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A series of new isothiocoumarin-3-carboxylic acids derivatives had been obtained based on the 5-arylidenerhodanines hydrolysis. Anticancer activity screening allowed identification of 7,8-dimethoxy-1-oxo-1H-isothiochromene-3- carboxylic acid (4-phenylthiazol-2-yl)-amide (30) with the highest level of antimitotic activity (GI50NCI-H322M/NSC Lung Cancer = 1.28 muM). Evaluation of the antitrypanosomal activity against Trypanosoma brucei brucei showed that investigated compounds did not exhibit significant antiparasitic effects. Additionally, the most pharmacologically attractive compounds were non-toxic and well tolerated by the experimental animals.

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Microbial fuel cells (MFCs) are known for their ability to enhance the removal rate of toxins while generating power. This research presents a performance assessment of MFCs for power generation and sulfamethoxazole (SMX) degradation using SMX acclimatized cultures. Experiments were performed in MFC batch mode using different SMX concentrations in synthetic wastewater. The experimental results showed that voltage generation was >400 mV up to the SMX concentration of 0.20 mM (at 400 Omega external resistance). Control experiments supported the inference that biodegradation was the main process for SMX removal compared to sorption by SMX acclimatized cultures and that the process results in efficient removal of SMX in MFC mode. The specific removal rates of SMX in MFC with SMX acclimatized sludge were 0.67, 1.37, 3.43, 7.32, and 13.36 mum/h at initial SMX concentrations of 0.04, 0.08, 0.20, 0.39, and 0.79 mM, respectively. Moreover, the MFC was able to remove >90% of the TOC from the wastewater up to SMX concentrations of 0.08 mM. However, this TOC removal produces negative effects at higher SMX concentrations due to toxic intermediates. Microbial community analysis revealed large changes in bacterial communities at the phylum, class, and genus levels after SMX acclimatization and MFC operation. Thauera, a well-known aromatic-degrading bacteria, was the most dominant genus present in post-acclimatized conditions. In summary, this study showed that acclimatized sludge can play an important role in the biodegradation of SMX in MFCs.

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By the action of 2-amino-5-ethylthio-1,3,4-thidiazole, 3-amino-5-methyl isoxazole and 2-amino benzimidazole on 4-hydroxy-2-oxo-2Hchromene-3-sulfonyl chloride, corresponding 4-hydroxy-2-oxo-2H-chromene-3-sulfonic acid (5-ethyl-[1,3,4]thiadiazol-2-yl)-amide, 4-hydroxy-2-oxo-2H-chromene-3-sulfonic acid (5-methyl-isoxazol-3-yl)-amide and 4-hydroxy-2-oxo-2H-chromene-3-sulfonic acid (1Hbenzimidazol-2-yl)-amide were formed and they have been isolated in satisfying yields. Based on the biological activity of chromene-2-ones and heterocyclic compounds condensed in position 3 and 4, we also studied microbiological activity of these new compounds (4-6), against Staphylococcus aureus ATCC 25923, Streptococcus pneumoniae, Aeromonas salmonicida, Bacillus spp and some of them exhibited significant activity.

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The aim of this work was to study sulfamethoxazole (SMX) removal efficiency and fate of corresponding sul genes in a stacked microbial fuel cell-constructed wetland coupled biofilm electrode reactor system (MFC-CW-BER). Findings showed that two stacked MFC-CWs could provide a relatively stable electricity supply to support the biofilm for SMX removal. Excellent SMX removal (>99.29%) was obtained in the BER-MFC-CW. Compared with the 2000 mug L?1 SMX influent, the relative abundance of the sul genes in biofilm media and effluent was enhanced with continuously high concentrations of SMX (4000 mug L?1). The relative abundances of sul genes in biofilm media and effluent increased as the hydraulic retention time decreased. However, there was no obvious variation in the relative abundance of sul genes in the effluent from MFC-CWs. No effect could be observe of the direct voltage and bioelectricity on the relative abundance of the sul genes in the BER.

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A novel strategy for the dehydrogenation of the NH?NH bond is disclosed using potassium tert-butoxide (tBuOK) in liquid ammonia (NH3) under air at room temperature. Its synthetic value is well demonstrated by the highly efficient synthesis of aromatic azo compounds (up to 100 % yield, 3 min), heterocyclic azo compounds, and dehydrazination of phenylhydrazine. The broad application of this strategy and its benefit to chemical biology is proved by a novel, convenient, one-pot synthesis of aliphatic diazirines, which are important photoreactive agents for photoaffinity labeling.

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The electrochemical abatement of the antibiotic sulfamethoxazole (SMX) from aqueous solutions at pH 3.0 has been carried out by anodic oxidation and electro-Fenton (EF) processes with H2O2 electrogeneration. The electrolyses have been performed using a small, undivided cell equipped with a Pt or thin film boron-doped diamond (BDD) anode and a carbon-felt cathode. The higher performance of the EF process with 0.2mM Fe2+ in a BDD/carbon felt cell is demonstrated. This is due to the higher production of OH radicals, as well as to the simultaneous degradation at the anode surface and in the bulk solution. At low current, the oxidation at the anode was predominant; at high current, SMX was pre-eminently degraded in the bulk. SMX was quickly destroyed under all the conditions tested, following pseudo first-order kinetics; however, the almost total removal of the total organic carbon was only achieved in the BDD/carbon felt cell. The reaction by-products were quantified by chromatographic techniques and thus, the reaction pathway for the mineralization of SMX by EF has been elucidated. Hydroxylation of SMX on the sulfanilic ring is suggested as the first step, followed by the formation of p-benzoquinone and 3-amino-5-methylisoxazole. Their oxidative cleavage led to the formation of five carboxylic acids that were finally mineralized to CO2; the release of NH4+, NO3-, and SO42- accounted for almost 100% of the initial nitrogen and sulfur content. The absolute rate constants for the oxidative degradation of SMX and the detected aromatic by-products have also been determined.

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Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.

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The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein: A is a moiety of formula (Il) and to pharmaceutically acceptable salts and solvates thereof, wherein X, Z, D, E, V, W, Y, R1, R2, R5, R6, L, and u are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula I to a patient in need thereof, and to compositions for treating such disorders which contain the compounds of formula (I). The invention also relates to methods of making the compounds of formula (I).

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Differences in the degradation and transformation of atrazine (ATZ), carbamazepine (CBZ), diclofenac (DCF), and sulfamethoxazole (SMX) in deionized water during UV and UV/H2O2 treatment using lowpressure (LP) and medium pressure (MP) UV lamps, were assessed using a collimated beam apparatus. UV doses ranged from 300700 mJ/cm2 and H2O2 doses ranged from 010 mg/L. Liquid chromatography with tandem mass spectrometry (LC-MS/MS) was used to measure concentrations of the parent compounds and quadrupole time-of-flight mass spectrometry (QToF-MS) was used to screen for transformation products following treatment. In general, there was little difference in compound degradation and transformation between LP and MP UV lamps in both UV and UV/H2O2 treatments. Removal of ATZ, SMX and DCF was largely attributed to direct photodegradation whereas CBZ was not appreciably removed by UV or UV/H2O2 treatment. All four compounds yielded transformation products following UV or UV/H2O2 treatment with LP and MP lamps. Transformation pathways were determined using accurate mass estimation to determine elemental composition, and relative abundance was determined using ion counts. For ATZ and CBZ, the transformation pathway was non-sequential, whereas for DCF and SMX, the transformation pathway was sequential. The approach outlined in this paper can be used to assess unknown transformation products formed during oxidation of organic micropollutants during water treatment.

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Sulfamethoxazole (SMX) is a widely prescribed pharmaceutical compound to treat bacterial infections in both human and animals. As an alternative treatment process for non-degradable pharmaceuticals by conventional water treatment processes, radiolysis using gamma radiation has been applied as one of the radical-based advanced oxidative processes. However, further information was limited with regard to the production mechanism and fate of radiolytic products after treatment. Therefore, the degradation characteristics of SMX using ionizing radiation were investigated in this study. In addition, some radiolytic products of SMX were identified, and a degradation pathway as a result of the radiolysis of SMX was proposed. The radiolytic products were analyzed using liquid chromatography quadrupole time-of-flight mass spectrometry, liquid chromatography tandem mass spectrometry, and ion chromatography. Molecular structures of the radiolytic products were elucidated by the interpretation of MS2fragmentation patterns of each product. In total, fifteen products were elucidated as a result of ionizing radiation treatment of aqueous SMX in the range 0.1?5.0 kGy. Hydroxylation, bond-cleavage, and the combined mechanism of cleavage and transformation were proposed as the predominant mechanisms, inducing the various radiolytic products. In particular, based on the comparison of the relative intensity and the quantified concentration using authentic standards, RP270-1 (hydroxylated SMX) and RP172 (sulfanilic acid), RP99 (3-amino-5-methylisoxazole), and RP96 (sulfate) were the most abundant products. Chromatographic profiles of radiolytic products also revealed the change of major products with increasing absorbed doses, from compounds that have high molecular weight (MW), to relatively lower MW. The results of this study lead to an understanding of the role of ionizing radiation on the fate of the parent compound and its degradation products when applied to pharmaceutical pollutants.

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