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SODIUM CHANNEL BLOCKER

The present invention relates to a compound represented by Chemical Formula, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of sodium channel blocker-related diseases.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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288-14-2, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 288-14-2, Name is Isoxazole, molecular formula is C3H3NO. In a Article, authors is Nakano, Ryuhta£¬once mentioned of 288-14-2

Efficient transformation of electron-rich arenes into diethyl 3-arylisoxazole-4,5-dicarboxylates

Treatment of electron-rich arenes with Tf2O and DMF, followed by the reaction with NH2OH¡¤HCl and then with Oxone in the presence of diethyl acetylenedicarboxylate generated diethyl 3-arylisoxazole-4,5-dicarboxylates in good to moderate yields. Other alkynes could be also used for the present one-pot transformation of arenes into 3-arylisoxazole derivatives. Click here and insert your abstract text.

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1072-67-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1072-67-9, Name is 5-Methylisoxazol-3-amine, molecular formula is C4H6N2O. In a Article, authors is Skrlep, Luka£¬once mentioned of 1072-67-9

A simple synthesis of 1-substituted diethyl pyrrole-3,4-dicarboxylates

A series of 1-substituted diethyl 1H-pyrrole-3,4-dicarboxylates 4a – o were prepared in 14-93% yield by acid-catalysed treatment of diethyl 2,3-bis[(E, E)-(dimethylamino)-methylidene]succinate (2) with various aliphatic and (hetero)aromatic primary amines 3a – o. The configuration of the C=C double bonds in the bis-enaminone 2 was determined by 1H NMR and HMBC spectroscopy.

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Isoxazole – Wikipedia,
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Effect of Building Block Transformation in Covalent Triazine-Based Frameworks for Enhanced CO2 Uptake and Metal-Free Heterogeneous Catalysis

Covalent triazine frameworks (CTFs) have provided a unique platform in functional material design for a wide range of applications. This work reports a series of new CTFs with two new heteroaromatic building blocks (pyrazole and isoxazole groups) through a building-block transformation approach aiming for carbon capture and storage (CCS) and metal-free catalysis. The CTFs were synthesized from their respective building blocks [(4,4?-(1H-pyrazole-3,5-diyl)dibenzonitrile (pyz) and 4,4?-(isoxazole-3,5-diyl)dibenzonitrile (isox))] under ionothermal conditions using ZnCl2. Both of the building blocks were designed by an organic transformation of an acetylacetone containing dinitrile linker to pyrazole and isoxazole groups, respectively. Due to this organic transformation, (i) linker aromatization, (ii) higher surface areas and nitrogen contents, (iii) higher aromaticity, and (iv) higher surface basicity was achieved. Due to these enhanced properties, CTFs were explored for CO2 uptake and metal-free heterogeneous catalysis. Among all, the isox-CTF, synthesized at 400 C, showed the highest CO2 uptake (4.92 mmol g?1 at 273 K and 2.98 mmol g?1 at 298 K at 1 bar). Remarkably, these CTFs showed excellent metal-free catalytic activity for the aerobic oxidation of benzylamine at mild reaction conditions. On studying the properties of the CTFs, it was observed that organic transformations and ligand aromatization of the materials are crucial factor to tune the important parameters that influence the CO2 uptake and the catalytic activity. Overall, this work highlights the substantial effect of designing new CTF materials by building-block organic transformations resulting in better properties for CCS applications and heterogeneous catalysis.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The literature of heterocyclic chemistry, part VII: 1997-1999

This chapter discusses the literature of heterocyclic chemistry and surveys monographs and reviews published during the period 1997-1999, as well as some work published earlier related to heterocyclic chemistry. The chapter is based mainly on short bibliographic papers published by the authors in Khimiya Geterotsiklicheskikh Soedinenii.

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The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4- oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38alpha MAP kinase inhibitor for the treatment of inflammatory diseases

A novel, potent and selective quinazolinone series of inhibitors of p38alpha MAP kinase has been identified. Modifications designed to address the issues of poor aqueous solubility and high plasma protein binding as well as embedded aniline functionalities resulted in the identification of a clinical candidate N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin- 3(4H)-yl]benzamide (AZD6703). Optimisation was guided by understanding of the binding modes from X-ray crystallographic studies which showed a switch from DFG ‘out’ to DFG ‘in’ as the inhibitor size was reduced to improve overall properties.

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Catalytic efficiency of designed catalytic proteins

The de novo design of catalysts that mimic the affinity and specificity of natural enzymes remains one of the Holy Grails of chemistry. Despite decades of concerted effort we are still unable to design catalysts as efficient as enzymes. Here we critically evaluate approaches to (re)design of novel catalytic function in proteins using two test cases: Kemp elimination and ester hydrolysis. We show that the degree of success thus far has been modest when the rate enhancements seen for the designed proteins are compared with the rate enhancements by small molecule catalysts in solvents with properties similar to the active site. Nevertheless, there are reasons for optimism: the design methods are ever improving and the resulting catalyst can be efficiently improved using directed evolution.

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New 1,2-diaryl-4-substituted-benzylidene-5-4H-imidazolone derivatives: Design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents

A new series of 1,2-diaryl-4-substituted-benzylidene-5-4H-imidazolone derivatives 10a-h was designed and synthesized for evaluation as selective COX-2 inhibitors, anti-inflammatory agents and as analgesic agents. All compounds were more selective for COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compounds 10a, 10b, 10e and 10f were the most COX-2 selective compounds (S.I.?=?10.76, 10.87, 8.69 and 9.14 respectively), the most potent anti-inflammatory derivatives (ED50?=?65.7, 60.2, 76.3 and 107.4?mumol/kg respectively) in comparison with Celecoxib (COX-2 S.I.?=?8.61, ED50?=?82.2?mumol/kg) and were less ulcerogenic (ulcer indexes?=?1.22?3.02) than Ibuprofen (ulcer index?=?20.25) and comparable to Celecoxib (ulcer index?=?2.93). The four derivatives (10a, 10b, 10e and 10f) showed considerable analgesic activities which are clearly parallel to their anti-inflammatory activities.

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Coordination compounds of manganese(II) with isoxazole, 3,5-dimethylisoxazole and 3-methyl,5-phenylisoxazole

A series of compounds of general formula Mn(L)nX2 have been prepared where L = isoxazole (isox), 3,5-dimethylisoxazole (3,5-diMeisox), 3-methyl,5-phenylisoxazole (3-Me,5-Phisox); 1, 2, 4; X = Cl, Br, I, SCN.The i.r., E.S.R. and electronic spectra, the magnetic moments and the conductivities of the compounds have been used to elucidate their structure.The ligands are generally bridging N and O-bonded and the complexes are hexacoordinate.

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1,4-Dihydropyridine derivatives

Novel therapeutic 1,4-dihydropyridine derivatives of the formula in which:, A is an optionally substituted non-fused azole moiety;, R is a lower alkyl group;, X is -CH2- , -S- , -SO- or -SO2- ;, n is 5, 6, 7 or 8; and, Ar is a phenyl group substituted once or twice by NO2, CF3 or Cl groups.

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