3973-08-8Relevant articles and documents
Electrochemical oxidation of amoxicillin on carbon nanotubes and carbon nanotube supported metal modified electrodes
Ferreira, Marta,Kuzniarska-Biernacka, Iwona,Fonseca, António M.,Neves, Isabel C.,Soares, Olívia S.G.P.,Pereira, Manuel F.R.,Figueiredo, José L.,Parpot, Pier
, p. 322 - 331 (2019/07/10)
The electrolysis of amoxicillin (AMX) was carried out on CNT, Pt/CNT and Ru/CNT modified electrodes based on Carbon Toray in 0.1 M NaOH, 0.1 M NaCl and 0.1 M Na2CO3/NaHCO3 buffer (pH 10) media with the aim of studying the significance of two factors, electrode material and pH, on the oxidative degradation and mineralization of AMX. For this purpose, the electrolysis products were identified by HPLC-MS and GC–MS, and quantified by HPLC-UV-RID and IC. The highest carbon mineralization efficiency, corresponding to 30% of the oxidized AMX, was found for Pt/CNT modified electrode in carbonate buffer medium. Regarding to the AMX conversion, the results show that the effect of pH is higher than that of the electrode material. Principal component analysis allowed to determine the experimental parameters vs. product distribution relationship and to elucidate the oxidation pathways for the studied electrodes. The results show that the hydroxylation of the aromatic ring and the nitrogen atom play an important role on the efficient degradation of AMX.
Method for preparing thiazole-4-formic acid
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Paragraph 0021; 0028-0029; 0031; 0038-0039; 0041; 0048-0049, (2019/04/17)
The invention discloses a method for preparing thiazole-4-formic acid. By the aid of the method, the problems of relatively high prices of raw materials used in old processes for thiabendazole which is one of important traditional pesticide and bactericide varieties and low yield of the thiabendazole can be solved. The method includes steps of generating thiazolidine-4-formic acid from L-cysteinehydrochloride, formaldehyde and pyridine; carrying out reaction on the thiazolidine-4-formic acid, methyl alcohol and HCl gas to generate thiazolidine-4-methyl formate; carrying out reaction on the thiazolidine-4-methyl formate, acetonitrile and MnO2 to generate thiazole-4-methyl formate; hydrolyzing the thiazole-4-methyl formate under the effect of sodium hydroxide to obtain the thiazole-4-formicacid which is a product. The method has the advantages of simple process synthetic route, mild reaction condition, low cost, environmental protection, safety, excellent application prospect, good social benefit and high economic benefit.
A process for the preparation method of thiabendazole
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Paragraph 0063; 0076; 0081; 0088; 0089; 0102, (2018/04/01)
The invention relates to a new method for synthesizing thiabendazole. Acetone and chlorine are taken as starting materials to synthesize chloroacetone, chloroacetone not subjected to separation can directly react with thiocarbamide to obtain 2-Amino-4-methylthiazole which is subjected to diazotization to obtain 4-methylthiazole, and 4-methylthiazole is oxidized to produce 4-thiazolecarboxylic acid, and finally, 4-thiazolecarboxylic acid reacts with o-phenylenediamine to obtain the target object thiabendazole. The thiabendazole is a broad-spectrum anthelmintic, can repel roundworms, hookworms, whipworms, pinworms, strongyloises stercoralis and trichinization, is also a broad-spectrum efficient disinfectant and is widely used as a fruit fresh-keeping agent and a bactericidal mildew inhibitor in various fields over the past decade in China.
Preparation method for thiazol-4-formic acid
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Paragraph 0023; 0029; 0030; 0031; 0032; 0033; 0034-0041, (2018/03/24)
The invention discloses a preparation method for thiazol-4-formic acid. The method comprises the following steps: uniformly mixing ethyl bromopyruvate, thiourea and water, performing ring closure reaction, then adding concentrated hydrochloric acid for uniform mixing, adding dropwise an aqueous solution of sodium nitrite, performing stirring for 1.5 to 2.5h, performing filtering, and extracting a filter cake to obtain the thiazol-4-formic acid. The method is easy to operate, low in cost and suitable for industrial production, and the raw materials are cheap and are easily to obtain; water is used as a reaction solvent, and can be reutilized, so that the method is environment-friendly and pollution-free; the yield is high, and can reach 90 percent.
Metal-mediated inhibition of escherichia coli methionine aminopeptidase: Structure-activity relationships and development of a novel scoring function for metal-ligand interactions
Schiffmann, Rolf,Neugebauer, Alexander,Klein, Christian D.
, p. 511 - 522 (2007/10/03)
We report the discovery of thiabendazole as a potent inhibitor (K 1 = 0.4 μM) of Escherichia coli methionine aminopeptidase (ecMetAP) and the synthesis and pharmacological evaluation of thiabendazole congeners with activity in the upper nanomolar range, Elucidation of the X-ray structure of ecMetAP in complex with thiabendazole and an unrelated inhibitor that was independently described by another group showed that that both compounds bind to an additional CoII ion at the entrance of the active site. This unexpected finding explains the inactivity of the compounds under in vivo conditions. It also allows us to discuss the structure-activity relationships of this series of compounds in a meaningful way, based upon docking runs with an auxiliary metal ion, We describe a new scoring function for the evaluation of metal-mediated inhibitor binding that, unlike the previously used scoring function implemented in the docking program, allows us to distinguish between active and inactive compounds, Finally, conclusions for the structure-based design of in vivo-active inhibitors of ecMetAP are drawn.
Thiourea inhibitors of herpes viruses. Part 1: Bis-(aryl)thiourea inhibitors of CMV
Bloom, Jonathan D.,DiGrandi, Martin J.,Dushin, Russell G.,Curran, Kevin J.,Ross, Adma A.,Norton, Emily B.,Terefenko, Eugene,Jones, Thomas R.,Feld, Boris,Lang, Stanley A.
, p. 2929 - 2932 (2007/10/03)
Bis-(aryl)thioureas were found to be potent and selective inhibitors of cytomegalovirus (CMV) in cultured HFF cells. Of these, the thiazole analogue 38 was investigated as a potential development candidate.
Design, synthesis, and evaluation of α-ketoheterocycles as class C β-lactamase inhibitors
Kumar, Sanjai,Pearson, Andre L.,Pratt
, p. 2035 - 2044 (2007/10/03)
A series of specific α-ketoheterocycles (benzoxazole, thiazole, imidazole, tetrazole, and thiazole-4-carboxylate) has been synthesized in order to assess their potential as β-lactamase inhibitors. The syntheses were achieved either by construction of the heterocycle (benzoxazole) from an appropriate α-hydroxyimidate, followed by oxidation of the alcohol, or by direct reaction of methyl phenaceturate with a lithiated heterocycle. The properties of these compounds in aqueous solution are described and their inhibitory activity against β-lactamases assessed. They did inhibit the class C β-lactamase of Enterobacter cloacae P99 but not the TEM β-lactamase. The most effective inhibitor of the former enzyme (Ki = 0.11 mM) was 5-(phenylacetylglycyl) tetrazole, probably because it is an anion at neutral pH. Interpretation of the results was aided by computational models of the tetrahedral adducts. Most of the compounds also inhibited α-chymotrypsin but not porcine pancreatic elastase.
