Ethylene thiourea appears as white to pale green crystals or an off-white solid. Odorless when pure, but technical product may have an amine odor. (NTP, 1992)
颜色/状态:
Needles, prisms from alcohol or amyl alcohol
气味:
Faint, amine odor
蒸汽压力:
2.02X10-6 mm Hg at 25 °C (est)
分解:
When heated to decomposition it emits very toxic fumes of /nitroxides/ and /sulfoxides/.
The metabolic decomposition of EBDCs in mammals is complex and results in the formation of carbon disulfide, EDA, a few ethylene bisthiuram disulfides, hydrogen sulfide, ethylene bisthiocyanate, and ETU. The latter is further broken down to moieties that are incorporated into compounds such as oxalic acid, glycine, urea, and lactose. /Dithiocarbamate pesticides/
After treating plants with dithiocarbamates, a large number of metabolites are found, including ETU, EU, imidazole derivatives, diisothiocyanates, diamines, disulfides, and other metabolites that are still unknown. /Dithiocarbamate pesticides/
The various metal derivatives of ethylene bisdithiocarbamic acid appear to be converted in the soil to /5,6-dihydro-3 H-imidazo [2,1-C]-1,2,4-dithiazole-3-thione/ (DIDT), ETU, carbon disulfide, hydrogen sulfide, and carbonyl sulfide ... The conversion by soil bacteria and fungi of DIDT into ETU has been demonstrated ... Even though ETU is slowly converted into EU in soil, pure cultures of soil bacteria and fungi were unable to effect this transformation. /Dithiocarbamate pesticides/
来源:Hazardous Substances Data Bank (HSDB)
代谢
ETU分解成乙烯二胺(EDA)、尿素、二氧化碳或草酸,或在哺乳动物、植物和环境中转化为咪唑衍生物。
ETU is broken down to ethylene diamine (EDA), urea, carbon dioxide, or oxalic acid, or is transformed to imidazole derivatives in mammals, plants, and the environment.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类:B2组可能的人类致癌物
Cancer Classification: Group B2 Probable Human Carcinogen
Evaluation: There is inadequate evidence in humans for the carcinogenicity of ethylenethiourea. There is sufficient evidence in experimental animals for the carcinogenicity of ethylenethiourea. Overall evaluation: Ethylenethiourea is not classifiable as to its carcinogenicity to humans (Group 3). In making its evaluation, the Working Group concluded that ethylenethiourea produces thyroid tumors in mice and rats by a non-genotoxic mechanism, which involves interference with the functioning of the thyroid peroxidase, resulting in a reduction in circulating thyroid hormone concn and incr secretion of thyroid stimulating hormone. Consequently, ethylenethiourea would not be expected to produce thyroid cancer in humans exposed to concn that do not alter thyroid hormone homeostasis. An additional consideration of the Working Group, based on lack of genotoxicity of ethylenethiourea, was that the liver tumors in mice and benign tumors in rats were also produced by a non-genotoxic mechanism. Evidence from epidemiological studies and from toxicological studies in experimental animals provide compelling evidence that rodents are substantially more sensitive than humans to the development of thyroid tumors in response to thyroid hormone imbalance.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
乙烯硫脲:合理预期为人类致癌物。
Ethylene Thiourea: reasonably anticipated to be a human carcinogen.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
国际癌症研究机构致癌物:乙烯硫脲
IARC Carcinogenic Agent:Ethylenethiourea
来源:International Agency for Research on Cancer (IARC)
毒理性
致癌物分类
国际癌症研究机构(IARC)致癌物分类:第3组:对其对人类的致癌性无法分类
IARC Carcinogenic Classes:Group 3: Not classifiable as to its carcinogenicity to humans
来源:International Agency for Research on Cancer (IARC)
Dithiocarbamates and their metabolic products /including ETU/ are found in certain organs, such as the liver, kidneys, and, especially, the thyroid gland, but accumulation of these compounds does not take place because of their rapid metabolism. /Dithiocarbamate pesticides/
ETU is rapidly absorbed, metabolized, and excreted in mammals. Up to 90% is eliminated via the urine and only a small amount via the feces. Distribution of ETU in the body appears to be fairly uniform with the exception of a relative accumulation in the thyroid.
ETU is rapidly absorbed from the gastrointestinal tract and cleared from the body in all the mammalian species that have been tested. After only 5 min, ETU appeared in the blood of rats administered an oral dose of 100 mg (14)C-ETU/kg bw. Within 48 hr, 82 - 99% of an oral dose was eliminated via the urine and about 3% via the feces ... /Another study found/ approximately 70% was eliminated in the urine and 1% in the feces. Comparable results were found for mice while in monkeys, 55% was eliminated via the urine within 48 hr and less than 1.5% via the feces ...
To study the accumulation and elimination of radioactivity by the thyroid gland of rats dosed with (14)C-ETU, dose levels of 2 and 200 ug labeled ETU were administered daily for 14 days. In another study, rats were dosed with 0, 0.1, 1, 10, 50, or 100 mg (14)C-ETU/kg diet, daily, for 7 days. The first study showed that the concentration of ETU and/or its metabolites in the thyroid is dose-dependent, and the second that the level of (14)C in the thyroid did not increase appreciably when the daily dose was increased above 50 mg/kg diet. Withdrawal of ETU from the diet led to an 80 - 94% reduction in the radioactivity in the thyroid after 17 days ...
Crystal structures of polyiodide salts and molecular complexes. 7. Interaction of thiones with molecular diiodine. The crystal structures of dithizone-diiodine, ethylenethiourea-bis(diiodine), bis(ethylenethiourea)-tris(diiodine), bis(dithizone)-heptakis(diiodine), and 1-(1-imidazolin-2-yl)-2-thioxoimidazolidinium triiodide-(ethylenethiourea-diiodine)
Melanocortin-4 receptor binding compounds and methods of use thereof
申请人:Millennium Pharmaceuticals, Inc.
公开号:US20040082779A1
公开(公告)日:2004-04-29
Provided are MC4-R binding compounds of the formula XVII:
1
wherein L
2
is a linker group, and P
1
, P
2
, P
3
, P
4
, Z
1
, Z
2
, Z
3
, Z
4
, Z
5
, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.
Structures of Addition Products of Acetylenedicarboxylic Acid Esters with Various Dinucleophiles. An application of C, H-spin-coupling constants
作者:Ulrich Vögeli、Wolfgang von Philipsborn、Kuppuswamy Nagarajan、Mohan D. Nair
DOI:10.1002/hlca.19780610207
日期:1978.3.8
Heterocyclic compounds obtained by addition of acetylenedicarboxylicacidesters to thioureas, cyclic amidines and o-difunctionalized aromatic systems have been studied by 13C-NMR. In particular, C, H-spin-coupling constants over two and three bonds were used to differentiate between the various constitutional isomers and to establish the configuration of trisubstituted exocyclic C, C-double bonds
Palladium(0)-Catalyzed, Copper(I)-Mediated Coupling of Boronic Acids with Cyclic Thioamides. Selective Carbon−Carbon Bond Formation for the Functionalization of Heterocycles<sup>†</sup>
作者:Hana Prokopcová、C. Oliver Kappe
DOI:10.1021/jo070408f
日期:2007.6.1
Employing controlled microwaveirradiation at 100 °C, most cross-couplings can be completed within 2 h and proceed in high yields. An advantage of using thioamides as starting materials is the fact that the system can be tuned to an alternative carbon−sulfur cross-coupling pathway by changing to stoichiometric copper(II) under oxidative conditions. Both types of thioamide cross-couplings are orthogonal to
[EN] cGAS ANTAGONIST COMPOUNDS<br/>[FR] COMPOSÉS ANTAGONISTES DU CGAS
申请人:IMMUNE SENSOR LLC
公开号:WO2017176812A1
公开(公告)日:2017-10-12
Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.