Orally dosed tebuthiuron was readily absorbed in mice, rats, rabbits, dogs, and ducks. The compound was extensively metabolized and the metabolites were rapidly excreted in the urine of mice, rats, rabbits, and dogs and in the mixture of urine and feces in ducks. The major metabolites of tebuthiuron were formed by N-demethylation of the substituted urea side chain in each species examined, including fish. Oxidation of the dimethylethyl group occurred in mice, rats, dogs, rabbits, and ducks. The N-demethylation reaction at the 3-position of the urea preceded through an N-hydroxymethyl intermediate. No accumulation of tebuthiuron or its metabolites was observed in the animals, a finding consistent with the low order of toxicity observed in other studies.
来源:Hazardous Substances Data Bank (HSDB)
代谢
在植物中，主要的代谢途径涉及叔丁基侧链的N-去甲基化和羟基化。
In plants, the principal metabolic pathways involve N-demethylation and hydroxylation of the tert-butyl side chain.
Tebuthiuron was administered by gavage to male and female ICR mice, Harlan rats, Dutch-Belted rabbits and beagle dogs at a dose of 10 mg/kg. Examination of urine extracts by thin-layer chromatography showed the presence of eight radioactively labeled metabolites in rat, rabbit and dog urine and seven in mouse urine. Small amt of unchanged tebuthiuron also were detected in each case (except the mouse). The major metabolites were formed by N-demethylation of the substituted urea side chain in each species examined. Oxidation of the dimethylethyl group also occurred in all species examined.
来源:Hazardous Substances Data Bank (HSDB)
代谢
在代谢研究中，给Fischer 344大鼠（公鼠和母鼠）单次低剂量口服（10 mg/kg）或重复低剂量口服（10 mg/kg x 14天）或单次高剂量（100 mg/kg）的(14)C-特丁脲。通过高效液相色谱和质谱分析尿液样本，鉴定出6种特丁脲的代谢物。主要的代谢物被鉴定为/N-[5-(2-羟基-1,1-二甲基乙基)-1,3,4-噻二唑-2-基]-N'-羟甲基-N-甲基脲/和/or/N-[5-(2-羟基-1,1-二甲基乙基)-1,3,4-噻二唑-2-基]-N-甲基脲/，都是特丁脲的羟基化代谢物。这种代谢物在0-24小时的大鼠尿液中的给药剂量占比为39.6-60.3%。第二丰富的代谢物被鉴定为特丁脲的代谢物/N-[5-(1,1-二甲基乙基)-1,3,4-噻二唑-2-基)脲/。在低剂量大鼠的0-24小时尿液中，这占了给药剂量的9-15%，而对于公鼠和母鼠，分别占了55.6%和57.3%。另外两种被鉴定的代谢物（/N-[5-(1,1-二甲基乙基)-1,3,4-噻二唑-2-基]-N-甲基脲/）(/ N-[5-(1,1-二甲基乙基)- 1,3,4-噻二唑-2-基]-N'-羟甲基-N-甲基脲/)和/N-[5-(2-羟基-1,1-二甲基乙基)-1,3,4-噻二唑-2-基]-N,N'-二甲基脲/，在公鼠和母鼠的0-24小时尿液中的给药剂量占比为2-10%。粪便中含有少量的/N-[5-(2-羟基-1,1-二甲基乙基)-1,3,4-噻二唑-2-基]-N-甲基脲/和/N-[5-(2-羟基-1,1-二甲基乙基)- 1,3,4-噻二唑-2-基]-N'-羟甲基-N-甲基脲/，平均占给药剂量的3.5%。
In a metabolism study male and female Fischer 344 rats were dose with (14)C-tebuthiuron at a single low oral dose (10 mg/kg), a repeated low oral dose (10 mg/kg x 14 days), or a single high dose (100 mg/kg) ... From HPLC and mass spectral analysis of urine samples, 6 metabolites of tebuthiuron were identified. The major metabolite was identified as /N-[5-(2-hyroxy-1, 1-dimethylethyl)-1, 3, 4-thiadiazol-2-yl]-N'-hydroxymethyl-N-methyl urea/ and/or/N-[5-(2-hydroxy-1, 1-dimethylethyl)-1, 3, 4-thiadiazol-2-yl]-N-methylurea/, both hydroxylated metabolites of tebuthiuron. This metabolite composed between 39.6-60.3% of the administered dose in 0-24 hour urine of male and female rats. The second most abundant metabolite was identified as metabolite /N-[5-(1, 1-dimethylethyl)-1, 3, 4-thiadiazol-2-yl) urea/ of tebuthiuron. This comprised between 9-15% of the administered dose in 0-24 hour urine of low dose rats, and between 55.6% and 57.3% of the administered dose for male and female rats, respectively. Two other metabolites identified, (/N-[5-(1, 1-dimethylethyl)-1, 3, 4-thiadiazol-2-yl]-N-methylurea/)/(/ N-[5-(1, 1-dimethylethyl)- 1, 3, 4-thiadiazol-2-yl]-N'-hydroxymethyl-N-methylurea/) and /N-[5-(2-hydroxy-1, 1-dimethylethyl)-1, 3, 4-thiadiazol-2-yl]-N, N'-dimethylurea/, comprised between 2-10% of the administered dose in male and female 0-24 hour urine. Feces contained minor amounts of / N-[5-(2-hydroxy-1, 1-dimethylethyl)-1, 3, 4-thiadiazol-2-yl]-N-methylurea / and / N-[5-(2-hydroxy-1, 1-dimethylethyl)- 1, 3, 4-thiadiazol-2-yl]-N'-hydroxymethyl-N-methylurea/, accounting for an average of 3.5% of the administered dose.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：D组 不可归入人类致癌性类别
Cancer Classification: Group D Not Classifiable as to Human Carcinogenicity
来源:Hazardous Substances Data Bank (HSDB)
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
毒性数据
LC50 (rat) >3696 mg/m3
大白鼠LC50>3696 mg/m3
LC50 (rat) >3696 mg/m3
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Skin contamination should be treated promptly by washing with soap and water. Contamination of the eyes should be treated immediately by prolonged flushing of the eyes with large amounts of clean water. If dermal or ocular irritation persists, medical attention should be obtained without delay. /Other Herbicides/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
解毒与急救
活性炭可能有效地限制刺激作用，并减少对这大多数或所有除草剂的吸收。/其他除草剂/
Activated charcoal is probably effective in limiting irritant effects and reducing absorption of most or all of these herbicides. /Other herbicides/
Tebuthiuron technical (99.6% pure) at 10 mg/kg (containing 5% w/w (14C)-EL103) was administered to ICR mice, Harlan rats, Dutch-belted rabbits and mallards by gavage (vehicle = water or 5% (w/v) acacia) and to beagle dogs by gelatin capsule. Bluegills received 25 ppm EL103 (plus 0.01% w/w (14C)-EL103) in the aquarium water. Tebuthiuron was readily absorbed by mice, rats, rabbits, dogs and ducks. It was extensively metabolized (with differences in proportions of metabolites produced) and metabolites were excreted in urine of mice, rats, rabbits and dogs and in urine/feces mix in ducks. By 96 hours, approximately 3% of metabolites were in feces of rats, dogs, rabbits and ducks, with 30% detected in feces of mice. ... Tebuthiruon did not accumulate (nor did metabolites) in tissues of any species tested.
Radiolabeled tebuthiuron was administered to male and female ICR mice, Harlan rats, Dutch-Belted rabbits and beagle dogs at a dose of 10 mg/kg by gavage. Elimination of radioactivity was virtually complete within 72 hours and recovery values at 96 hours were 96.3, 94.5, 94.3 and 95.7% in the mouse, rat, rabbit and dog, respectively. In the rats, rabbits and dogs, the radioactivity was excreted almost exclusively in the urine. In the mice, 30% of the radioactivity was excreted in the feces.
/It has been/ reported that 94 to 96% of a single oral dose of tebuthiuron (10 mg/kg) was excreted in the urine of rats, rabbits and dogs. In mice, 66% was excreted in the urine, and 30% in the feces. These data indicate that tebuthiuron was well absorbed (about 70 to 96%) from the gastrointestinal tract.
... Tebuthiuron /was administered/ in the diet to 20 pregnant Wistar rats at levels of 100 or 200 ppm for 6 days prior to delivery. Forty-eight hr after delivery, radiolabelled tebuthiuron was reintroduced into the diet at the same levels as before. Radioactive label was detected in the milk at mean levels of 2.7 and 6.2 ppm for the 100 and 200 ppm groups, respectively.
[EN] 3-[(HYDRAZONO)METHYL]-N-(TETRAZOL-5-YL)-BENZAMIDE AND 3-[(HYDRAZONO)METHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE DERIVATIVES AS HERBICIDES<br/>[FR] DÉRIVÉS DE 3-[(HYDRAZONO))MÉTHYL]-N-(TÉTRAZOL-5-YL)-BENZAMIDE ET DE 3-[(HYDRAZONO)MÉTHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE UTILISÉS EN TANT QU'HERBICIDES
申请人：SYNGENTA CROP PROTECTION AG
公开号：WO2021013969A1
公开（公告）日：2021-01-28
The present invention related to compounds of Formula (I): or an agronomically acceptable salt thereof, wherein Q, R2, R3, R4, R5 and R6 are as described herein. The invention further relates to compositions comprising said compounds, to methods of controlling weeds using said compositions, and to the use of compounds of Formula (I) as a herbicide.
[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。
[EN] HERBICIDALLY ACTIVE HETEROARYL-S?BSTIT?TED CYCLIC DIONES OR DERIVATIVES THEREOF<br/>[FR] DIONES CYCLIQUES SUBSTITUÉES PAR HÉTÉROARYLE À ACTIVITÉ HERBICIDE OU DÉRIVÉS DE CELLES-CI
申请人：SYNGENTA LTD
公开号：WO2011012862A1
公开（公告）日：2011-02-03
The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
The present invention provides triazole compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
本发明提供了三唑化合物，可用作乙酰辅酶A羧化酶（ACC）的抑制剂，以及其组合物和使用方法。
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”).
