57237-97-5Relevant academic research and scientific papers
Enhanced Antigiardial Effect of Omeprazole Analog Benzimidazole Compounds
Arreguin-Espinosa, Roberto,Calderón-Jaimes, Ernesto,Cuevas-Cruz, Miguel,Gómez-Manzo, Saúl,Hernández-Ochoa, Beatriz,Méndez-Tenorio, Alfonso,Marcial-Quino, Jaime,Ramírez-Nava, Edson Jiovany,Rocha-Ramírez, Luz María,Sánchez-Carrillo, Adrián,Santos-Segura, Araceli
, (2020/09/18)
Giardiasis is a diarrheal disease that is highly prevalent in developing countries. Several drugs are available for the treatment of this parasitosis; however, failures in drug therapy are common, and have adverse effects and increased resistance of the parasite to the drug, generating the need to find new alternative treatments. In this study, we synthesized a series of 2-mercaptobenzimidazoles that are derivatives of omeprazole, and the chemical structures were confirmed through mass, 1H NMR, and 13C NMR techniques. The in vitro efficacy compounds against Giardia, as well as its effect on the inhibition of triosephosphate isomerase (TPI) recombinant, were investigated, the inactivation assays were performed with 0.2 mg/mL of the enzyme incubating for 2 h at 37 ?C in TE buffer, pH 7.4 with increasing concentrations of the compounds. Among the target compounds, H-BZM2, O2N-BZM7, and O2N-BZM9 had greater antigiardial activity (IC50: 36, 14, and 17 μM on trophozoites), and inhibited the TPI enzyme (K2: 2.3, 3.2, and 2.8 M?1 s?1) respectively, loading alterations on the secondary structure, global stability, and tertiary structure of the TPI protein. Finally, we demonstrated that it had low toxicity on Caco-2 and HT29 cells. This finding makes it an attractive potential starting point for new antigiardial drugs.
Process for the preparation of organic compounds containing a sulfinyl or sulfonyl group in the presence of epsilon-phthalimidoperhexanoic acid
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Page 4, (2008/06/13)
A process for the oxidation of thioethers to sulfoxides or sulfones or for the oxidation of sulfoxides to sulfones by treatment of thioethers or sulfoxides with an oxidizing amount of ε-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.
Process for the preparation of organic compounds containing a sulfinyl or sulfonyl group
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Page 3, (2008/06/13)
A process for the oxidation of thioethers to sulfoxides or sulfones or for the oxidation of sulfoxides to sulfones by treatment of thioethers or sulfoxides with an oxidizing amount of ε-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.
Synthesis of New 1-Carbamoyl-5-fluorouracil Conjugates, Derived from Omeprazole and Cimetidine
Quelever, Gilles,Sturtz, Georges
, p. 817 - 822 (2007/10/03)
New 1-carbamoyl-5-fluorouracil conjugates which consist of a combination of 5-fluorouracil and anti-ulcer derivatives were designed in order to investigate their antitumor activity toward gastric carcinoma.The synthesis of these new analogs was achived using a coupling reaction between 1-chloroformyl-5-fluorouracil and 1-(ω-aminoalkyl) derivatives of well-known anti-ulcer compounds, ie, omeprazole and cimetidine. - Keywords: 5-fluorouracil; 1-carbamoyl-5-fluorouracil; omeprazole; cimetidine.
Studies on (H+-K+)-ATPase Inhibitors of Gastric Acid Secretion. Prodrugs of 2-benzimidazole Proton-Pump Inhibitors
Sih, John C.,Im, Wha Bin,Robert, Andre,Graber, David R.,Blakeman, David P.
, p. 1049 - 1062 (2007/10/02)
The synthesis of N-substituted benzimidazole (H+-K+)-ATPase or proton-pump inhibitors is described.These compounds were prepared to function as prodrugs of the parent N-H compound and evaluated for their ability to inhibit gastric (H
Anti-ulcer and gastric antisecretory activity of a series of thioethers and related sulphoxides
Beattie,Crossley,Dickinson,Dover
, p. 277 - 285 (2007/10/02)
A series of thioethers containing a pyridinium moiety were prepared and tested for gastric antisecretory and anti-ulcer activity. Following initial screening two compounds 2-(3-chlorobenzylthio)-1-methylpyridinium chloride and 2-(2-fluorobenzylthio)-1-methylpyridinium chloride were investigated further. By modification of substituent groups some separation of anti-ulcer and antisecretory activity was achieved. Subsequently it was found that the pyridinium moiety could be replaced and a number of related thioethers and sulphoxides were synthesised and were also found to be active. A wide range of structural variations were found to be possible with retention of activity.
Methods for treating gastrointestinal inflammation
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, (2008/06/13)
The present invention relates to the novel cytoprotective use for known heterocyclyalkylsulfinylbenzimidazoles, and novel, substantially non-antisecretory unit dose pharmaceutical compositions thereof.
Substituted 2-[pyridylalkylenesulfinyl]-benzimidazoles with gastric acid secretion inhibiting effects
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, (2008/06/13)
Compounds having the structural formula STR1 PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND THE USE THEREOF FOR AFFECTING GASTRIC ACID SECRETION; INTERMEDIATE PRODUCTS HAVING THE STRUCTURAL FORMULA STR2 AND METHODS FOR PREPARING THE SAME.
