds with a few earlier ones indicated the 4-OMe-phenyl analog 6 and the 4-NHMe-phenyl analog 9 with a CF3, and the 4-OEt-phenyl analog 19 with a CHF2 group at C-3 to possess superior potency than celecoxib. In addition to its impressive anti-inflammatory, antipyretic, analgesic and anti-arthritic properties, compound 6 (DRF-4367) was found to possess an excellent pharmacokinetic profile, gastrointestinal (GI) safety in the long-term arthritis study and COX-2 potency in human whole blood assay. Thus, compound 6 was selected as an orally active anti-inflammatory candidate for pre-clinical evaluation.

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Benzofuran – Wikipedia,
Benzofuran | C8H2092O – PubChem

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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 90843-31-5, help many people in the next few years.Formula: C10H10O2

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Synthesis, and antitubercular and antimicrobial activity of 1?-(4-chlorophenyl)pyrazole containing 3,5-disubstituted pyrazoline derivatives

A new series of 1?-(4-chlorophenyl)-5-(substituted aryl)-3?-(substituted aryl)-3,4-dihydro-2H,1?H-[3,4?]bipyrazolyl derivatives (6a-e, 8a-e, 10a-e) have been synthesized, characterized and screened for antimicrobial and antitubercular activity. Among the synthesized compounds, the minimum inhibition concentration of 10e was found to be as low as 1.56 mug ml-1 and that of 10c was 6.25 mug ml-1 as compared to the standard anti-tb drugs pyrazinamide and streptomycin.

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Benzofuran – Wikipedia,
Benzofuran | C8H2080O – PubChem

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Substituted indoles and their use as integrin antagonists

The present invention relates to novel substituted indole compounds that are antagonists of alpha V (alphav) integrins, for example alphavbeta3 and alphavbeta5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by alphavbeta3 and alphavbeta5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: 1where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.

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Benzofuran – Wikipedia,
Benzofuran | C8H2067O – PubChem

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Design, synthesis and structure-activity relationship studies of novel and diverse cyclooxygenase-2 inhibitors as anti-inflammatory drugs

Because of the pivotal role of cyclooxygenase (COX) in the inflammatory processes, non-steroidal anti-inflammatory drugs (NSAIDs) that suppress COX activities have been used clinically for the treatment of inflammatory diseases/syndromes; however, traditional NSAIDs exhibit serious side-effects such as gastrointestinal damage and hyper sensitivity owing to their COX-1 inhibition. Also, COX-2 inhibition-derived suppressive or preventive effects against initiation/proliferation/invasion/motility/recurrence/metastasis of various cancers/tumours such as colon, gastric, skin, lung, liver, pancreas, breast, prostate, cervical and ovarian cancers are significant. In this study, design, synthesis and structure-activity relationship (SAR) of various novel {2-[(2-, 3- and/or 4-substituted)-benzoyl, (bicyclic heterocycloalkanophenyl)carbonyl or cycloalkanecarbonyl]-(5- or 6-substituted)-1H-indol-3-yl}acetic acid analogues were investigated to seek and identify various chemotypes of potent and selective COX-2 inhibitors for the treatment of inflammatory diseases, resulting in the discovery of orally potent agents in the peripheral-inflammation model rats. The SARs and physicochemical properties for the analogues are described as significant findings. For graphical abstract: see Supplementary Material. (www.informahealthcare.com/enz)

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2082O – PubChem

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of 5-Acetyl-2,3-dihydrobenzo[b]furan, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 90843-31-5, in my other articles.

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 5-Acetyl-2,3-dihydrobenzo[b]furan, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 90843-31-5, Name is 5-Acetyl-2,3-dihydrobenzo[b]furan, molecular formula is C10H10O2

GLYCOSIDASE INHIBITORS

Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer’s disease.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of 5-Acetyl-2,3-dihydrobenzo[b]furan, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 90843-31-5, in my other articles.

Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2063O – PubChem

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Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)- ethyl acrylamides

Bioisosteric replacement studies led to the identification of N-(1-benzo[1,3]dioxol-5-yl-ethyl)-3-(2-chloro-phenyl)-acrylamide ((S)-3) as a highly potent KCNQ2 opener, and 3-(2,6-difluoro-phenyl)-N-[1-(2,3-dihydro- benzofuran-5-yl)-ethyl]-acrylamide ((S)-4), and N-[1-(2,3-dihydro-1H-indol-5-yl) -ethyl]-3-(2-fluoro-phenyl)-acrylamide ((S)-5) as highly efficacious KCNQ2 openers. In contrast, their respective R enantiomers showed significantly less or no appreciable KCNQ2 opener activity even at the highest concentration tested (10muM). Because of its high potency and moderate efficacy as well as its convenient synthesis, (¡À)-3 was selected as a reference compound for analyzing efficacies of KCNQ openers in electrophysiology studies. Compounds (S)-4 and (S)-5 demonstrated significant activity in reducing neuronal hyperexcitability in rat hippocampal slices. The synthesis and the KCNQ2 opener activity of these acrylamides are described.

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Benzofuran – Wikipedia,
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Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins

A series of novel tricyclic triazine-di-N-oxides (TTOs) related to tirapazamine have been designed and prepared. A wide range of structural arrangements with cycloalkyl, oxygen-, and nitrogen-containing saturated rings fused to the triazine core, coupled with various side chains linked to either hemisphere, resulted in TTO analogues that displayed hypoxia-selective cytotoxicity in vitro. Optimal rates of hypoxic metabolism and tissue diffusion coefficients were achieved with fused cycloalkyl rings in combination with both the 3-aminoalkyl or 3-alkyl substituents linked to weakly basic soluble amines. The selection was further refined using pharmacokinetic/pharmacodynamic model predictions of the in vivo hypoxic potency (AUCreq) and selectivity (HCD) with 12 TTO analogues predicted to be active in vivo, subject to the achievement of adequate plasma pharmacokinetics.

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Benzofuran – Wikipedia,
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4,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES

The present invention relates to a compounds of formula I wherein R1, R1”, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (beta-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated beta-amyloid levels or beta-amyloid deposits, particularly Alzheimer”s disease.

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Benzofuran – Wikipedia,
Benzofuran | C8H2060O – PubChem

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Related Products of 90843-31-5, 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, 90843-31-5, molcular formula is C10H10O2, introducing its new discovery.

One-pot three-component reactions of methyl ketones, phenols and a nucleophile: An expedient way to synthesize densely substituted benzofurans

Three-component reactions of phenylglyoxal monohydrate, phenols, and indoles were developed with the aid of acid-catalyst, which produced various densely substituted benzofurans with good to excellent yields. On the basis of this observation, a one-pot, step-wise reaction was developed by using methyl ketones instead of using phenylglyoxal component in I2/DMSO system. At last, three-component reaction offered a useful way to synthesize densely substituted benzofurans starting from simple and easily available substrates. The indole component can be replaced by some other nucleophiles, such as 1,2,4-trimethoxybenzene and thiophenol.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H2076O – PubChem