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The novel compounds of formula (I) of the instant invention are selective kappa opioid agonists useful in the treatment of arthritis, hypertension, pain, inflammation, migraine, inflammatory disorders of the gastrointestinal tract, IBS, and psoriasis. The compounds, novel intermediates useful in their preparations and pharmaceutical compositions containing them, are part of the invention. STR1

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Benzofuran – Wikipedia,
Benzofuran | C8H2654O – PubChem

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A series of acyloxyalkyl and amidooxyalkyl ketones appended to a carbobenzyloxy aspartic acid core have been prepared. The most potent of these new inhibitors was 4i with a Ki of 0.5 muM. These two series provide an improved understanding of the binding requirements for the hydrophobic prime side of ICE.

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Benzofuran – Wikipedia,
Benzofuran | C8H2667O – PubChem

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Cycloaddition chemistry of 2-vinyl-substituted indoles and related heteroaromatic systems

(Chemical Equation Presented) The intramolecular Diels-Alder cycloaddition reaction (IMDAF) of several N-phenylsulfonylindolyl-substituted furanyl carbamates containing a tethered pi-bond on the indole ring were examined as an approach to the iboga alkaloid catharanthine. Only in the case where the tethered pi-bond contained two carbomethoxy groups did the [4 + 2]-cycloaddition occur. Push-pull dipoles generated from the Rh(II)-catalyzed reaction of diazo imides, on the other hand, undergo successful intramolecular 1,3-dipolar cycloaddition across both alkenyl and heteroaromatic pi-bonds to provide novel pentacyclic compounds in good yield and in a stereocontrolled fashion. The facility of the cycloaddition was found to be critically dependent on conformational factors in the transition state. Ligand substitution in the rhodium(II) catalyst markedly altered the product ratio between [3 + 2]-cycloaddition and intramolecular C-H insertion. The variation in reactivity reflects the difference in electrophilicity between the various rhodium carbenoid intermediates. Intramolecular C-H insertion is enhanced with the more electrophilic carbene generated using Rh(II) perfluorobutyrate.

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Benzofuran – Wikipedia,
Benzofuran | C8H2676O – PubChem

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Reference of 64175-51-5, 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, 64175-51-5, molcular formula is C10H8O3, introducing its new discovery.

Syntheses of Furano Compounds: Part XLIV. Syntheses of 2-CarboxybenzoFuran-3-Acetic Acid and 3-CarboxybenzoFuran-2-Acetic Acid

1-Carboxybenzofuran-3-acetic acid and 3-carboxybenzofuran-acetic acid have been synthesised. A new synthesis of benzofuran-3-acetic acid, a plant hormone is reported.

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Benzofuran – Wikipedia,
Benzofuran | C8H2659O – PubChem

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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, 64175-51-5, name is 2-(Benzofuran-3-yl)acetic acid, introducing its new discovery. name: 2-(Benzofuran-3-yl)acetic acid

Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of mycobacterium tuberculosis inha

Tuberculosis (TB) is one of the world’s oldest and deadliest diseases, killing a person every 20 s. InhA, the enoyl-ACP reductase from Mycobacterium tuberculosis, is the target of the frontline antitubercular drug isoniazid (INH). Compounds that directly target InhA and do not require activation by mycobacterial catalase peroxidase KatG are promising candidates for treating infections caused by INH resistant strains. The application of the encoded library technology (ELT) to the discovery of direct InhA inhibitors yielded compound 7 endowed with good enzymatic potency but with low antitubercular potency. This work reports the hit identification, the selected strategy for potency optimization, the structure-activity relationships of a hundred analogues synthesized, and the results of the in vivo efficacy studies performed with the lead compound 65.

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Benzofuran – Wikipedia,
Benzofuran | C8H2665O – PubChem

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Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase

We report comprehensive structure-activity relationship studies on a novel series of c-Jun N-terminal kinase (JNK) inhibitors. Intriguingly, the compounds have a dual inhibitory activity by functioning as both ATP and JIP mimetics, possibly by binding to both the ATP binding site and to the docking site of the kinase. Several of such novel compounds display potent JNK inhibitory profiles both in vitro and in cell.

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Benzofuran – Wikipedia,
Benzofuran | C8H2662O – PubChem

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BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY

The present invention relatesto a pharmaceutical composition comprising acompound of the formula Ias described belowor a tautomeror a pharmaceutically acceptable salt thereof; to the compound of the formula Ias described below or a tautomer or a phar- maceutically acceptable salt thereof for use as a medicament, especially for use in the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization, and to certain novel compoundsof the formula Ias described below or a tautomer or a pharmaceuti- cally acceptable salt thereof. Formula (I) wherein X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; X4 is CR4 or N; with the proviso that at most two of X1, X2, X3 and X4 are N; L1, L2 are a bond or a bivalent radical such as C1-C6-alkylene or C3-C8-cycloalkylene; A is 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated carbocyclic ring which may carry one or more substituents R9; or L2-A forms a group C1-C6-alkylene-OR13, C1-C6-alkylene-SR14 or C1-C6-alkylene-NR15R16; and R1, R2, R3, R4, R5, R6, R9, R13, R14, R15 and R16 are as defined in the claims and the description.

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Benzofuran – Wikipedia,
Benzofuran | C8H2657O – PubChem

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Condensed pyridine bases. Synthesis and reactions of benzofuro[2,3-c] indeno[2,1-e]-, benzothieno[2,3-c]indeno[2,1-e]-, benzofuro-[3,2-c]indeno[2,1-e] – and thieno[2,3:4?,5?]-thieno[3,2-c]indeno[2,1-e]pyridines

Condensation of hetarene carboxaldehydes with phthalide gave 2-(3-hydroxy-1-oxoinden-2-yl)benzo[b]furan and 2-(3-hydroxy-1-oxoinden-2-yl)-5- ethylthieno[2,3-b]thiophene. Starting from hetaryl acetic acids gave 3-(3-hydroxy-1-oxoinden-2-yl)benzo[b]furan and 3-(3-hydroxy-1-oxoinden-2-yl) benzo[b]thiophene. Acylation of 3-hydroxy-1-oxoinden-2-yl-substituted heterocycles using acetic anhydride in the presence of 70% HClO4 leads to the formation of pentacyclic pyrilium salts. Pentacyclic indenopyridines are prepared by treating the pyrilium salts with ammonia. The reaction of the carbonyl group in the indenopyridines with hydroxylamine, hydrazine hydrate, and in reduction using NaBH4 has been studied.

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Design and synthesis of tailored human caseinolytic protease P inhibitors

Human caseinolytic protease P (hClpP) is important for degradation of misfolded proteins in the mitochondrial unfolded protein response. We here introduce tailored hClpP inhibitors that utilize a steric discrimination in their core naphthofuran scaffold to selectively address the human enzyme. This novel inhibitor generation exhibited superior activity compared to previously introduced beta-lactones, optimized for bacterial ClpP. Further insights into the bioactivity and binding to cellular targets were obtained via chemical proteomics as well as proliferation- and migration studies in cancer cells.

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Benzofuran – Wikipedia,
Benzofuran | C8H2668O – PubChem