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Benzofuran derivatives are the scaffold of many natural products, many of which are biologically active and/or found to have high potential as pharmacological agents. Therefore, benzofuran derivatives are expected to be invaluable moieties as far as biology and pharmacology are concerned. In this review, we try to highlight the recent advances in the synthetic approaches to a wide variety of its derivatives in particular those showing biological activity.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H415O – PubChem

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LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H426O – PubChem

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Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“”ABC””) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“”CFTR””). The present invention also relates to methods of treating CFTR mediated diseases using compounds of the present invention.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H398O – PubChem

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Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H405O – PubChem

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The lead identification of a novel potent selective PPARgamma agonist, DS-6930 is reported. To avoid PPARgamma-related adverse effects, a partial agonist was designed to prevent the direct interaction with helix 12 of PPARgamma-LBD. Because the TZD group is known to interact with helix 12, the TZD in efatutazone (CS-7017) was replaced to discover novel PPARgamma intermediate partial agonist 8i. The optimization of 8i yielded 13ac with high potency in vitro. Compound 13ac exhibited robust plasma glucose lowering effects comparable to those of rosiglitazone (3 mg/kg) in Zucker diabetic fatty rats. Upon toxicological evaluation, compound 13ac (300 mg/kg) induced hemodilution to a lower extent than rosiglitazone; however, 13ac elevated liver enzyme activities. X-ray crystallography revealed no direct interaction of 13ac with helix 12, and the additional lipophilic interactions are also suggested to be related to the maximum transcriptional activity of 13ac.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H422O – PubChem

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Application of 13196-11-7, 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, 13196-11-7, Benzofuran-6-ol, introducing its new discovery.

The Palladium catalysed cross coupling of 2-halo- or metallo-benzofurans with both 5-metallo- or halo-resorcinol tricarbonyl chromium(O)complexes and the uncomplexed resorcinols, has been evaluated and in consequence, moracin M has been synthesised in good yield by the cross coupling of 6-(t-butyldiphenylsiloxy)-2-trimethylstannylbenzofuran with 5-iodoresorcinolbis(triisopropylsilyl) ether and fluoride ion deprotection of the product.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H411O – PubChem

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Enzymatic cis-dihydroxylation of benzo[b]thiophene, benzo[b]furan and several methyl substituted derivatives was found to occur in both the carbocyclic and heterocyclic rings. Relative and absolute configurations and enantiopurities of the resulting dihydrodiols were determined. Hydrogenation of the alkene bond in carbocyclic cis-dihydrodiols and ring-opening epimerization/reduction reactions of heterocyclic cis/trans-dihydrodiols were also studied. The relatively stable heterocyclic dihydrodiols of benzo[b]thiophene and benzo[b]furan showed a strong preference for the trans configuration in aqueous solutions. The 2,3-dihydrodiol metabolite of benzo[b]thiophene was utilized as a precursor in the chemoenzymatic synthesis of the unstable arene oxide, benzo[b]thiophene 2,3-oxide.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H409O – PubChem

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Benzofuran derivatives and benzofuransare presented as scaffolds in complex molecules and have attracted much attention and prevalent interest due to their interesting biological activity. They also exist in several numbers of naturally occurring compounds and exhibiting biological activity. In this review, we will try to underscore the reactivity of benzofurans through comprehension and giving a full perspective to the readers.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H416O – PubChem

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Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 18F, 123I, 124I, 125I, or 11C. Also provided are in vivo techniques for using these and other tracers as analytical and diagnostic tools to study sulfotransferase distribution and activity, in health and disease, and to evaluate therapeutic interventions.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H396O – PubChem

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Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are various substituent groups; andone of X1 and X2 is N or CR?, and the other is NR? or CHR? wherein R? is hydrogen, OH, C1-6alkyl, or C3-7cycloalkyl; or when one of X1 and X2 is N or CR? then the other may be S or O;and their use as pharmaceuticals.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H400O – PubChem