- Synthesis, characterization and antitumor activity of Cu(II), Co(II), Zn(II) and Mn(II) complex compounds with aminothiazole acetate derivative
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This paper presents the synthesis of complex compounds of type [M(L1)2], where M(II)= Cu (1), Co (2), Zn (3), L1=2-aminothiazole-4-acetate and [Mn(L1)2(H2O)] (4) using ethyl 2-(2-aminothiazole-4-yl) acetate (L), and characterization by elemental analysis, magnetic susceptibilities, IR, 1H-NMR, UV-Vis spectroscopy and for [Mn(L1)2(H2O)] also by X-ray diffraction. In vitro cytotoxicity studies were performed on human cervix adenocarcinoma, HeLa cells. The antitumor selectivity was assessed using normal human peripheral blood mononuclear cells, PBMC as control. Versita Sp. z o.o.
- Alexandru, Maria-Gabriela,Velickovic, Tanja Cirkovic,Jitaru, Ioana,Grguric-Sipka, Sanja,Draghici, Constantin
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- Synthesis, characterization and molecular docking studies of acetamide derivatives of 2-aminothiazole and 2-dihydropyridinone derivative of benzimidazole
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An efficient and easy synthesis of highly functionalized thiazole and pyridinone-substituted benzimidazole derivatives has been developed. The imino carbon of the benzimidazole derivative is coupled with the nitrogen atom of 1,4-dihydropyridinone and the aminothiazole-substituted acetic acid is condensed with two differently functionalized aniline, in two different reactions to form the amide linkages. These two amides and pyridinone-coupled benzimidazole are characterized by IR, 1H & 13C NMR and mass spectral studies. They are further evaluated for their antibacterial activity against the gram-positive bacterium Staphylococcus epidermidis and the fungus Saccharomyces cerevisiae by molecular docking method. All the three synthesized compounds had relatively lesser binding energy than what the standard drugs chloramphenicol and fluconazole have and may be considered as better inhibitors.
- Anbazhagan, V.,Britto, S.,Kanagasabapathy, G.
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- One-pot method for preparing cefotiam intermediate 2-aminothiazole-4-acetic acid
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The invention discloses a one-pot method for preparing a cefotiam intermediate that is 2-aminothiazole-4-acetic acid. The method is technically characterized by comprising the following steps: 1) by taking water as a solvent, carrying out ring closing by using thiourea and ethyl 4-chloroacetoacetate at a proper temperature and a proper molar ratio to generate ethyl 2-aminothiazole-4-acetate; afterthe reaction is finished, directly carrying out the next step of reaction on the reaction solution; 2) adding a certain amount of an alkali into the reaction solution for a hydrolysis reaction at a proper temperature, and 3) after the reaction is finished, adding a certain amount of an acid into the reaction solution at a proper temperature to adjust the pH value, and separating out the product.
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Paragraph 0041; 0043
(2020/08/25)
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- Study on a New Method for Synthesis of Mirabegron
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Mirabegron is a muscle relaxing drug for the treatment of overactive bladder. The existing synthetic methods for mirabegron produced intermediate product 4-(2-(phenethylamino)ethyl)aniline, which complicated the final product purification process. In this study, we designed a new synthetic route for mirabegron with low cost starting materials and a production of mirabegron at a 99.6% purity and a 61% overall yield. Particularly, this new synthetic route did not produce side product 4-(2-(phenethylamino)ethyl)aniline, which significantly simplified the product purification process.
- Xu, Guiqing,Mao, Shen,Mao, Longfei,Jiang, Yuqin,Zhou, Yong,Shen, Jiaxuan,Dong, Wenpei
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p. 2703 - 2707
(2017/09/26)
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- Thiazole, imidazole and oxazole compounds and treatments of disorders associated with protein aging
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Provided are, among other things, compounds of formula I or IA, . Also provided are methods of treatment with such compounds.
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- Method for treating glaucoma IIB
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Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, wherein J is oxygen, sulfur, or N—Rd.
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- Triazolo-pyrimidine intermediates
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There are disclosed a β-lactam compound represented by the formula (I): STR1 wherein R1 represents an acyl group; M represents a hydrogen atom, a protective group of an eliminatable group which is easily hydrolyzable in a human body; B represents a group represented by the formula (b): STR2 where at least one of R2, R3 and R9 represent a group represented by the formula: -A-OR4 where R4 represents a hydrogen or a lower alkyl group; and A represents a straight or branched alkylene group having 1 to 6 carbon atoms; and a remaining group or groups are each independently a hydrogen atom; a cyano group; a lower alkyl group which may be substituted by a halogen atom; a carbamoyl group which may be substituted by a lower alkyl group; a cycloalkyl group; or a carboxyl group which may be substituted by a protective group of an eliminatable group which is easily hydrolyzable in a human body, and also when R9 is -A-OR4, R2 and R3 may be combined with each other to form an alkylene group having 3 to 4 carbon atoms; and Z represents a nitrogen atom or a group represented by the formula: C-R10 where R10 represents a hydrogen atom, a carboxyl group or a lower alkyl group which may be substituted by a hydroxy group or a lower alkoxy group, or its pharmaceutically acceptable salt, and a process for preparing the same, an intermediate for synthesis of the same and a medicinal composition for bacterially infectious disease therapy containing the same.
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