- Modification of existing antibiotics in the form of precursor prodrugs that can be subsequently activated by nitroreductases of the target pathogen
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The use of existing antibiotics in the form of prodrug followed by activation using enzymes of pathogenic origin could be a useful approach for antimicrobial therapy. To investigate this idea, a common antibiotic, sulfamethoxazole has been redesigned in t
- ?elik, Ayhan,Yeti?, Gülden,Ay, Mehmet,Güng?r, Tu?ba
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- 0D/1D AgI/MoO3 Z-scheme heterojunction photocatalyst: Highly efficient visible-light-driven photocatalyst for sulfamethoxazole degradation
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Low dimension nano photocatalysts show great potential in the field of treating contaminated water for their large surface area and size effect. In this study, a 0D/1D AgI/MoO3 Z-scheme photocatalyst with striking photocatalytic performance was constructed successfully. The one-dimensional MoO3 nanobelts were prepared by a simple hydrothermal method, and then it was modified by AgI nanoparticles in a handy deposition approach. When choosing sulfamethoxazole (SMZ) as the target contaminant, the rate constant value of the optimal 0D/1D AgI/MoO3 composite could hit up to 0.13 min?1, which is nearly 22.4 times and 32.5 times as that of pure MoO3 (0.0058 min?1) and AgI (0.0040 min?1), respectively. A series of detailed characterizations give evidences that the charge transfer in the composite followed Z scheme mechanism. Therefore, efficient separation/transfer and the remained high redox activity of photogenerated carriers played a vital role in the sharply enhanced photocatalytic properties. The possible degradation pathways of SMZ were proposed based on the intermediates detected by high-performance liquid chromatography-mass spectrometry (HPLC-MS). Meanwhile, the magnificent cyclic stability makes the material a promising material in the practical application.
- Xu, Jing,Chen, Juan,Ao, Yanhui,Wang, Peifang
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supporting information
p. 3226 - 3230
(2021/05/29)
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- Insights into the electrochemical degradation of sulfamethoxazole and its metabolite by Ti/SnO2-Sb/Er-PbO2 anode
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Electrochemical degradation of sulfamethoxazole (SMX) and its metabolite acetyl-sulfamethoxazole (Ac-SMX) by Ti/SnO2-Sb/Er-PbO2 were investigated. Results indicated that the electrochemical degradation of SMX and Ac-SMX followed pseu
- Wang, Yanping,Zhou, Chengzhi,Wu, Jinhua,Niu, Junfeng
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supporting information
p. 2673 - 2677
(2020/06/01)
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- Insight into sulfamethoxazole degradation, mechanism, and pathways by AgBr-BaMoO4 composite photocatalyst
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A composite photocatalyst, AgBr-BaMoO4 was fabricated by two step method; microwave hydrothermal and precipitation-deposition. The as prepared photocatalyst samples were characterized by various techniques. The facet coupling was seen between the (204) plane of BaMoO4 and (200)/(222) planes of AgBr on the basis of XRD/HRTEM analysis. The pharmaceutical pollutant, sulfamethoxazole was adopted to investigate the photocatalytic performances of samples under UV–vis irradiation. The AgBr-BaMoO4 composite degraded the aqueous sulfamethoxazole drug in UV–vis light about 64% within 75 min, which was attributed to efficient separation of photogenerated electron–hole pairs across the interface between Ag/AgBr and BaMoO4. The multi-electron induced oxygen reduced reaction (ORR) was observed. The radical trapping experiment indicates that OH? has major role for sulfamethoxazole degradation. The four successive photodegradation of sulfamethoxazole in UV–vis light indicates the stability of composite photocatalyst. Furthermore, the three different degradation pathways were designed on the basis of retention time and molecular masses of 18 degraded organic fragments that was confirmed by high-performance liquid chromatography photodiode array (HPLC-PDA) and high resolution-quadruple time of flight electrospray ionization mass spectroscopy (HR-QTOF ESI/MS) techniques. The total organic carbon (TOC) analysis suggested the mineralization of SMZ by composite photocatalyst. This study not only demonstrates the enhancement of photocatalytic performance of wide band gap semiconductor by making composite with narrow band gap semiconductor but also detail degradation pathways and mechanisms of sulfamethoxazole.
- Ray, Schindra Kumar,Dhakal, Dipesh,Lee, Soo Wohn
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p. 686 - 695
(2018/07/14)
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- Effects of water environmental factors on the photocatalytic degradation of sulfamethoxazole by AgI/UiO-66 composite under visible light irradiation
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It is necessary to find visible light responsive photocatalysts for rapid and simple degradation of organic pollutants in water environment. In this work, a visible light responsive composite photocatalyst AgI/UiO-66 was prepared by an in situ growth method. Sulfamethoxazole (SMZ) antibiotic was selected as the target contaminant to probe the photocatalytic performance of the as-prepared AgI/UiO-66 composite under visible light irradiation. The results showed that the photocatalytic performance of the AgI/UiO-66 composite enhanced significantly compared to pure AgI. The effects of typical environment factors (i.e. pH, inorganic salt ions and common anions) on the degradation of SMZ were evaluated extensively. Results showed that the investigated pH (5.2, 7.0, 9.5) had no apparent effect on the photocatalytic degradation of SMZ except pH 2.5, at which the degradation rate of SMZ decreased significantly. In addition, inorganic salt ions and Cl?, HCO3? and SO42? anions in water exhibited no apparent effect on the degradation of SMZ. The effect of water matrix on the degradation of SMZ was also investigated. In the river water, the removal efficiency of SMZ was reduced compared with the cleaner water matrix. The capture experiments of radicals confirmed that superoxide radicals ([rad]O2?) and hydroxyl radicals ([rad]OH) were the main active species for the photocatalytic degradation of SMZ in the present work. Finally, the tentative degradation pathways of SMZ were proposed based on the intermediates analysis.
- Wang, Chao,Xue, Yao,Wang, Peifang,Ao, Yanhui
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p. 314 - 322
(2018/03/22)
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- NOVEL OLEFIN DERIVATIVE
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The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound. A compound of formula (I′): wherein R1 is substituted or unsubstituted aryl etc., R2 is each independently hydrogen, substituted or unsubstituted alkyl etc., R3 is each independently hydrogen, substituted or unsubstituted alkyl etc., n is an integer from 0 to 3, R12 is hydrogen, substituted or unsubstituted alkyl etc., Ring A is aromatic carbocycle or aromatic heterocycle, R9 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., m is an integer from 0 to 4, R4 and R5 is each independently hydrogen, substituted or unsubstituted alkyl etc., R6 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., R13 is hydrogen, substituted or unsubstituted alkyl etc., X5 is bond etc., R7 is hydrogen or substituted or unsubstituted alkyl, R8 is substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted alkenylcarbonyl etc.
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Paragraph 0519-0521
(2015/09/28)
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- Metabolic and chemical origins of cross-reactive immunological reactions to arylamine benzenesulfonamides: T-cell responses to hydroxylamine and nitroso derivatives
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Exposure to sulfamethoxazole (SMX) is associated with T-cell-mediated hypersensitivity reactions in human patients. T-cells can be stimulated by the putative metabolite nitroso SMX, which binds irreversibly to protein. The hydroxylamine and nitroso deriva
- Castrejon, J. Luis,Lavergne, Sidonie N.,El-Sheikh, Ayman,Farrell, John,Maggs, James L.,Sabbani, Sunil,O'Neill, Paul M.,Kevin Park,Naisbitt, Dean J.
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experimental part
p. 184 - 192
(2011/02/16)
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- In vivo and in vitro anti-leishmanial activities of 4-nitro-N-pyrimidinand N-pyrazin-2-ylbenzenesulfonamides, and N2-(4-nitrophenyl)-N 1propylglycinamide
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A series of compounds containing the nitrobenzene and sulfonamido moieties were synthesized and their leishmanicidal effect was assessed in vitro against Leishmania infantum promastigotes. Among the compounds evaluated, the p-nitrobenzenesulfonamides 4Aa
- Auxiliadora Dea-Ayuela,Castillo, Encarna,Gonzalez-Alvarez, Marta,Vega, Celeste,Rolón, Miriam,Bolas-Fernández, Francisco,Borras, Joaquín,Eugenia González-Rosende
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experimental part
p. 7449 - 7456
(2011/02/23)
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- The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: Polar region modifications
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The structure-activity relationship study focused on the polar region of the HTS hit A-80040 (1) producing several series of potent and selective ACC2 inhibitors. The SAR suggests a compact lipophilic pocket that does not tolerate polar and ionic groups.
- Xu, Xiangdong,Weitzberg, Moshe,Keyes, Robert F.,Li, Qun,Wang, Rongqi,Wang, Xiaojun,Zhang, Xiaolin,Frevert, Ernst U.,Camp, Heidi S.,Beutel, Bruce A.,Sham, Hing L.,Gu, Yu Gui
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p. 1803 - 1807
(2007/10/03)
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- Novel acetyl-CoA carboxylase (ACC) inhibitors and their use in diabetes, obesity and metabolic syndrome
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The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
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Page/Page column 46
(2008/06/13)
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- Reactive oxygen species generation and its role in the differential cytotoxicity of the arylhydroxylamine metabolites of sulfamethoxazole and dapsone in normal human epidermal keratinocytes
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Cutaneous drug reactions (CDR) are responsible for numerous minor to life-threatening complications. Though the exact mechanism for CDR is not completely understood, evidence suggests that bioactivation of drugs to reactive oxygen or nitrogen species is a
- Vyas, Piyush M.,Roychowdhury, Sanjoy,Woster, Patrick M.,Svensson, Craig K.
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p. 275 - 286
(2007/10/03)
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- Synthesis and reactions of nitroso sulphamethoxazole with biological nucleophiles: Implications for immune mediated toxicity
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Sulphamethoxazole hydroxylamine (SMX-NHOH) and nitroso sulphamethoxazole (SMX-NO) were prepared by a modified literature procedure. SMX-NO produced a complex set of unstable intermediates with sulphur nucleophiles, but did not react with amino containing compounds. No reactions were observed between sulphamethoxazole (SMX) / SMX-NHOH and the nucleophiles used in this study. Thus antigens formed from N-oxidation of SMX are likely to be unstable in vivo.
- Naisbitt, Dean J.,Neill, Paul M.,Pirmohamed, Munir,Park, B. Kevin
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p. 1511 - 1516
(2007/10/03)
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