Simple exploration of 3-Hydroxytetrahydrofuran

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CYCLOALKYLOXY-AND HETEROCYCLOALKYLOXYPYRIDINE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR

Certain cycloalkyloxy- and heterocycloalkyloxypyridine compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Esters of l-dopa: structure-hydrolysis relationships and ability to induce circling behaviour in an experimental model of hemiparkinsonism

A number of carboxylate esters of L-dopa, some of which are novel, were examined for their physicochemical and biological properties. A few esters of tyrosine and phenylalanine were included for comparison. The compounds displayed great differences in their lipophilicity and stability towards chemical and enzymatic (human plasma) hydrolysis. Within subseries, relationships exist between structural properties and rate constants of chemical or enzymatic hydrolysis. In an experimental model of hemiparkinsonism (circling behaviour in rats), some of the L-dopa esters (the isopropyl, sec-butyl and 2-(tetrahydropyranyl)methyl esters) showed an activity distinctly greater than that of L-dopa, although the difference was not statistically significant.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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C-O bond hydrogenolysis of cyclic ethers with OH groups over rhenium-modified supported iridium catalysts

Hydrogenolysis of tetrahydrofurfuryl alcohol to 1,5-pentanediol and other related substrates such as 3-hydroxytetrahydrofuran and 1,2-cyclohexanediol proceeds over Ir-ReOx/SiO2 catalyst. TOF values are higher than those of Rh-ReOx/SiO2, which has been reported to be an effective catalyst. The selectivity to the product, where the C-O bond neighboring the C-OH group in the substrate is dissociated, is comparable to or higher than that of Rh-ReOx/SiO2. Hydrogenolysis of most substrates except 1,2-cyclohexanediol proceeds via the direct mechanism where hydride species formed from hydrogen molecule attacks the anti-position of C-O bond. In the case of hydrogenolysis of 1,2-cyclohexanediol where attack of anti-position of C-O bond is unfavorable, indirect mechanism involving dehydrogenation to 2-hydroxycyclohexanone is responsible for the formation of cyclohexanol.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Design and synthesis of orally bioavailable 4-methyl heteroaryldihydropyrimidine based hepatitis B virus (HBV) capsid inhibitors

Targeting the capsid protein of hepatitis B virus (HBV) and thus interrupting normal capsid formation have been an attractive approach to block the replication of HBV viruses. We carried out multidimensional structural optimizations based on the heteroaryldihydropyrimidine (HAP) analogue Bay41-4109 (1) and identified a novel series of HBV capsid inhibitors that demonstrated promising cellular selectivity indexes, metabolic stabilities, and in vitro safety profiles. Herein we disclose the design, synthesis, structureactivity relationship (SAR), cocrystal structure in complex with HBV capsid proteins and in vivo pharmacological study of the 4-methyl HAP analogues. In particular, the (2S,4S)-4,4-difluoroproline substituted analogue 34a demonstrated high oral bioavailability and liver exposure and achieved over 2 log viral load reduction in a hydrodynamic injected (HDI) HBV mouse model.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors

Eight series of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, MCF-7 and PC-3). Most of the forty nine target compounds showed excellent antiproliferative activity against one or several cancer cell lines. The compound 13a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with the IC50 values of 1.09 ¡À 0.04 muM, 1.34 ¡À 0.13 muM and 1.23 ¡À 0.09 muM, respectively. Eight selected compounds were further selected to evaluated for the inhibitory activity against EGFR kinase. Three of them showed equal activity against EGFR kinase to positive control afatinib. AnnexinV-FITC, propidium iodide (PI) double staining and acridine orange single staining results indicated that the compound 13a could induce apoptosis of human lung cancer A549 cells.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Aromatic polycyclic carboxylic acid derivatives (by machine translation)

The invention belongs to the field of medical technology, in particular to general formula (I) indicated by the aromatic ring carboxylic acid derivatives GPR40 receptor agonist, a pharmaceutically acceptable salt, an ester thereof or a stereoisomer thereof, wherein R1 , R2 , R3 , R4 , R5 , R6 And R7 Such as defined in the specification; the invention also relates to methods of preparing such compounds, pharmaceutical preparation and pharmaceutical composition, and the compounds and pharmaceutical compositions in the preparation as GPR40 receptor agonists for the prevention and/or for the treatment of diabetes in the application. . (by machine translation)

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Extended knowledge of 22929-52-8

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TDO2 INHIBITORS

Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators

A new series of potent fused thiazole mGlu5 receptor positive allosteric modulators (PAMs) (10, 11 and 27-31) are disclosed and details of the SAR and optimization are described. Optimization of alkynyl thiazole 9 (Lu AF11205) led to the identification of potent fused thiazole analogs 10b, 27a, 28j and 31d. In general, substituted cycloalkyl, aryl and heteroaryl carboxamides, and carbamate analogs are mGlu5 PAMs, whereas smaller alkyl carboxamide, sulfonamide and sulfamide analogs tend to be mGlu5 negative allosteric modulators (NAMs).

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS

Compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 are defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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A newly isolated strain capable of effectively degrading tetrahydrofuran and its performance in a continuous flow system

A Gram-negative strain DT4, capable of growing aerobically on tetrahydrofuran (THF) as the sole carbon and energy source was isolated from a pharmaceutical wastewater treatment plant. It was identified as Pseudomonas oleovorans by morphological and physiological characteristics as well as Biolog profiling and 16S rDNA sequence. Cells of P. oleovorans DT4 pre-cultured in THF could degrade 5 mM THF completely without lag phase. The generation time of 2.7 h and the maximum degradation rate of 203.9 mg THF/(h g dry weight) were observed, demonstrating that DT4 bears the highest THF-degrading activity in ever described strains. Furthermore, THF concentration as high as 100 mM was tolerated by the culture. Several important compounds including gamma-butyrrolactone and benzene could be directly metabolized, whereas other pollutants (e.g., tetrahydropyrane) could be cometabolized by DT4. THF removal was achieved in a continuous flow system with the maximum specific growth rate 0.113 h-1 and half-saturation constant 1.224 mg/L, indicating the great potential of THF bioremediation in future full-scale application.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem