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Fibroblast growth factor 2 (FGF2) signaling plays an important role in angiogenesis. Heparin/heparan sulfate (HS) is required for FGF2 signaling but heparin mimics either promotes or inhibits FGF2 signaling. To take advantage such properties of heparin mimics, a series of N-heteroaroyl aminosaccharide derivatives were designed and synthesized as FGF2 signaling modulators. The bioactivity was determined in a FGF2 and heparin-dependent cell proliferation assay using FGFR1c expressing BaF3 cells. We found that most of the compounds inhibited heparin- and FGF2-dependent BaF3 cell proliferation while three compounds promoted the cell proliferation. These results suggest that the small molecular heparin mimics approach might be useful in developing novel anti-angiogenic agents.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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(D)-Glucosamine and other nutritional supplements have emerged as safe alternative therapies for osteoarthritis, a chronic and degenerative articular joint disease. N-acetyl-(D)-glucosamine, a compound that can be modified at the N position, is considered to improve the oral bioavailability of (D)-glucosamine and has been proven to possess greater in vitro chondroprotective activity compared with the parent agent. In this study, to further utilize these properties, we focus on the modification of the N position with a benzenesulfonyl and different isoxazole formyl groups. Among these compounds, the 3-(2-chlorobenzene)-5-methyl-isoxazole formyl chloride and p-methoxybenzenesulfonyl chloride modifying structures proved to be the most active of the series and efficiently processed the chondrocytes in vitro. These novel N-position substitution compounds may represent promising leads for osteoarthritis drug development.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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This invention describes a process for the preparation of N-(4-trifluoromethyl)-5-methylisoxazole-4-carboxamide commonly known as leflunomide comprising : (a) reacting ethylaceto acetate, triethylorthoformate, and acetic anhydride with simultaneous distillation to form ethyl ethoxymethyleneacetoacetic ester; (b) reacting the ethyl ethoxymethyleneacetoacetic ester with aqueous hydroxylamine without using any external base and without any distillation to form ethyl-5-methylisoxazole-4-carboxylate; (c) reacting the ethyl-5-methylisoxazole-4-carboxylate with strong acid to form -5-methylisoxazole-4-carboxylic acid; (d) 5-methylisoxazole-4-carboxylic acid is reacted with thionyl chloride in presence of N, N-Dimethylformamide and equimolar of 4-trifluoromethylaniline without any external base to obtain highly pure Leflunomide.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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A compound of the formula STR1 where R1 is the radical of the formula II or III STR2 is suitable for the production of a pharmaceutical for the treatment of inflammations, carcinomatous diseases, or autoimmune diseases. A compound of the formula IV STR3 is suitable for the production of specific antibodies against a compound of the formula I for the discovery of specific-binding proteins from cell extracts, serum, blood, or synovial fluids, for the purification of proteins, for the modification of microtiter plates, or for the preparation of chromatography material, in particular of affinity chromatography material, and for use in diagnostics.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The present paper deals with the development of stability indicating a reversed phase high-performance liquid chromatographic (RP-HPLC) method for leflunomide, a disease-modifying antirheumatic drug in presence of its degradation products formed during forced decomposition studies. Forced degradation studies were performed on the bulk drug by using acid (0.1 N hydrochloric acid), base (0.1 N sodium hydroxide), water (neutral hydrolysis), 3% v/v hydrogen peroxide (oxidation), dry heat (60C) and UV light (254 nm). Degradation was observed for leflunomide in acidic and basic media only and the formed degradation products were found to be 5-methylisoxazole-4-carboxylic acid (degradation product-1) and 4-(trifluoromethyl)-aniline (degradation product-2). Successful separation of the drug from the degradation products formed under different stress conditions was achieved on a Novapak C18 column (150 mm × 3.9 mm, 4 mum particle size) using methanol- phosphate buffer (pH 5.3; 20 mM) (7:3, v/v) as the mobile phase at a flow rate of 1 mL/min. The detection wavelength was 260 nm. The developed method was completely validated and proved to be robust. As the method could effectively separate the drug from its degradation products, it can be employed for analysis of the samples of stability study.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Chemistry is traditionally divided into organic and inorganic chemistry. COA of Formula: C5H5NO3, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 42831-50-5

Positron emission tomography has emerged as the leading method for medical imaging with fluorine-18 as the most widely used radioactive isotope. Here we report a semi-automated method for the preparation of valuable [ 18F]trifluoromethylcopper, as well as its use for the radiosynthesis of [18F]trifluoromethylarenes and heteroarenes. Mild conditions of [18F]trifluoromethylation make this method particularly useful for the radiosynthesis of pharmacologically relevant [18F] trifluoromethylarenes and heteroarenes. 18F Radiochemistry: A semi-automated method for the fast preparation of radiolabelled (trifluoromethyl)copper is reported (see scheme), thus making [ 18F]CuCF3 almost as accessible as [18F]fluoride itself for the preparation of radiolabelled trifluoromethylated probes. It can be used for the preparation of radiolabelled trifluoromethylarenes from arylboronic acids and aryliodides. This methodology is clean, efficient and consistent with the specific requirements of radiochemistry.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The present invention relates to compounds of the formula [image] and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Compounds of the following formula have pharmaceutical properties: STR1 in which X is R1 (HO)C=C(CN)–, R1 (CO)–CH(CN)– or STR2 R1 and R2 are each hydrogen or C1-6 alkyl, R3, R4 and R5 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halo-substituted C1-4 alkyl, halo-substituted C1-4 alkoxy, halo-substituted C1-4 alkylthio, C2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R’R”N- where R’ and R” are each hydrogen or C1-4 alkyl R'”CONH– where R'” is C1-4 alkyl, R6, R7 and R8 are each C1-6 alkyl, halo-substituted C1-6 alkyl or optionally substituted phenyl, or R6 and R7, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R6, R7 and R8 together with the carbon atom to which they are attached, form a bicycloalkyl group containing 4 to 9 carbon atoms; and salts thereof.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Novel Leflunomide analogues were synthesized and evaluated in vivo against thioacetamide (TAA) induced liver fibrosis in rats. All the animals which were treated with the new analogues showed improved or comparable survival rates to those treated with Leflunomide. Animals which were treated with compounds 8d, 8e, 9 and 11 have shown improved liver parameters than Leflunomide treated animals. Histopathology of the liver has shown that compound 8a is the most active compound, which decreases fibrosis to a minimal level and compounds 8c, 8e and 11 are active compounds with fibrosis score 2-3 which is better than that of Leflunomide.

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Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The aim of the present study is to design and synthesize a series of novel 4(3H)-quinazolinone derivatives containing an isoxazole moiety and evaluate their antifungal activity against Gibberella zeae (G. zeae), Fusarium oxysporum (F. oxysporum), Cytospora mandshurica (C. mandshurica), Phytophthora infestans (P. infestans), and Pellicularia sasakii (P. sasakii), and their antibacterial activity against Ralstonia solanacearum (R. solanacearum) and Xanthomomu oryzae pv. oryzae (Xoo). Bioassay results showed that the target compounds 8a?8o had certain antifungal activities against the test fungus at the concentration of 50?mug/mL, which were lower than those of Hymexazol and Epoxiconazole. Meanwhile, preliminary bioassay results showed that compounds 8a?8o had better antibacterial activity against R. solanacearum and Xoo at 200 and 100?mug/mL. In particular, compound 8i exhibited significant antibacterial activity against Xoo in vitro, with an inhibition rate of 100% at 200?mug/mL, which was superior to those of Bismerthiazol (72%) and Thiodiazole copper (35%).

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Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem