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5-Bromo-N-[4-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-butyl)]-2, 3-dimethoxybenzamide 1 is a potent and selective sigma2 receptor ligand suitable for further development. A series of new analogues, incorporating a variety of isoquinoline and carboxylic acid moieties, linked together with either a linear or cyclic amine spacer have been synthesised and assessed for their sigma1/sigma2 binding affinity and selectivity. Compounds with a rigid piperidine spacer gave Ki values for the sigma2 receptor between 8.7-845 nM. Changing the configuration of the methoxy groups on the isoquinoline moiety resulted in molecules with sigma2Ki values of 4.4-133 nM whereas varying the length and flexibility of the carbon spaces gave sigma2Ki values 0.88-15.0 nM, some of the most active, selective sigma2 ligands to date. Thus, the flexibility and length of the carbon linker and the carboxylic acid moiety are confirmed to be key to the exceptional binding affinity and selectivity for this active series. Additionally, the incorporation of a halogen on selected carboxylic acid moieties provided a convenient strategy for the introduction of a radiohalogen for applications in pharmacological and imaging studies.

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Benzofuran – Wikipedia,
Benzofuran | C8H1727O – PubChem

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The invention belongs to the field of medical technology, relates to the general formula I indicated by the amide pyridine derivatives, its stereoisomers and its pharmaceutically acceptable salt, hydrate, solvate or prodrug, wherein substituent Ar, M, R, Py has the definition given in the specification. The invention also relates to processes for preparing formula I compounds, pharmaceutical compositions containing the above-mentioned compound and the above compounds and pharmaceutical compositions used for the preparation of the treatment and prevention of shallow fungi and deep fungal diseases use in medicine. (by machine translation)

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A metal-free C-H oxidation for the construction of allylic esters has been developed. The use of a commercially available and inexpensive catalyst and oxidant, and readily available starting materials, coupled with the operational simplicity of the reaction, renders the methodology a useful alternative to other approaches typically employed in the synthesis of allylic esters.

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Carbonaceous nanomaterials (multi-walled carbon nanotubes (MWCNTs), graphene, and graphene oxide (GO)) have attracted attention over the last decade as adsorbents suitable for the analysis of organic and inorganic pollutants. In the present paper we review methods of mycotoxin analysis that involve sample extraction with carbonaceous nanosorbents, reported from 2011 onwards. Recent studies have highlighted the advantages of magnetically modified MWCNTs and GO in mycotoxin analysis, which may enable sample isolation through magnetic separation, reduce the interaction of nanoparticles, and enhance the recovery of analytes. The papers covered in this review point to promising applications of functionalised carbonaceous nanosorbents in mycotoxin analysis. While GO based sorbents can be effective for the adsorption of relatively polar aflatoxins, MWCNTs with high specific surface area and reduced agglomeration achieved through modification with silica and magnetic particles are preferred for the extraction of less polar mycotoxins.

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This manuscript describes the preparation of new small molecule inhibitors of Bacillus anthracis lethal factor. Our starting point was the symmetrical, bis-quinolinyl compound 1 (NSC 12155). Optimization of one half of this molecule led to new LF inhibitors that were desymmetrized to afford more drug-like compounds.

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Benzofuran – Wikipedia,
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Provided herein are quinolines, e.g., a compound of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurological disease, neurodegenerative disorder, or diabetes. Also provided herein are methods of their use for modulating the activity of a sarcoplasmic/endoplasmic reticulum C2+ ATPase.

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Benzofuran – Wikipedia,
Benzofuran | C8H1644O – PubChem

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Plant disease caused by soil-borne fungus Gaeumannonyces graminis (Gg) is controlled by applying to the seed or the soil a fungicide which has the following general formula: STR1

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Benzofuran – Wikipedia,
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Provided herein are quinolines, e.g., a compound of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurological disease, neurodegenerative disorder, or diabetes. Also provided herein are methods of their use for modulating the activity of a sarcoplasmic/endoplasmic reticulum C2+ ATPase.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1644O – PubChem

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A variety of aromatic and aliphatic carboxylic acids were smoothly converted into the corresponding nitriles in good yields in a one-pot procedure by treatment with ethyl iodide/K2CO3/18-crown-6, followed by sodium diisobutyl-tert-butoxyaluminium hydride (SDBBA-H), and finally treatment with molecular iodine or 1,3-diiodo-5,5-dimethylhydantoin (DIH), and aqueous ammonia. This method is useful for the conversion of various aromatic and aliphatic carboxylic acids into the corresponding nitriles in a one-pot procedure. A variety of aromatic and aliphatic carboxylic acids were smoothly converted into the corresponding nitriles in good yields in a one-pot procedure by treatment with ethyl iodide/K2CO3/18-crown-6, followed by sodium diisobutyl-tert-butoxyaluminium hydride (SDBBA-H), and finally treatment with molecular iodine or 1,3-diiodo-5,5-dimethylhydantoin (DIH), and aqueous ammonia. Copyright

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Benzofuran – Wikipedia,
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The emergence of drug-resistant HIV from a widespread antiviral chemotherapy targeting HIV protease in the past decades is unavoidable and provides a challenge to develop alternative inhibitors. We synthesized a series of allophenylnorstatine-based peptidomimetics with various P3, P2, and P2 moieties. The derivatives with P2 tetrahydrofuranylglycine (Thfg) were found to be potent against wild type HIV-1 protease and the virus, leading to a highly potent compound 21f (KNI-1657) against lopinavir/ritonavir- or darunavir-resistant strains. Co-crystal structures of 21f and the wild-type protease revealed numerous key hydrogen bonding interactions with Thfg. These results suggest that the strategy to design allophenylnorstatine-based peptidomimetics combined with Thfg residue would be promising for generating candidates to overcome multidrug resistance.

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