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The catecholaminergic and serotoninergic neurons in the brain change their performance according to the physiological need via a catecholaminergic/serotoninergic activity enhancer (CAE/SAE) mechanism. Phenylethylamine (PEA), tyramine and tryptamine are the presently known endogenous CAE/SAE substances which enhance the impulse propagation mediated release of catecholamines and serotonin in the brain. A PEA derivative, (-)deprenyl (selegiline), known as a selective inhibitor of MAO-B, is for the time being the only CAE/SAE substance in clinical use. Aiming to develop a selective CAE/SAE substance much more potent than (-)deprenyl, a series of new 1-aryl-2-alkylaminoalkanes, structurally unrelated to PEA and the amphetamines, was designed and prepared. Among them, (-)1-(benzofuran-2-yl)-2-propylaminopentane ((-)BPAP) was selected as a promising candidate substance for further studies. (-)BPAP significantly enhanced in rats the impulse propagation mediated release of catecholamines and serotonin in the brain 30 min after acute injection of 0.36 nmol/kg sc. In the shuttle box, (-)BPAP was in rats about 130 times more potent than (-)deprenyl in antagonizing tetrabenazine induced inhibition of performance. (±)BPAP protected cultured hippocampal neurons from the neurotoxic effect of beta-amyloid in 10-14-10-15 M concentration.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1124O – PubChem

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New furan derivatives of o-divinylbenzenes were synthesized and their photochemical reactivity has been investigated in neutral and acidic medium. Depending of the structure of the starting materials and pH value, the new cyclization (11, 16, 20), cycloaddiotion (12, 13, endo-17, exo-18), electrocyclization (21, 22) and dimeric (15, 19) products were isolated. While photochemical investigation in neutral medium showed that the main intramolecular process is cycloaddition, in the case of acidic photochemistry, due to the protonation of the starting molecule, electrocyclization process comes to expression and formation of dihydronaphtalene products 21 and 22.

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Reference:
Benzofuran – Wikipedia,
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To explore the structure-activity relationships (SAR) of demethylvancomycin (2) and find more effective new chemical entities than known glycopeptides for the treatment of Clostridium difficile (C. difficile), 17 novel N-substituted (N-arylmethylene or -aliphatic substituents) demethylvancomycin derivatives were prepared. These analogues have been evaluated in vitro for their antibacterial activities against C. difficile and Enterococcus faecium (E. faecium). Compounds 5d, 5h, and 5i with N-arylmethylene substituents, structurally similar to Oritavancin, showed more potent antibacterial activity against C. difficile than vancomycin (1) or demethylvancomycin (2). Meanwhile, compound 5k with an undecyl side chain showed the most potent antibacterial activity against E. faecium (vancomycin-resistant strain).

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Benzofuran – Wikipedia,
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(Chemical Equation Presented) The Mukayiama aldol reaction of aldehydes is efficiently accomplished with a low concentration of the dimeric alumatrane catalyst 2 at mild or subambient temperatures. Our protocol tolerates a wide variety of electron-rich, neutral, and deficient aryl, alkyl, and heterocyclic aldehydes. A wide variety of enol silyl ethers are also tolerated. An intermediate that was isolated provides mechanistic information regarding the role of dimeric 2 in the Mukaiyama aldol reaction. Experimental evidence is presented for the stronger Lewis acidity of 5 compared with F3B.

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Benzofuran – Wikipedia,
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The present invention relates to Fluoromalonyl Halfthioesters (F-MAHTs) of formula (I), wherein R1 represents hydrogen, halogen, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group; and R2 represents an optionally substituted aryl group, an optionally substituted cycloalkyl group, an optionally substituted heteroaryl group, an optionally substituted heterocyclyl group; an optionally substituted alkyl group. The invention further relates to their synthesis and to their use, particularly as masked fluoroacetates in the preparation of pharmaceutical active ingredients.

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Benzofuran – Wikipedia,
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In order to explore new furan-based functional materials, investigate the effect of the degree of branching on their optoelectronic properties and search for three-dimensional organic semiconductors from planar pi-conjugated molecules, the compounds 1,4-bis[2-(benzofuran-2-yl)vinyl]benzene (2BFVB) with a linear shape, 1,3,5-tris[2-(benzofuran-2-yl)vinyl]benzene (3BFVB) with a star shape and 1,2,4,5-tetra[2-(benzofuran-2-yl)vinyl]benzene (4BFVB) with a cruciform shape were synthesized and compared. 2BFVB adopts a two-dimensional herringbone packing motif and there are two kinds of molecular conformation. The crystal packing of 3BFVB is more sensitive to the crystallization conditions. Two single-crystal phases and one thin-film phase were found. 3BFVB (beta-phase) molecules pack into a three-dimensional cofacial herringbone structure. 4BFVB forms an inter-inserted two-dimensional hexagonal packing structure. The molecular shape and aggregate packing exert remarkable effects on the optoelectronic properties. The quantum yield of 2BFVB is very high both in the solution (74%) and in the crystalline solid (76%) states. The high solid emission efficiency of 2BFVB is possibly related to the two molecular conformations in the herringbone-arranged H-aggregates. Both 2BFVB and 3BFVB display hole-transport abilities. The performance of 3BFVB amorphous film is nearly equal to that of its crystalline film, which would be helpful in simplifying device fabrication. This study shows that the substitution degree exerts drastic effects on solubility, polymorphism, crystal packing and optoelectronic properties. the Partner Organisations 2014.

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Benzofuran – Wikipedia,
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The analytical colour reaction of iminodibenzyl with hetaryl/aryl aldehydes was studied in detail to clarify the mechanism of the reaction path. On the basis of synthetic and structural analytical investigations iminodibenzyl-aryl/hetaryl-carbenium ions were found to be the decisive products responsible for the colour reaction. In order to analyse the scope and limitations of this aromatic electrophilic substitution reaction some related aniline derivatives with different nucleophilicity were also investigated by reaction with furan-2-carbaldehyde. In this context new 4,5- diamino-2-cyclopenten-1-ones were formed and characterized which gave rise to valuable structural information concerning the aniline/furan-2-carbaldehyde colour reaction frequently used in the analytical chemistry of aminoglycoside antibiotics.

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Benzofuran – Wikipedia,
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The synthesis of (S)-2-(4-tert-butylphenoxy)-3-(benzoxazol-5-yl) propanoic acid derivatives (2a-k) were described and their in vitro antibacterial activities were determined against Gram-negative and -positive bacteria. These compounds were found to exert a broad spectrum of activity against the screened bacteria, but poor MIC values were found for Candida albicans fungi. Compound 2b bearing a hydrophobic aromatic tie was the most active derivative against all bacteria studied with MIC values ranging from 0.098 to 0.78 mug/mL. The activity of 2b against B. subtilis was 2-fold higher than Penicillin, and 8- to 510-fold higher than other control antibiotics.

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Benzofuran – Wikipedia,
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An improved synthesis of gamma-hydroxybutenolides 1a – d was achieved via crossed aldol condensation between aldehydes 2a – d and the protected gamma-hydroxy-beta-methylbutenolides 3 or 4 using the bulky Lewis acid, aluminum tris(2,6-diphenylphenoxide) (ATPH). Using this same methodology, the gamma-hydroxybutenolides 17a – d having various heteroaromatic rings were synthesized and their anti-tumor activities were evaluated.

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Benzofuran – Wikipedia,
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Two oxathiozolidine-S-oxide templates have been developed and used in a four-component coupling protocol for the synthesis of a wide range of chiral sulfinimines in high enantiomeric excesses. The templates can be synthesized from cheap commodity chemicals in three steps in high yields. Furthermore the template is easily recovered in high yields for recycling.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1021O – PubChem