Difethialone | 104653-34-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: Difethialone
• 英文别名: 3-[3-[4-(4-bromophenyl)phenyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-hydroxythiochromen-4-one
• CAS: 104653-34-1
• 化学式: C₃₁H₂₃BrO₂S
• 分子量: 539.5
• InChiKey: VSVAQRUUFVBBFS-UHFFFAOYSA-N

物化性质

• 熔点：
  203-227°
• 沸点：
  658.3±55.0 °C(Predicted)
• 密度：
  1.3614 g/cm3(Temp: 25 °C)
• 溶解度：
  氯仿：微溶；甲醇：微溶
• 颜色/状态：
  White, slightly yellowish powder
• 蒸汽压力：
  0.074 mPa at 25 °C= 5.55X10-7 mm Hg @ 25 °C

计算性质

• 辛醇/水分配系数(LogP)：
  8.3
• 重原子数：
  35
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  62.6
• 氢给体数：
  1
• 氢受体数：
  3

ADMET

毒理性

• 相互作用

以下药物可能会增加对香豆素或香豆素衍生物的反应：酒精（急性中毒）、别嘌醇、氨基水杨酸、胺碘酮、雄激素类固醇、水合氯醛、氯霉素、西咪替丁、吉非贝齐、复方新诺明、达那唑、右旋甲状腺素钠、二氮嗪、二氟尼柳、双硫仑、红霉素、依他尼酸、非诺洛芬钙、胰高血糖素、布洛芬、吲哚美辛、流感病毒疫苗、异烟肼、米索前列醇、甲芬那酸、甲巯咪唑、甲硝唑、咪康唑、萘啶酸、新霉素（口服）、己酮可可碱、保泰松、丙氧酚、丙硫氧嘧啶、奎尼丁、奎宁、水杨酸盐、链激酶、磺吡酮、磺胺类药物、舒林酸、四环素、噻嗪类药物、甲状腺药物、三环类抗抑郁药、尿激酶、维生素E。/香豆素和香豆素衍生物/

The following drugs ... may increase ... response to coumarin or indandione derivatives: alcohol (acute intoxication), allopurinol, aminosalicylic acid, amiodarone, anabolic steroids, chloral hydrate, chloramphenicol, cimetidine, clofibrate, co-trimoxazole, danazol, dextrothyroxine sodium, diazoxide, diflunisal, disulfiram, erythromycin, ethacrynic acid, fenoprofen calcium, glucagon, ibuprofen, indomethacin, influenza virus vaccine, isoniazid, meclofenamate, mefenamic acid, methylthiouracil, metronidazole, miconazole, nalidixic acid, neomycin (oral), pentoxifylline, phenylbutazone, propoxyphene, propylthiouracil, quinidine, quinine, salicylates, streptokinase, sulfinpyrazone, sulfonamides, sulindac, tetracyclines, thiazides, thyroid drugs, tricyclic antidepressants, urokinase, vitamin E. /Coumarin & indandione derivatives/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

以下是可能会降低香豆素或香豆素衍生物类药物效果的药物：酒精（慢性酒精中毒）、巴比妥类药物、卡马西平、皮质类固醇、促皮质激素、乙氯戊醇、氯喹咪唑、灰黄霉素、巯嘌呤、美沙酮、含有雌激素的口服避孕药、利福平、螺内酯、维生素K。/香豆素和香豆素衍生物/

The following drugs ... may ... decrease ... response to coumarin or indandione derivatives: alcohol (chronic alcoholism), barbiturates, carbamazepine, corticosteroids, corticotropin, ethchlorvynol, glutethimide, griseofulvin, mercaptopurine, methaqualone, oral contraceptives containing estrogen, rifampin, spironolactone, vitamin K. /Coumarin & indandione derivatives/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

人类暴露于第二代和茚满二酮类抗凝剂会产生与抗凝效果一致的 symptoms（例如，血肿，呕血，血尿，容易瘀伤）。对于暴露情况的治疗，特别是大量和反复暴露的情况，可能需要维生素 K1 疗法，并需在数月内监测凝血酶原时间。

Human exposure to second-generation and indandione anticoagulants produces symptoms consistent with anticoagulation effects (e.g., hematomas, hematemesis, hematuria, easy bruisability). Treatment of cases of exposure, particularly of substantial and repeated exposure, may require vitamin K1 therapy and monitoring of prothrombin times for periods of many months.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

我们报告了一位22岁的男性患者，因生命威胁性的凝血障碍被送往急诊室，其凝血酶原时间波动在5%至37%之间，因子II、VII、IX和X的活动性非常低。在入院前的一个月里，患者使用了杀鼠剂地亚硫磷，没有任何预防措施来避免意外接触。在获得口服维生素K1之前，患者通过使用新鲜冰冻血浆来维持。这种药物纠正了凝血障碍。

We report a 22 years old male, admitted to the emergency room due to a life threatening coagulation disorder, with prothrombin times fluctuation between 5 and 37% and very low activity of factors II, VII, IX and X. In the month prior to the admission, the patient had used the rodenticide difethialone, without any precaution to avoid accidental exposure. The patient was maintained with fresh frozen plasma until oral vitamin K1 was obtained. This medication corrected the coagulation disorder.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

荷兰犬类抗凝血杀鼠剂中毒的发生、诊断和治疗通过荷兰毒物控制中心（NPCC）对荷兰兽医进行的调查进行了评估。调查包括了54只狗的信息，其中32只由咨询NPCC的兽医治疗，22只被送往乌特勒支大学伴侣动物诊所（UUCCA）。被怀疑的毒物包括溴敌隆（n = 19）、溴鼠灵（n = 14）、杀鼠迷（n = 8）、敌鼠隆（n = 6）和氯鼠灵（n = 1）。在6只狗中，毒物的身份未知。在31只出现出血的狗中，有2只在接受兽医治疗后不久死亡，有2只在入住UUCCA后不久死亡。出血症状尤其出现在溴敌隆中毒的狗中（n = 16）。在没有出血的狗中，除了1只外，其余都是在就诊前24小时内摄入毒物。治疗方法各不相同，最常见的是催吐和使用维生素K。治疗方案的选择取决于摄入毒物后的时间长度、临床体征以及初次检查时是否怀疑有抗凝血毒性。

The occurrence, the diagnosis, and the treatment of anticoagulant rodenticide poisoning in dogs in the Netherlands was evaluated by a survey among Dutch veterinarians carried out by the National Poisons Control Center (NPCC). The survey included information on 54 dogs, 32 being treated by veterinarians who consulted the NPCC and 22 that were admitted to the Utrecht University Clinic for Companion Animals (UUCCA). The poisons that were suspected were brodifacoum (n = 19), bromadiolone (n = 14), difenacoum (n = 8), difethialone (n = 6) and chlorophacinone (n = 1). In 6 dogs the identity of the poison was unknown. Of 31 dogs with hemorrhages, 2 died shortly after presentation to practitioners and 2 died shortly after admission to the UUCCA. Signs of bleeding occurred especially in poisoning by brodifacoum (n = 16). In all but one of the dogs without hemorrhages, the intake of poison had taken place within 24 hours before presentation. The method of treatment varied, with the induction of vomiting and the use of vitamin K mentioned most. The choice of therapy was determined by the length of time after intake of the poison, the clinical signs and whether or not an anticoagulant toxicosis was suspected at the time of the initial examination.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在大鼠中，口服给药后，difethialone在血液中具有短半衰期，肝脏中具有较长半衰期，并且主要通过粪便排出，几乎没有代谢。

In rats, following oral admin, difethialone is characterised by a short half-life in blood, a longer half-life in liver, and an essentially fecal elimination with almost complete absence of metabolism.

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• [EN] MICROBIOCIDAL OXADIAZOLE DERIVATIVES<br/>[FR] DÉRIVÉS D'OXADIAZOLE MICROBIOCIDES
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2017157962A1

  公开（公告）日：2017-09-21

  Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially fungicides.

  式(I)的化合物，其中取代基如权利要求1所定义，作为杀虫剂特别是杀菌剂有用。
• [EN] INSECTICIDAL TRIAZINONE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZINONE INSECTICIDES
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2013079350A1

  公开（公告）日：2013-06-06

  Compounds of the formula (I) or (I'), wherein the substituents are as defined in claim 1, are useful as pesticides.

  式(I)或(I')的化合物，其中取代基如权利要求1所定义的那样，可用作杀虫剂。
• Novel insecticides
  申请人：Syngenta Participations AG

  公开号：EP2540718A1

  公开（公告）日：2013-01-02

  Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.

  式I的化合物 其中取代基如权利要求1所定义，并且式I化合物的农药可接受盐以及所有立体异构体和互变异构形式可用作杀虫剂，并且可以按照已知的方法制备。
• Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
  申请人：Dow AgroSciences LLC

  公开号：US20180279612A1

  公开（公告）日：2018-10-04

  This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

  这份披露涉及具有对节肢动物门、软体动物门和线虫门害虫具有杀虫效用的分子领域，用于生产此类分子的过程，用于此类过程的中间体，含有此类分子的杀虫组合物，以及使用此类杀虫组合物对抗此类害虫的过程。这些杀虫组合物可以用作螨虫剂、杀虫剂、螨虫剂、软体动物杀虫剂和线虫杀虫剂。本文件披露了具有以下式（“式一”）的分子。
• [EN] MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO<br/>[FR] MOLÉCULES PRÉSENTANT UNE UTILITÉ EN TANT QUE PESTICIDE, ET LEURS INTERMÉDIAIRES, COMPOSITIONS ET PROCÉDÉS
  申请人：DOW AGROSCIENCES LLC

  公开号：WO2017040194A1

  公开（公告）日：2017-03-09

  This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions aga inst such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula ("Formula One").

  这份披露涉及具有对节肢动物门、软体动物门和线虫门害虫有用的分子领域，用于生产这种分子的过程，用于这种过程的中间体，含有这种分子的杀虫剂组合物，以及使用这种杀虫剂组合物对抗这些害虫的过程。这些杀虫剂组合物可以用作螨虫剂、杀虫剂、螨虫剂、软体动物杀虫剂和线虫杀虫剂。本文件披露了具有以下化学式（“化学式一”）的分子。