- The synthesis and evaluation of phenoxyacylhydroxamic acids as potential agents for Helicobacter pylori infections
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Two series of ω-phenoxy contained acylhydroxamic acids as novel urease inhibitors were designed and synthesized. Biological activity evaluations revealed that ω-phenoxypropinoylhydroxamic acids were more active than phenoxyacetohydroxamic acids. Out of these compounds, 3-(3,4-dichlorophenoxy)propionylhydroxamic acid c24 showed significant potency against urease in both cell free extract (IC50 = 0.061 ± 0.003 μM) and intact cell (IC50 = 0.89 ± 0.05 μM), being over 450- and 120-fold more potent than the clinically prescribed urease inhibitor AHA, repectively. Non-linear fitting of experimental data (V-[S]) suggested a mixed-type inhibition mechanism and a dual site binding mode of these compounds.
- Ni, Wei-Wei,Liu, Qi,Ren, Shen-Zhen,Li, Wei-Yi,Yi, Li-Li,Jing, Heng,Sheng, Li-Xin,Wan, Qin,Zhong, Ping-Fu,Fang, Hai-Lian,Ouyang, Hui,Xiao, Zhu-Ping,Zhu, Hai-Liang
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supporting information
p. 4145 - 4152
(2018/07/13)
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- Catalytic Olefin hydroalkoxylation by nano particles of pollucite
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The catalytic hydroalkoxylation of α,β-unsaturated esters, nitriles, and ethers with aliphatic and aromatic alcohols over pollucite using thermal and microwave-assisted methods was investigated. To study the effect of the alcohol structures on the mechanism of the hydroalkoxylation reaction, different alcohols, such as methanol to butanol, cyclohexanol, phenol, and 2-ethylhexanol were used. The activities of pollucite, in contrast to other basic solids, were scarcely affected by the presence of air and moisture. The correlation between alcohol acidity and reaction activity is discussed. The prepared pollucite was characterized by X-ray diffraction, volumetric nitrogen adsorption surface area analysis, and CO2 temperature-programmed desorption. Scanning electron microscopy analysis revealed that the size of the modified nano catalyst particles was under 40nm.
- Zamanian, Sara,Kharat, Ali Nemati
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p. 981 - 986
(2015/06/25)
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- Kinetics and mechanism of thermal gas-phase elimination of β-substituted carboxylic acids
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3-Phenoxypropanoic acid (1), 3-(phenylthio)propanoic acid (2), and 4-phenylbutanoic acid (3) were pyrolysed between 520 and 682 K. Analysis of the pyrolysates showed the elimination products to be acrylic acid and the corresponding arene. Pyrolysis of ethyl 3-phenoxypropanoate (4) and its methyl analogue (5), ethyl 3-(phenylthio)propanoate (6) and its methyl counterpart (7), and 3-phenoxypropane nitrile (8) were also investigated between 617 and 737 K. The thermal gas-phase elimination kinetics and product analysis are compatible with a thermal retro-Michael reaction pathway involving a four-membered cyclic transition state.
- Al-Awadi,Abdallah,Dib,Ibrahim,Al-Awadi,El-Dusouqui
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p. 5769 - 5777
(2007/10/03)
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