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Compounds having the general structure formula (I) and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Electric Literature of 10288-72-9, Chemical engineers ensure the efficiency and safety of chemical processes, adapt the chemical make-up of products to meet environmental or economic needs, and apply new technologies to improve existing processes. 10288-72-9, Name is 6-Hydroxy-1,4-benzodioxane,introducing its new discovery.

The O-heterocycles, benzo-1,4-dioxane, phthalan, isochroman, 2,3-dihydrobenzofuran, benzofuran, and dibenzofuran are important building blocks with considerable medical application for the production of pharmaceuticals. Cytochrome P450 monooxygenase (P450) Bacillus megaterium 3 (BM3) wild type (WT) from Bacillus megaterium has low to no conversion of the six O-heterocycles. Screening of in-house libraries for active variants yielded P450 BM3 CM1 (R255P/P329H), which was subjected to directed evolution and site saturation mutagenesis of four positions. The latter led to the identification of position R255, which when introduced in the P450 BM3 WT, outperformed all other variants. The initial oxidation rate of nicotinamide adenine dinucleotide phosphate (NADPH) consumption increased ?140-fold (WT: 8.3 ± 1.3 min-1; R255L: 1168 ± 163 min-1), total turnover number (TTN) increased ?21-fold (WT: 40 ± 3; R255L: 860 ± 15), and coupling efficiency, ?2.9-fold (WT: 8.8 ± 0.1%; R255L: 25.7 ± 1.0%). Computational analysis showed that substitution R255L (distant from the heme-cofactor) does not have the salt bridge formed with D217 in WT, which introduces flexibility into the I-helix and leads to a heme rearrangement allowing for efficient hydroxylation.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

9/23/2021 News Awesome and Easy Science Experiments about 70918-54-6

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Antagonists of peripheral type 1 cannabinoid receptors (CB1) may have utility in the treatment of obesity, liver disease, metabolic syndrome and dyslipidemias. We have targeted analogues of the purine inverse agonist otenabant (1) for this purpose. The non-tissue selective CB1 antagonist rimonabant (2) was approved as a weight-loss agent in Europe but produced centrally mediated adverse effects in some patients including dysphoria and suicidal ideation leading to its withdrawal. Efforts are now underway to produce compounds with limited brain exposure. While many structure-activity relationship (SAR) studies of 2 have been reported, along with peripheralized compounds, 1 remains relatively less studied. In this report, we pursued analogues of 1 in which the 4-aminopiperidine group was switched to piperazine group to enable a better understanding of SAR to eventually produce compounds with limited brain penetration. To access a binding pocket and modulate physical properties, the piperazine was functionalized with alkyl, heteroalkyl, aryl and heteroaryl groups using a variety of connectors, including amides, sulfonamides, carbamates and ureas. These studies resulted in compounds that are potent antagonists of hCB1 with high selectivity for hCB1 over hCB2. The SAR obtained led to the discovery of 65 (Ki = 4 nM, >1,000-fold selective for hCB1 over hCB2), an orally bioavailable aryl urea with reduced brain penetration, and provides direction for discovering peripherally restricted compounds with good in vitro and in vivo properties.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

23-Sep-2021 News More research is needed about 70918-54-6

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1,4-Benzodioxane-2-carboxylic acid and isochroman-1-carboxylic acid were treated with thionyl chloride, and the resulting acid chlorides reacted with p-aminobenzoic acid in dioxane in the presence of pyridine to produce the corresponding amido acids. The latter were converted into acid chlorides which were brought into reaction with various amines to obtain a number of new diamides.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Herein is described the synthesis and structure-activity relationship of a novel series of aromatic and heteroaromatic 3-(1-benzyl-4-piperidinyl)propan-1-one derivatives that display potent and selective inhibition of the enzyme acetylcholinesterase (AChE). 1-(2-Methyl-6-benzothiazolyl)-3-(N-benzyl-4-piperidinyl)propan-1-one hydrochloride, 6d, is one of the most active compounds within this series exhibiting an IC50 for the inhibition of the AChE enzyme equal to 6.8 nM.Compound 6d has shown a dose-dependent elevation of total acetylcholine (ACh) levels in the mouse forebrain with an oral ED50 = 9.8 mg/kg.In addition, in vivo microdialysis experiments in the rat demonstrate that 6d increases extracellular ACh (100percent over basal) 1-3 h postdose with an oral ED50 = 4.8 mg/kg.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

9/23/2021 News Final Thoughts on Chemistry for 70918-54-6

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Application of 70918-54-6, You could be based in a university, combining chemical research with teaching; or in a public-sector research center, helping to ensure national healthcare provision keeps pace with new discoveries. In a document type is Article, and a compound is mentioned, 70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid, introducing its new discovery.

It had been reported that some dioxygenated rings fusing with the quinazoline scaffold could lead to new EGFR inhibitors. Based on this, several kinds of oxygenated alkane quinazoline derivatives were synthetized and evaluated as EGFR inhibitors. Their antiproliferative activities were tested against four cancer cell lines: A431, MCF-7, A549, and B16-F10. Most derivatives could counteract EGF-induced EGFR phosphorylation, and their potency was comparable to the reference compound Erlotinib. The size of the fused dioxygenated ring was crucial for the biological activity and the heptatomic ring derivative 19 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the cellular assay.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

09/23/21 News Extracurricular laboratory:new discovery of 70918-54-6

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The invention discloses a method for amide derivatives, its general structure shown in formula (I): Wherein R1 Is selected from H, OH or CH3 , R2 Is selected from H, OH or CH3 , R3 Is selected from H, OH or CH3 . The amide derivatives of the invention to angiotensin II-mediated ApoE- / – Mouse model has demonstrated good biological activity, of the present invention the amide derivatives in the prevention and/or for treating cardiovascular diseases with positive in, can be hypertension, hyperlipidemia and/or atherosclerosis in more in-depth research. (by machine translation)

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.Read on for other articles about Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine!

Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, With the volume and accessibility of scientific research increasing across the world, it has never been more important to continue building the reputation for quality and ethical publishing we’ve spent the past two centuries establishing. Type is Article, and a compound is mentioned, 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, introducing its new discovery.

In a search for therapeutic agents for the treatment of osteoporosis and bone fracture, we found that 2-benzothiopyran-1-carboxamide derivatives 1, derived from ipriflavone as a lead compound, increase cellular alkaline phosphatase activity in cultures of rat bone marrow stromal cells. Further modification of 1 has led to the discovery of more potent 3-benzothiepin-2- carboxamide derivatives 2. Of these, 3-benzothiepin derivatives bearing a 4- (dialkoxyphosphorylmethyl)phenyl group on the 2-carboxamide moiety such as 2h and 2q exhibited significant improvement of activity compared to ipriflavone. Asymmetric synthesis of 2h and 2q revealed that the (-)-isomers possessed activities superior to those of the (+)-isomers. Further evaluation of these compounds using the mouse osteoblastic cell line MC3T3-E1 revealed that (-)- 2q enhanced the effect of bone morphogenetic protein. In addition, application of a sustained-release agent containing 2q increased the area of newly formed bone in a rat skull defect model. Based on these findings, (-)- 2q was selected for further investigation as a new drug stimulating bone formation. Synthesis and structure-activity relationships for this novel series of 2-benzothiopyran and 3-benzothiepin derivatives are detailed.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Sep-21 News Archives for Chemistry Experiments of 22013-33-8

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Electric Literature of 22013-33-8,The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine,introducing its new discovery.

Small molecules based upon natural product dimers that exhibit cytotoxic activity were synthesized and evaluated for their anti-proliferative activity in human breast cancer cell lines. A central isophthalic core structure linking aromatic amines containing 3,5-disubstitutions produced the most active compounds. This series of compounds was found to be more active against the estrogen receptor positive cell line MCF-7 than the estrogen receptor negative cell line, SKBr3.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

23-Sep-2021 News Our Top Choice Compound: 10288-72-9

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The present invention relates to pyrimidine derivatives of formula (I) wherein (R1)n, R3, R4a, R4b, R5a, R5b and Ar1 are as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem