- 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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- 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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- Efficient Synthesis of Benzothiazinone Analogues with Activity against Intracellular Mycobacterium tuberculosis
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8-Nitrobenzothiazinones (BTZs) are a promising class of antimycobacterial agents currently under investigation in clinical trials. Starting from thiourea derivatives, a new synthetic pathway to BTZs was established. It allows the formation of the thiazinone ring system in one synthetic step and is applicable for preparation of a wide variety of BTZ analogues. The synthetic procedure furthermore facilitates the replacement of the sulphur atom in the thiazinone ring system by oxygen or nitrogen to afford the analogous benzoxazinone and quinazolinone systems. 36 BTZ analogues were prepared and tested in luminescence-based assays for in vitro activity against Mycobacterium tuberculosis (Mtb) using the microdilution broth method and a high-throughput macrophage infection assay.
- Richter, Adrian,Narula, Gagandeep,Rudolph, Ines,Seidel, Rüdiger W.,Wagner, Christoph,Av-Gay, Yossef,Imming, Peter
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supporting information
(2021/12/27)
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- Crystal structures and antimicrobial activities of copper(II) complexes of fluorine-containing thioureido ligands
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Cu(II) complexes with N-4-fluorobenzoylpiperidine-1-carbothioimidate (L1), N-2-fluorobenzoylpiperi-dine-1-carbothioimidate (L2) and 2-fluorobenzoate (L3) have been synthesized and characterized by elemental analysis, Fourier Transform infrared (FT-IR), Ul
- Liu, Huanhuan,Yang, Wen,Zhou, Weiqun,Xu, Yunlong,Xie, Juan,Li, Mengying
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p. 387 - 394
(2013/10/22)
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- [1,2,4]-Dithiazoli(di)ne derivatives, inducers of gluthathione-S-transferase and NADPH quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular
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The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of
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Page/Page column 6
(2008/06/13)
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- 1-(Methyldithiocarbonyl)imidazole: A useful thiocarbonyl transfer reagent for synthesis of substituted thioureas
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1-(Methyldithiocarbonyl)imidazole 1 and its N-methyl quaternary salt 2 have been shown to be efficient methyldithiocarbonyl and thiocarbonyl transfer reagents for the synthesis of dithiocarbamates, symmetrical and unsymmetrical mono-, di- and tri-substituted thioureas in high yields under mild and simple non-hazardous reaction conditions. (C) 2000 Elsevier Science Ltd.
- Mohanta, Pramod K.,Dhar, Sanchita,Samal,Ila,Junjappa
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p. 629 - 637
(2007/10/03)
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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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- Derivatives of cephalosporins, their process of separation and antibiotic drugs containing the said derivatives
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The present invention relates to cephalosporins having the formula: STR1 in which COOA is an acidic radical, salt or ester, and R1 represents a group: STR2 in which RA and RB are H or alkyl or together form a cycloalkyl with the carbon to which they are bonded, R2 and R3 are H, alkyl or alkenyl, R4 and R5 are H, alkyl or alkenyl or together form a ring to the nitrogen atom with which they are bonded. This invention also relates to a process for the preparation of these compounds and to drugs containing them.
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