... Three different doses of TCMTB in olive oil were given to male rats by gavage for 3 weeks. Urine was collected daily and the metabolites were analysed as thioethers by derivatization with pentafluorobenzyl-bromide by gas chromatography-mass spectrometry. The parent chemical was not detected in urine samples, but two metabolites of TCMTB were identified. 2-Mercaptobenzothiazole (2-MBT) was the main metabolite, and its excretion varied according to the dose. The second metabolite was 2-(mercaptomethylthio)benzothiazole. The amount of 2-MBT excreted in rat urine was 66 +/- 12% (SD), 51 +/- 20% and 44 +/- 9% for TCMTB doses of 15, 75 and 150 mg/kg, respectively. Two doses, 75 and 150 mg/kg, caused diuresis in rats during the 1 week of dosing. During the 3-week TCMTB treatment, rat liver microsomal CYP enzyme profile was not significantly changed.
Organic nitriles are converted into cyanide ions through the action of cytochrome P450 enzymes in the liver. Cyanide is rapidly absorbed and distributed throughout the body. Cyanide is mainly metabolized into thiocyanate by either rhodanese or 3-mercaptopyruvate sulfur transferase. Cyanide metabolites are excreted in the urine. (L96)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
毒性总结
识别和使用:硫氰酸,(2-苯并噻唑基硫基)甲基酯(TCMTB)是一种具有刺激性气味的油。它被用作木材防腐剂、海洋生物杀灭剂、杀菌剂,以及油漆中的防腐剂。它还广泛应用于皮革生产。人类暴露和毒性:在TCMTB工厂中一致出现的症状包括眼睛周围干燥的皮肤、带血的鼻涕、鼻出血、脱皮、皮肤灼热或瘙痒以及皮肤发红或皮疹。根据动物研究,美国环保局将TCMTB归类为C组,可能的 human carcinogen(人类致癌物)。
动物研究:在大鼠中,TCMTB具有中等到低度的急性口服毒性,而在兔中具有低度的皮肤毒性。在啮齿动物的亚慢性口服暴露后,TCMTB导致轻度到重度胃部病变的发生率增加,这些病变的特点是炎症、增生、坏死和溃疡。在一项为期21天的大鼠皮肤毒性研究中,TCMTB在所有剂量组中从治疗第3-4天开始产生剂量依赖性的皮肤刺激,并逐渐发展为焦痂形成。中剂量和高剂量组的大鼠出现了溃疡、出血和慢性皮炎。还注意到体重增加减少、食物消耗减少以及血液学(血红蛋白、红细胞压积和分叶中性粒细胞的变化)和临床化学变化(血尿素氮、葡萄糖、球蛋白升高和血清天门冬氨酸转氨酶(AST)升高)。然而,临床化学变化与肝脏或肾脏的任何治疗相关发现不一致。在一项慢性大鼠毒性/致癌性研究中,在最高测试剂量20 mg/kg/天下未观察到不良影响。然而,中剂量和高剂量水平的雄性大鼠睾丸间质细胞腺瘤的发生率有统计学上的显著增加,并且具有高度显著的阳性剂量相关趋势。治疗还与中剂量和高剂量水平的雌性大鼠甲状腺C细胞腺瘤的发生率可能增加有关,这具有高度显著的阳性剂量相关趋势,但在与同期对照组的比较中未达到统计学显著水平。在细菌基因突变试验中,TCMTB被发现不具有诱变性,并未在大鼠肝细胞试验中引起非计划DNA合成(UDS)的增加。TCMTB在小鼠体内微核试验中也未发现具有染色体畸变。因此,TCMTB不具有诱变或遗传毒性。
生态毒性研究:在三种幼年鲑科鱼类(Oncorhynchus kisutch, O. tshawytscha 和 O. mykiss)中评估了TCMTB。发现TCMTB对鳃组织学具有浓度和时间依赖性效应,在浓度为6微克/升时即可观察到损害。检查了抑制游泳速度和观察到的鳃损伤之间的关系。这些游泳速度的降低可能代表了由于TCMTB诱导的鳃结构改变导致的鳃氧气传输能力的限制。
IDENTIFICATION AND USE: Thiocyanic acid, (2-benzothiazolylthio) methyl ester (TCMTB) is an oil with a pungent odor. It is used as wood preservative, marine biocide, fungicide, and as a preservative in paint. It is also widely employed in leather production. HUMAN EXPOSURE AND TOXICITY: Symptoms consistently elevated in TCMTB mills included dry skin around the eyes, blood-stained mucus from the nose, nose bleed, peeling skin, burning or itching skin, and skin redness or rash. TCMTB has been classified by EPA as group C, possible human carcinogen, based on animal studies. ANIMAL STUDIES: TCMTB was of moderate to low acute oral toxicity in rats and of low dermal toxicity in rabbits. Following subchronic oral exposures to rodents, TCMTB caused increased incidence of mild to severe stomach lesions characterized by inflammation, hyperplasia, necrosis, and ulceration. In a 21-day rat dermal toxicity study, TCMTB produced dose-dependant dermal irritation in all dose groups beginning on treatment days 3-4, which progressed to eschar formation. Rats in the mid and high dose group had ulcers, hemorrhages and chronic dermatitis. Decreased body weight gain, food consumption, and hematological (changes in hemoglobin, hematocrit, and segmented neutrophils) and clinical chemistry changes (blood urea nitrogen, glucose, globulins, and elevated serum aspartate aminotransferase (AST) were also noted. However, the clinical chemistry changes did not correspond to any treatment-related findings in the liver or kidney. In a chronic rat toxicity/carcinogenicity study, no adverse effects were noted at the highest dose tested of 20 mg/kg/day. However, there was a statistically significant increase in the incidence of testicular interstitial cell adenomas in males of mid- and high-dose levels that had a highly significant positive dose-related trend. Treatment was also associated with a possible increased incidence of thyroid C-cell adenomas in females of the mid- and high-dose levels, which had a highly significant positive dose-related trend, but did not attain a statistically significant level in the pairwise comparison with concurrent controls. TCMTB was found to be negative for mutagenicity in the gene mutation assay with bacteria and did not cause an increase in unscheduled DNA synthesis (UDS) in the rat hepatocytes assay. TCMTB was also found to be negative for chromosomal aberrations in the in vivo micronucleus assay in mice. Therefore, TCMTB is not mutagenic or genotoxic. ECOTOXICITY STUDIES: TCMTB was evaluated in three species of juvenile salmonids (Oncorhynchus kisutch, O. tshawytscha and O. mykiss). TCMTB was found to have both a concentration- and time-dependent effect on gill histology with damage apparent at concns as low as 6 ug/L. The relationship between the inhibitory effect on swimming speed and the observed gill damage was examined. These reductions in swimming speed may represent a limitation in gill oxygen transfer capacity resulting from TCMTB-induced alteration of gill structure.
Organic nitriles decompose into cyanide ions both in vivo and in vitro. Consequently the primary mechanism of toxicity for organic nitriles is their production of toxic cyanide ions or hydrogen cyanide. Cyanide is an inhibitor of cytochrome c oxidase in the fourth complex of the electron transport chain (found in the membrane of the mitochondria of eukaryotic cells). It complexes with the ferric iron atom in this enzyme. The binding of cyanide to this cytochrome prevents transport of electrons from cytochrome c oxidase to oxygen. As a result, the electron transport chain is disrupted and the cell can no longer aerobically produce ATP for energy. Tissues that mainly depend on aerobic respiration, such as the central nervous system and the heart, are particularly affected. Cyanide is also known produce some of its toxic effects by binding to catalase, glutathione peroxidase, methemoglobin, hydroxocobalamin, phosphatase, tyrosinase, ascorbic acid oxidase, xanthine oxidase, succinic dehydrogenase, and Cu/Zn superoxide dismutase. Cyanide binds to the ferric ion of methemoglobin to form inactive cyanmethemoglobin. (L97)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌物分类
对人类不具有致癌性(未被国际癌症研究机构IARC列名)。
No indication of carcinogenicity to humans (not listed by IARC).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
该物质可以通过吸入其气溶胶和通过吞食被吸收进人体。
The substance can be absorbed into the body by inhalation of its aerosol and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
毒理性
吸入症状
咳嗽。
Cough.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
1.周国泰,化学危险品安全技术全书,化学工业出版社,1997 2.国家环保局有毒化学品管理办公室、北京化工研究院合编,化学品毒性法规环境数据手册,中国环境科学出版社.1992 3.Canadian Centre for Occupational Health and Safety,CHEMINFO Database.1998 4.Canadian Centre for Occupational Health and Safety, RTECS Database, 1989
Muthusubramanian, Lakshmi; Mitra, Rajat B.; Sundara Rao, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1996, vol. 35, # 12, p. 1331 - 1334
[EN] SUBSTITUTED QUINAZOLINES AS FUNGICIDES<br/>[FR] QUINAZOLINES SUBSTITUÉES, UTILISÉES EN TANT QUE FONGICIDES
申请人:SYNGENTA PARTICIPATIONS AG
公开号:WO2010136475A1
公开(公告)日:2010-12-02
The present invention relates to a compound of formula (I) wherein wherein the substituents have the definitions as defined in claim 1or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
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。
Thieno-pyrimidine compounds having fungicidal activity
申请人:Brewster Kirkland William
公开号:US20070093498A1
公开(公告)日:2007-04-26
The present invention relates to thieno[2,3-d]-pyrimidine compounds having fungicidal activity.
本发明涉及具有杀真菌活性的噻吩[2,3-d]-嘧啶化合物。
[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。
THIENYLPYRIDYLCARBOXAMIDES
申请人:Dunkel Ralf
公开号:US20110105564A1
公开(公告)日:2011-05-05
Novel thienylpyridylcarboxamides of the formula (I)
The present application is also directed to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.