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Isoxazoles bearing alkyl or carbamoyl groups were transformed into the corresponding pyrazoles in high yields by the treatment with hydrazine in methanol in the presence of a hydrogenation catalyst, e.g., Raney nickel, at ambient temperature. For the synthesis of N-substituted pyrazoles, hydrogenolysis of isoxazole followed by the treatment with substituted hydrazine was required. 3(5)-Aryl- or acylamido-substituted isoxazoles are less suitable for such transformations.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Chemoenzymatic syntheses of two key intermediates in the preparation of a potent beta-3 receptor agonist 1 are described. A lipase-catalysed hydrolytic desymmetrisation is employed in a new synthesis of intermediate 7, which avoids the use of alkyl-tin reagents. A second biotransformation delivers chiral chlorohydrin 5 from its parent ketone in greater enantiomeric excess than the previously-described Noyori-reduction process. A brief discussion of the enantioselectivity of a set of single-point mutants of Sporobolomyces salmonicolor aldehyde reductase in this bioreduction is also presented.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The photodegradation and phytotoxicity of the pharmaceutical antibiotic, sulphamethoxazole (SMX) and the azo-dye reactive-red-194 (RR194) under visible-light irradiation of TiO2 nanoparticles modified by silver and zirconium was investigated. The results indicated that sulphamethoxazole and its toxic degradation by product, 3-amino-5-methylisoxazole and RR-194 could be degraded efficiently by the co-doped Zr/Ag-TiO2 catalyst. PL studies and ROS generation results suggested that the effective charge separation was carried out while irradiation of the modified TiO2 nanoparticles. Phytotoxicity tests demonstrated lower percentage of germination in P. vulgaris (40%), V. radiata (30%) and P. lunatus (30%) of the seeds treated with 50 ppm of SMX, compared to the seeds treated with the degradation products (100%). The results with 50 ppm of RR-194 also showed lower percentage of germination in P. vulgaris (40%), V. radiata (50%) and P. lunatus (30%) compared to the degradation products (100%). Furthermore, significant increase in root and shoot development was observed in the seeds treated with the degraded products when compared with SMX and RR-194. Overall, this study contributes to further understanding the photodegradation mechanisms, degradation products and environmental fate of SMX and RR-194 in water which helps in the evaluation and mitigation of the environmental risk of SMX and RR-194 for water reuse and crop irrigation.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Treatment of glomerular diseases remains challenging. There are limited therapeutic options currently available for focal segmental glomerulosclerosis (FSGS) and immunoglobulin A nephropathy (IgAN) and they are generally ineffective in a substantial proportion of patients who progress to end-stage kidney disease during long-term followup. Standard management involving renin-angiotensin-aldosterone system (RAAS) inhibitors, corticosteroids and various immunosuppressive therapies does not always achieve.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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A series of new synthesized N-bis(trifluoromethyl)alkyl-N’-substituted ureas have been tested in the National Cancer Institute (NCI, Bethesda, USA) by Program NCI-60 DTP Human Tumor Cell Line Screen at a single high dose (10 -5 M). COMPARE analysis has been carried out for all tested compounds. The tested compounds showed antitumor activity against individual cell lines. The most sensitive cell lines relative to the tested compounds are: 5g Leukemia RPMI-8226 (GI% 52.7), Non-Small Cell Lung cancer HOP-92 (GI % 88.53), NCI-H522 (GI % 64.41), Melanoma UACC-62 (GI% 53.08), SK-MEL-5 (GI % 74.63), Breast cancer MDA-MB-468 (GI% 51.29), T-47D (GI % 65.1), 5b Leukemia K-562 (GI % 55.55), 7m Leukemia HL-60(TB) (GI % 51.76).

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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A compendium of phase change enthalpies published in 2010 is updated to include the period 1880-2015. Phase change enthalpies including fusion, vaporization, and sublimation enthalpies are included for organic, organometallic, and a few inorganic compounds. Part 1 of this compendium includes organic compounds from C1-C10. Part 2 of this compendium, to be published separately, will include organic and organometallic compounds from C11 to C192. Sufficient data are presently available to permit thermodynamic cycles to be constructed as an independent means of evaluating the reliability of the data. Temperature adjustments of phase change enthalpies from the temperature of measurement to the standard reference temperature, T = 298.15 K, and a protocol for doing so are briefly discussed.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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We report herein the SAR studies of a series of indole- and indolizine-glyoxylamides that demonstrate substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types of various origins (e.g., breast, colon, uterine).

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Cancer diseases are widely recognised as an important medical problem and killing millions of people in a year. Chemotherapeutic drugs are successful against cancer in many cases and different compounds, including the analogues of natural substances, may be used for anticancer agents. Nucleoside analogues also have become a necessity for the treatment of cancer diseases. Nucleoside, nucleotide and base analogues have been utilised for decades for the treatment of viral pathogens, neoplasms and in anticancer chemotherapy. This review focuses on the different types of nucleosides and their potential role as anticancer agents. It also discusses the nucleoside analogues approved by FDA and in process of approval. The effect of the substitution on the nucleoside analogues and their pharmacological role is also discussed in the review. Owing to the advances in computational chemistry, it concludes with the future advancement and possible outcome of the nucleoside analogues. Also, it depicts the development of heterocyclic nucleoside analogues, explores the QSAR of the synthesised compounds and discusses the 3 D QSAR pharmacophore modelling in order to examine their potential anti-cancer activities.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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In this work, the effect of supporting electrolytes on the simultaneous electrochemical oxidation of the pharmaceuticals sulfamethoxazole (SMX), propranolol (PRO), and carbamazepine (CBZ) in aqueous solutions has been studied. Based on the identified by-products, the degradation mechanisms were proposed and the acute toxicity was evaluated for each electrolyte. Assays were carried out in batch mode in a 2 L undivided reactor using a niobium coated with boron-doped diamond (Nb/BDD) mesh anode and Ti cathode at 2.5 A in presence of different supporting electrolytes (Na2SO4, NaCl, or NaBr) at the same concentration of 7 mM. The degradation rates were higher in the assays with NaCl and NaBr. Reaction by-products were identified by gas chromatography?mass spectrometry. Indirect oxidation by electrogenerated reactive halogen species (RHS) was the main mechanism when halide ions were used as electrolytes. Ten by-products were detected using Na2SO4 as electrolyte, while 19 (12 non-halogenated and 7 halogenated) and 20 (10 non-halogenated and 10 halogenated) using NaCl and NaBr respectively. The proposed degradation pathways involve transformation (hydroxylation, deamination, desulfonation, and halogenation) and bond rupture to produce less molecular weight compounds and their further transformation until total degradation. Chlorinated and brominated by-products confirm halogenation reactions. The electrogenerated RHS presented a significant inhibition effect on Vibrio fischeri; nevertheless, acute toxicity was not presented using Na2SO4 as electrolyte and a pharmaceutical concentration of 5 mug/L. In this view, the role of the supporting electrolyte in electrochemical oxidation process is crucial since it strongly influence degradation rate, by-products, and acute toxicity.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Pyridazin-3(2H)-one derivatives of formula (I) are found to inhibit PDE-4:, wherein R1, R2 and R4 are organic radicals, R3is a cyclic group, and R5 is an ester or an aryl or heteroaryl group.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem