- Synthesis, characterization and biological applications of bismuth(III) complexes with aroylthiourea ligands
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This work describes the synthesis, structural characterization and biological applications of three new bismuth(III) complexes with aroylthiourea-based ligands: [Bi(La)3(HLa)] (1), [Bi2(Lb)4(μ-Lb)2]?2(C3H6O) (2), and [Bi6(μ-Lc)6(μ3-NO3)2(μ6-NO3)](NO3)3?4H2O (3), where HLa = N-benzoyl(N′,N′-diethylthiourea), HLb = N-benzoyl(morpholinylthiourea), and H2Lc = N2,N6-bis(diethylcarbamothioyl)pyridine-2,6-dicarboxamide. The ligands HLa and HLb were considered as monopodal, while H2Lc as bipodal. All compounds were characterized by melting point determination, Fourier-transform infrared spectroscopy (FTIR), proton proton and carbon-13 nuclear magnetic resonance spectroscopy (NMR), mass spectrometry (MS), elemental analysis (EA) and single-crystal X-ray diffraction (SC-XRD). Structural analysis showed that compound 1 was a mononuclear heptacoordinate complex, while compound 2 presented a dinuclear structure and compound 3 was built up by a hexanuclear framework. The proligands, the new complexes, and Bi(NO3)3?5H2O had their antibacterial activities evaluated against E. coli (ATCC 25922), S. aureus (ATCC 25923), and P. aeruginosa (ATCC 27853). The in vitro disk-diffusion (DD) method showed the ability of compound 2 to inhibit two types of bacteria (P. aeruginosa and S. aureus). In the results of minimum inhibitory concentration (MIC), all complexes showed significant activity against the tested microorganisms except for compound 1. The inorganic salt used for comparison showed antibacterial activity only against P. aeruginosa and the ligands showed no apparent activity. Compound 2 presented the best antibacterial activity among the tested substances, and its performance was remarkable even when compared to other similar compounds found in the literature, attesting the importance of targeting bismuth(III) aroylthioureas for further research on new drugs development.
- Burrow, Robert Alan,Chuy, Gabriela Pereira,Lang, Ernesto Schulz,Vizzotto, Bruno Stefanello,de Oliveira, Marcielli Indiara,dos Santos, Sailer Santos
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- Compound and color filter
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PROBLEM TO BE SOLVED: To provide a color material which can realize excellent contrast even when subjected to a thermal history of 200°C or more required in a production process in manufacturing a color filter. SOLUTION: The invention provides compounds represented by the formula (I) in the figure. (In the general formula (I), B represents an optionally substituted aromatic group or an optionally substituted heterocyclic group; [A]n- represents any n-valent anion; and R1, R2, R3 and R4 each independently represent a hydrogen atom, C1-8 alkyl group or phenyl group.) SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0126; 0127
(2018/12/14)
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- Biochemical and pharmacological evaluation of 4-hydroxychromen-2-ones bearing polar C-3 substituents as anticoagulants
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The objective of this study was to investigate in vitro and in vivo anticoagulant activity of sixteen 4-hydroxycoumarin derivatives bearing polar C-3 scaffolds. The activity was evaluated by measuring prothrombin time. Enhanced anticoagulant activity in vitro was observed for all tested compounds. Upon successive administration of 0.5 mg/kg of body weight to adult Wistar rats, over a period of five days, four derivatives (2b, 4c, 5c and 9c) presented anticoagulant activity in vivo. The most active compound was 2b, with PT = 30.0 s. Low or non-toxic effects in vivo were determined based on the catalytic activity of liver enzymes and the concentration of bilirubin, iron and proteins. Metabolic pathways of the most active compounds in vivo were determined after GC/MS analysis of collected rat urine samples. The excretion occurs by glucuronidation of 7-hydroxy forms of tested derivatives. In vivo results were described using PLS-based CoMFA and CoMSIA 3D-QSAR studies, which showed CoMFA-SE (q2 = 0.738) and CoMSIA-SEA (q2 = 0.763) to be the statistically most relevant models. Furthermore, molecular docking and DFT mechanistic studies performed on the rat VKORC1 homology model revealed interactions between the 4-OH coumarin group in the form of phenolic anion and the Cys135 catalytic site in the transition state.
- Mladenovic, Milan,Mihailovic, Mirjana,Bogojevic, Desanka,Vukovic, Nenad,Sukdolak, Slobodan,Matic, Sanja,Niciforovic, Neda,Mihailovic, Vladimir,Maskovic, Pavle,Vrvic, Miroslav M.,Solujic, Slavica
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scheme or table
p. 144 - 158
(2012/09/21)
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- COLORED CURABLE COMPOSITION, COLOR RESIST, INK-JET INK, COLOR FILTER AND METHOD FOR PRODUCING THE SAME, SOLID-STATE IMAGE PICKUP DEVICE, IMAGE DISPLAY DEVICE, LIQUID CRYSTAL DISPLAY, ORGANIC EL DISPLAY, AND COLORANT COMPOUND AND TAUTOMER THEREOF
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A colored curable composition including: at least one selected from the group consisting of a compound represented by the following Formula (1a) and a tautomer thereof; and at least one polymerizable compound, wherein R11, R12, R13, R14, R15, and R16 each independently represent a hydrogen atom or a monovalent substituent; and R11 and R12, and R15 and R16 independently may bond to each other in each pair to form a ring.
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Page/Page column 118-119
(2010/12/29)
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- Synthesis and antimicrobial evaluation of some novel 2-aminothiazole derivatives of 4-hydroxy-chromene-2-one
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Syntheses of 2-aminothiazole derivatives of 4-hydroxy-chromene-2-one 2c-10c are reported in this paper. These compounds 2c-10c were prepared from 3-(2-bromoacetyl)-4-hydroxy-chromene-2-one 1 and corresponding thiourea derivatives 2b-10b using Hantzsch reaction. The structures of all compounds were confirmed by IR and 1H-NMR spectroscopy and elemental analyses. The molecules 2c-10c were evaluated for in vitro antimicrobial activity against ten bacteria and twelve fungi. All tested compounds exhibited antibacterial and antifungal activity.
- Vukovic, Nenad,Sukdolak, Slobodan,Solujic, Slavica,Milosevic, Tanja
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experimental part
p. 491 - 496
(2009/04/04)
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- A convenient and efficient method for the synthesis of mono- and N,N-disubstituted thioureas
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A convenient method for the synthesis of mono- and N,N-disubstituted thioureas by the debenzoylation of N-substituted- and N,N-disubstituted- N′-benzoylthioureas with hydrazine hydrate under solvent-free conditions has been developed. N-Substituted-N′-benzoylthioureas and hydrazine hydrate were mixed, and stirred at room temperature without a solvent to give the corresponding N-substituted thioureas in high yields.
- Kodomari, Mitsuo,Suzuki, Masato,Tanigawa, Keiko,Aoyama, Tadashi
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p. 5841 - 5843
(2007/10/03)
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- Selenoureas and thioureas are effective superoxide radical scavengers in vitro
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Oxygen radicals, such as superoxide radicals, embellishing DNA, protein, lipids, etc., and carrying out the obstacle of the function of a cell is known. It depends for the oxidant level in the living body on the balance of a generation system and an elimination system of oxygen radicals, and research which controls an oxidant level in the living body is briskly done by taking in the substance which eliminates an oxygen radical. We investigated scavenging effects of superoxide radicals by selenoureas and thioureas using a highly sensitive and quantitative chemiluminescence method. At 330 nM, five selenoureas and five thioureas scavenged fractions of superoxide radicals (O 2-) ranging from 8.4% to 87.6%. Among five N,N-unsubstituted selenoureas and N,N-unsubstituted thioureas 1-selenocarbamoylpiperidine and 1-thiocarbamoylpyrrolidine were the most effective scavengers. A possibility that selenoureas could use it as a new superoxide anion-scavenging substance from the result of this research became clear.
- Takahashi, Hitoe,Nishina, Atsuyoshi,Fukumoto, Ryo-Hei,Kimura, Hirokazu,Koketsu, Mamoru,Ishihara, Hideharu
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p. 2185 - 2192
(2007/10/03)
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- Synthesis of mono- and N,N-disubstituted thioureas and N-acylthioureas
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1-Benzotriazole-1-carbothioamide (2), prepared from 1-cyanobenzotriazole (1) and hydrogen sulfide, reacts with amines to give thioureas 3a-e. Reactions of (benzotriazol-1-yl)carboximidamides 4a-d,f-j and acyl- 5a-f,i-k or arylaminocarbonyl- 5g,h (benzotri
- Katritzky, Alan R.,Kirichenko, Nataliya,Rogovoy, Boris V.,Kister, Jeremy,Tao, Hui
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p. 1799 - 1805
(2007/10/03)
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- Preparation of N,N-unsubstituted selenoureas and thioureas from cyanamides
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Reaction of cyanamides with LiAlHSeH and LiAlHSH in the presence of HCl in diethyl ether provided the corresponding N,N-unsubstituted selenoureas and thioureas in moderate to high yields, respectively.
- Koketsu, Mamoru,Fukuta, Yoshihisa,Ishihara, Hideharu
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p. 6333 - 6335
(2007/10/03)
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- PIPERIDINE DERIVATIVES, PROCESS FOR OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula STR1 used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P-and neurokinin-dependent pathologies.
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- Synthesis of Mesoionic Triazoline Nucleosides
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A new type of protected mesoionic triazoline nucleoside was synthesized by the reaction protected 1,2-dideoxy-hydrazino-D-ribose or 1-deoxy-hydrazino-D-ribose with isothiouronium compounds.The three compounds obtained 10a, 10f and 16a were deprotected with tetrabutylammonium fluoride.They showed no activity against HSV-1 virus.
- Yokoyama, Masataka,Ikuma, Toshihiro,Obara, Nobutoshi,Togo, Hideo
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p. 3243 - 3247
(2007/10/02)
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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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