- THIURAM MONOSULFIDES AS A NEUTRAL CARRIER FOR COPPER(II)-SELECTIVE MEMBRANE ELECTRODE
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Poly(vinyl chloride) membrane electrodes that are sensitive and selective to copper(II) ion were developed.The electrodes based on tetramethyl, tetraethyl and dipyrrolidine thiuram monosulfides as a neutral carrier, exhibit a Nernstian behavior to copper(II) ion in the activity range of 10-1 M to 10-6 M - 10-8 M.Properties of the electrodes are briefly discussed.
- Kamata, Satsuo,Bhale, Ajay,Uda, Takaharu
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- Development of disulfide-derived fructose-1,6-bisphosphatase (FBPase) covalent inhibitors for the treatment of type 2 diabetes
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Fructose-1,6-bisphosphatase (FBPase), as a key rate-limiting enzyme in the gluconeogenesis (GNG) pathway, represents a practical therapeutic strategy for type 2 diabetes (T2D). Our previous work first identified cysteine residue 128 (C128) was an important allosteric site in the structure of FBPase, while pharmacologically targeting C128 attenuated the catalytic ability of FBPase. Herein, ten approved cysteine covalent drugs were selected for exploring FBPase inhibitory activities, and the alcohol deterrent disulfiram displayed superior inhibitory efficacy among those drugs. Based on the structure of lead compound disulfiram, 58 disulfide-derived compounds were designed and synthesized for investigating FBPase inhibitory activities. Optimal compound 3a exhibited significant FBPase inhibition and glucose-lowering efficacy in vitro and in vivo. Furthermore, 3a covalently modified the C128 site, and then regulated the N125–S124–S123 allosteric pathway of FBPase in mechanism. In summary, 3a has the potential to be a novel FBPase inhibitor for T2D therapy.
- Xu, Yi-xiang,Huang, Yun-yuan,Song, Rong-rong,Ren, Yan-liang,Chen, Xin,Zhang, Chao,Mao, Fei,Li, Xiao-kang,Zhu, Jin,Ni, Shuai-shuai,Wan, Jian,Li, Jian
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- Syntheses, properties, crystal and molecular structure of a novel neutral pentanuclear copper(I) iodide species. Copper(I) complexes with tetraethylthiuram monosulfide
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The reaction of copper(I) iodide with tetraethylthiuram monosulfide LEt afforded the novel copper(I) pentanuclear neutral complex [CU5LEt2I5]·EtOH·MeCN 1. Its crystal structure may be described as a very distorted octahedral central Cu3I3 cage having two additional CuLEt(I) units fused to the central cage by means of two iodine and one sulfur bridging atom. All copper(I) atoms in 1 are tetrahedral and both sulfur ligands are bidentate. The solvent molecules occupy intermolecular vacancies generated by the manner in which 1 is packed in space. In contrast, other copper(I) halides CuX (X = Cl or Br) with tetraethylthiuram monosulfide afforded the copper(I) complexes [CuLEt(X)] (X = Cl 2 or Br 3) which exist in the solid state as monomeric units featuring three-co-ordinate copper(I). The ligands are bidentate and co-ordination is completed by the halogen atoms. The complexes were additionally characterized by IR and 1H NMR spectra as well as magnetic susceptibility measurements. Complexes 2 and 3 can be alternatively prepared by sulfur abstraction from the disulfides, using triphenylphosphine. Copper(I) iodide and tetraethylthiuram monosulfide failed to yield a mononuclear compound under a variety of experimental conditions.
- Victoriano, Luis I.,Garland, Maria Teresa,Vega, Andres,Lopez, Cesar
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p. 1127 - 1131
(2007/10/03)
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- Method for preparing stearically hindered aryl phosphites
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A new process is disclosed for the manufacture of hindered aryl phosphites using derivatives of mercaptothiazole or dithiocarbamic acid as catalysts. Ortho-tertiary alkyl aryl phosphites are produced by the reaction of a phosphorus trihalide with an ortho-tertiary alkyl phenolic compound in the presence of the aforementioned catalysts.
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- Pesticidal compositions containing phosphoric esters and divalent sulphur compounds
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Pesticidal composition comprising: a pesticidal, phosphoric ester the molecule of which has at least one alkyl group of 1 to 3 carbon atoms, 0.05 to 10% of an agent stabilizing the said ester against decomposition by protonisation, together with adjuvants characterized in that the stabilizing agent comprises at least one sulphur compound containing per molecule at least one divalent sulphur atom of which one valence is bonded to an atom chosen from sulphur, carbon, nitrogen, hydrogen, and metals capable of giving a salt, the other valence being bonded to an atom chosen from hydrogen, the carbon atom already noted, a second carbon atom, the nitrogen atom already noted, a second nitrogen atom, the metal atom already noted in the case of a metal of valence greater than one, a second atom of metal and oxygen when the first valence is not attached to an atom of hydrogen, the proportion of sulphur calculated with reference to the weight of the sulphur compound being between 5 and 99%. Process for stabilizing a phosphoric ester of which the molecule possesses at least one alkyl group containing 1 to 3 carbon atoms characterized in that there is added to the phosphoric ester or to a mixture which contains it, 0.05 to 10% calculated on the weight of the phosphoric acid ester of an agent capable of stabilizing the said phosphoric ester against protonisation and comprising at least one sulphur compound such as that defined thereupon.
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