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Aim: New triazolotetrahydrobenzothienopyrimidinone derivatives were synthesized. Experimental: Their structures were confirmed, and their anti-inflammatory, antimicrobial activities and ulcerogenic potentials were evaluated. Results: Compounds 7a, 10a and 11a showed minimal ulcerogenic effect and high selectivity toward human recombinant COX-2 over COX-1 enzyme with IC50 values of 1.39, 1.22 and 0.56 muM, respectively. Their docking outcome correlated with their biological activity and confirmed the high selectivity binding toward COX-2. Compound 12b displayed antimicrobial activity comparable to that of ampicillin against Escherichia coli while compounds 6 and 11c were similar to ampicillin against Staphylococcus aureus. In addition, compounds 7a, 9a, 10b and 11c showed dual anti-inflammatory/antimicrobial activities. Conclusion: This work represents a promising matrix for developing new potential anti-inflammatory, antimicrobial and dual antimicrobial/anti-inflammatory candidates. Quality Control of Isoxazole

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The purpose of this study was to investigate pesticide residues in fruits and vegetables from the Aegean region of Turkey. A total of 1423 samples of fresh fruit and vegetables were collected from 2010 to 2012. The samples were analysed to determine the concentrations of 186 pesticide residues. The analyses utilized ultrahigh performance liquid chromatography coupled with tandem mass spectrometry (UPLC/MS/MS) and gas chromatography with an electron capture detector (GC-ECD) confirmed by gas chromatography with mass spectrometry (GC-MS) after a multi-residue extraction procedure (the QuEChERS method). The results were evaluated according to maximum residue limits (MRLs) for each commodity and pesticide by Turkish Regulation. All pomegranate, cauliflower and cabbage samples were pesticides-free. A total of 754 samples contained detectable residues at or below MRLs, and 48 (8.4%) of the fruit samples and 83 (9.8%) of the vegetable samples contained pesticide residues above MRLs. MRL values were most often exceeded in arugula, cucumber, lemon, and grape commodities. All detected pesticides in apricot, carrot, kiwifruit and leek were below the MRLs. Acetamiprid, chlorpyriphos and carbendazim were the most detected pesticide residues.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 1072-67-9, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1072-67-9, name is 5-Methylisoxazol-3-amine. In an article,Which mentioned a new discovery about 1072-67-9

Isoxazolyl Schiff bases have been prepared from the corresponding amines by reaction with 2-nitrobenzaldehydes. These nitro compounds undergo de-oxygenative cyclization to give indazoles via nitrenes on heating with triethyl phosphite in acetonitrile. Isoxazolyl indazoles have also been synthesized in a one-pot reaction.

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In this study, a novel strain capable of degrading sulfamethoxazole (SMX) was isolated and identified as Acinetobacter sp. The effect of influencing factors, such as initial SMX concentration (5?240 mg/L), temperature (15?35 C), and pH (5?7), on SMX degradation was investigated. The results showed that when the initial SMX concentration was in the range of 5?240, the removal efficiency was 100%. The optimal condition for SMX biodegradation and microbial growth was determined to be 25 C and pH = 7.0 in terms of the removal efficiencies of SMX and total organic carbon (TOC). Four metabolite compounds were detected during the process of SMX biodegradation, and the degradation pathways were tentatively proposed. In summary, Acinetobacter sp. was highly efficient in mineralizing SMX, which has the potential to be used for degrading SMX in water and wastewater.

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A series of novel imidazo[1,2-b]isoxazoles 3 and their Mannich bases 4-6 were synthesized via convenient reactions. The reaction of 3-aminoisoxazole 1 with substituted phenacyl bromides 2 in dry ethanol afforded the corresponding 6-methyl-3-aryl imidazo[1,2-b]isoxazoles 3 in good yields. Compounds 3 on treatment with 37% formaline and secondary amines furnished the corresponding novel Mannich bases viz., 6-methyl-3-aryl-2-(morpholine/pyrrolidin-1-yl/piperidin-1-yl)-methyl-imidazo[1,2-b]isoxazoles 4-6.

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Co/Al2O3-EPM (i.e., prepared by electroless plating method) is a new potential catalyst with high catalytic capacity and stability, which has not been used for peroxymonosulfate (PMS) activation. In this study, the sulfamethoxazole (SMX) in aqueous solution was degraded by the Co/Al2O3-EPM/PMS system. First, characteristics of Co/Al2O3-EPM were analyzed by using X-ray powder diffraction (XRD), Fourier transform infrared (FTIR) and X-ray photoelectron spectroscopy (XPS). Then, the key parameters of Co/Al2O3-EPM dosage, PMS dosage and initial pH were optimized, respectively. The maximum SMX removal (98.5%) and total organic carbon (TOC) removal (25.6%) were obtained under the optimal conditions of Co/Al2O3-EPM = 0.8 g/L, PMS = 0.2 mM, initial pH = 6.3 and treatment time = 10 min. Also, the ions effects in Co/Al2O3-EPM/PMS system for SMX removal were investigated integrally. Besides, three control experiments (i.e., Co/Al2O3-EPM alone, PMS alone and homogeneous Co(II)/PMS systems) were conducted under the optimal conditions to verify the superiority of Co/Al2O3-EPM/PMS system. Furthermore, the degradation pathways of SMX were proposed according its intermediates detected by high performance liquid chromatography-mass spectrometry (HPLC-MS), and their biological toxicity were evaluated by activated sludge. In addition, the free radical identification experiment confirms that sulfate radical (SO4[rad]?) was the dominant active matter for SMX removal. The generation of SO4[rad]? during the reaction process in Co/Al2O3-EPM/PMS system was quantified indirectly via high performance liquid chromatography (HPLC). Finally, the possible reaction mechanism of Co/Al2O3-EPM/PMS system for SMX removal was proposed thoroughly. In brief, this study provided a new catalyst for PMS activation and all the results confirm that Co/Al2O3-EPM is a robust and high efficient catalyst for PMS activation.

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This paper describes the synthesis and the antileishmanial activity of new pyrazolyl benzenesulfonamide derivatives. These were elucidated by spectrometric methods. Some compounds showed a significant in vitro activity against Leishmania amazonensis, highlighting the derivative 1e. These pyrazolyl benzenesulfonamide derivatives did not show any toxicity in murine macrophage.

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A concise, regiocontrolled route to isoxazoles, based on the condensation of an ester with a metallated imine, has been developed. The intermediate vinylogous amides react smoothly with hydroxylamine to provide, after dehydration, substituted isoxazoles. The method has been used for the multi-kilo scale preparation of ABT-418, a novel cholinergic channel activator.

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The present disclosure provides substituted cyclohexylamine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, and R7 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

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Protoporphyrinogen oxidase (PPO) has been identified as one of the most promising targets for herbicide discovery. A series of novel phthalimide derivatives were designed by molecular docking studies targeting the crystal structure of mitochondrial PPO from tobacco (mtPPO, PDB: 1SEZ) by using Flumioxazin as a lead, after which the derivatives were synthesized and characterized, and their herbicidal activities were subsequently evaluated. The herbicidal bioassay results showed that compounds such as 3a (2-(4-bromo-2,6-difluorophenyl)isoindoline-1,3-dione), 3d (methyl 2-(4-chloro-1,3-dioxoisoindolin-2-yl)-5-fluorobenzoate), 3g (4-chloro-2-(5-methylisoxazol-3-yl) isoindoline-1,3-dione), 3j (4-chloro-2-(thiophen-2-ylmethyl)isoindoline-1,3-dione) and 3r (2-(4-bromo-2,6-difluorophenyl)-4-fluoroisoindoline-1,3-dione) had good herbicidal activities; among them, 3a showed excellent herbicidal efficacy against A. retroflexus and B. campestris via the small cup method and via pre-emergence and post-emergence spray treatments. The efficacy was comparable to that of the commercial herbicides Flumioxazin, Atrazine, and Chlortoluron. Further, the enzyme activity assay results suggest that the mode of action of compound 3a involves the inhibition of the PPO enzyme, and 3a showed better inhibitory activity against PPO than did Flumioxazin. These results indicate that our molecular design strategy contributes to the development of novel promising PPO inhibitors.

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