- Fluorine-containing benzothiazole as a novel trypanocidal agent: Design, in silico study, synthesis and activity evaluation
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Trypanosoma cruzi (T. cruzi) is the etiologic agent of Chagas disease. In the bloodstream of humans, this parasite is in the trypomastigote stage and can infect host cells. Its metabolism is dependent on the glycolysis pathway, and one enzyme important fo
- Cuevas-Hernández, Roberto I.,Correa-Basurto, José,Flores-Sandoval, César A.,Padilla-Martínez, Itzia I.,Nogueda-Torres, Benjamín,Villa-Tanaca, María De Lourdes,Tamay-Cach, Feliciano,Nolasco-Fidencio, Juan J.,Trujillo-Ferrara, José G.
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- A fluorinated phenylbenzothiazole arrests the trypanosoma cruzi cell cycle and diminishes the infection of mammalian host cells
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Chagas disease (CD) is a human infection caused by Trypanosoma cruzi. CD was traditionally endemic to the Americas; however, due to migration it has spread to countries where it is not endemic. The current chemotherapy to treat CD induces several side eff
- Crispim, Marcell,Da Silva, Marcelo Santos,Elias, Maria Carolina,Girard, RichardM. B. M.,Silber, Ariel Mariano,Cuevas-Hernández, Roberto I.,Martínez-Cerón, Sarai,Trujillo-Ferrara, José G.
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- Method for preparing benzothiazole compound through microwave catalysis in water phase
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The invention discloses a method for preparing a benzothiazole compound through/under microwave catalysis in a water phase. A water-soluble coordination compound is used as a catalyst, and a reactionof inorganic sulfide, 2-iodoaniline and aldehyde is efficiently catalyzed through microwaves in a pure water phase. The method for preparing the benzothiazole compound is environmentally friendly, convenient to operate, safe, cheap and efficient. Compared with the prior art, the method is applied to a large quantity of functional groups, high in yield, simple to operate, safe, low in cost and environmentally friendly and produces a few byproducts.
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Paragraph 0016; 0023
(2018/05/16)
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- Synthesis of some novel 4-benzothiazol-2-yl-benzoyl-1H-pyrazoles, and evaluation as antiangiogenic agents
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Some 4-(1,3-benzothiazol-2-yl)-benzoyl-1H-pyrazole derivatives have been synthesized by reaction of o-aminothiophenol (1) with different electrophilic and nucleophilic reagents. All of the newly synthesized compounds were evaluated for cytotoxicity against breast cancer cell line MCF-7. Two of the compounds were more potent than tamoxifen and three were as potent as tamoxifen. These results were consistent with percentage inhibition of human VEGF compared with control untreated cells.
- El-Meguid, Eman Ali Abd,Ali, Mamdouh Moawad
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p. 1521 - 1536
(2016/04/26)
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- Weinreb amide as an efficient reagent in the one pot synthesis of benzimidazoles and benzothiazoles
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One pot synthesis of 2-substituted benzimidazoles/benzothiazoles through condensation is followed by cyclization of Weinreb amide with o-diaminoarene or o-aminothiophenol is reported. In the presence of boron trifluoride etherate in 1,4-dioxane solvent, a high yield (75-94%) was achieved within 60 min. Weinreb amide shows high selectivity in the reaction, even in presence of other active functional groups such as carboxyl, halogen, cyano, and methoxy.
- Bommegowda, Yadaganahalli K.,Lingaraju, Gejjalagere S.,Thamas, Saji,Vinay Kumar, Koravangala S.,Pradeepa Kumara, Challanayakanahally S.,Rangappa, Kanchugarakoppal S.,Sadashiva, Marilinganadoddi P.
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supporting information
p. 2693 - 2695
(2013/06/05)
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- O-aminophenol-containing AB-monomer for heterocyclic rigid-rod polymers
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A novel o-aminophenol-carboxylic AB-monomer with the following chemical structure: for synthesizing new rigid-rod polybenzobisazoles was prepared from the corresponding nitrobenzothiazolecarboxylic acid via an enzymatic process.
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Page/Page column 4
(2009/03/07)
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- Conversion of 2-(4-carboxyphenyl)-6-nitrobenzothiazole to 4-(6-amino-5-hydroxybenzothiazol-2-yl)benzoic acid by a recombinant E. coli strain
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E. coli C43(DE3)pNbzAHabA, expressing nitroreductase and mutase enzymes, converts 2-(4-carboxyphenyl)-6-nitrobenzothiazole to 4-(6-amino-5- hydroxybenzothiazol-2-yl)benzoic acid. The Royal Society of Chemistry 2006.
- Nadeau, Lloyd J.,Spain, Jim C.,Kannan, Ramamurthi,Tan, Loon-Seng
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p. 564 - 565
(2008/02/08)
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- Methods for the solid phase synthesis of combinatorial libraries of benzimidazol, benzoxazoles, benzothiazoles, and derivatives thereof
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The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
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