5 Sprague-Dawley rats per sex received a single oral gavage dose of [Phenyl- U-14C] ET-751 at 5 mg/kg. Immediately after dosing, each animal was transferred to a glass metabolism cage. Urine and feces were collected at 24 hour intervals through 96 hours. ... Metabolites in urine and feces were evaluated by high performance liquid chromatography (HPLC) and 2-D thin layer chromatography. ... Metabolites were identified in urine and feces ... As with [Pyrazole-5-14C] ET-751, the proposed metabolic pathways were ester hydrolysis and N-demethylation on the pyrazole ring 1 position and hydrolysis of the ether bond on 5 position of the phenyl ring to phenol and methylation to the methoxy moiety.
20 male Sprague-Dawley rats received non-labelled ET-751 Technical by oral gavage at 5 mg/kg/day for 14 days. On the 15th day, they received a single oral gavage dose of [Pyrazole-5- 14C] ET-751 at 5 mg/kg. ... Metabolites in urine, feces, plasma, and gastrointestinal contents were identified using high performance liquid chromatography (HPLC). At 96 hours, the total values were 26.66% and 64.44% for urine and feces respectively. ... At 96 hours, concentrations were at or below the limits of detection in all samples. Metabolites in urine, feces, and plasma were identified ... The proposed metabolic pathways were ester hydrolysis and N-demethylation on the pyrazole ring 1 position and hydrolysis of the ether bond on 5 position of the phenyl ring to phenol and methylation to the methoxy moiety.
6 male Sprague-Dawley rats with cannulated bile ducts received a single oral gavage dose of [Pyrazole-5-14C] ET-751 at 5 mg/kg. ... High performance liquid chromatography was used to identify metabolites. 17.90% (feces), 19.66% (urine) and 36.09% (bile) of dosed radioactivity were excreted during 48 hours post-dosing. 13.86% was found in the gastrointestinal contents and 2.86% in the gastrointestinal tract at 48 hours. Absorption from oral administration was estimated as 55.75% (urine and bile content combined). Metabolites in urine, feces, gastrointestinal tract, and gastrointestinal contents were identified ... Proposed metabolic pathways were ester hydrolysis and N-demethylation on the 1 position of the pyrazole ring and hydrolysis of the ether bond on the 5 position of the phenyl ring to the phenolic hydroxy moiety.
5 Sprague-Dawley rats per sex per group received a single dose of [Pyrazole-5-14C] ET-751 at 5 or 500 mg/kg followed by sacrifice 3, 6, 9, 24, 96, or 168 hours later. ... Metabolites were identified in urine, plasma, and feces ... Proposed metabolic pathways were ester hydrolysis and N-demethylation on the pyrazole ring 1 position and hydrolysis of the ether bond on the 5 position of the phenyl ring to phenol and methylation to the methoxy moiety.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：可能对人类致癌
Cancer Classification: Likely to be Carcinogenic to Humans
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
副作用
职业性肝毒素 - 第二性肝毒素：在职业环境中的毒性效应潜力是基于人类摄入或动物实验的中毒病例。
Occupational hepatotoxin - Secondary hepatotoxins: the potential for toxic effect in the occupational setting is based on cases of poisoning by human ingestion or animal experimentation.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Pyraflufen-ethyl was readily absorbed and excreted within 96 hours following a single or repeated oral dose of 5 mg/kg (plasma t1/2 of 3 to3.5 hours). However, at a dose of 500 mg/kg, absorption was saturated as indicated by Cmax values which did not reflect the 100- fold dose differential (2.7 to 2.8 Fg eq/g for the low-dose group and 100 to 107 Fg eq-hr/g for the high-dose group). Following single or multiple oral low doses (5 mg/kg) of pyraflufen ethyl, urinary excretion accounted for 27 to 33% of the administered radioactivity suggesting that a multiple exposure regimen did not affect the absorption/excretion processes. Urinary excretion was reduced to only 5 to 7% following a single 500 mg/kg dose. Excretion via the feces accounted for the remainder of the administered radioactivity in all treatment groups. Analysis of biliary excretion following a single 5 mg/kg dose showed that 36% of the administered dose appeared in the bile. Based upon the excretion data, total bioavailability of a low dose was approximately 56%. Biliary excretion data were not available for a high-dose group which prevented a definitive assessment of bioavailability. Excretory patterns did not exhibit gender-related variability. However, plasma and blood clearance was more rapid in females than in males as shown by plasma/blood radioactivity time-course and the greater AUC values for males (32.3 vs 18.4 Fg eq-hr/g for the low-dose group and 2,738 vs 1,401 Fg eq-hr/g for the high-dose group). Radioactivity concentrations indicated tissue concentrations at or near detection limits (generally <0.01 Fg eq/g and never exceeding 0.02 Fg eq/g) at 96 hours postdose for any tissues. Therefore, neither pyraflufen-ethyl nor its metabolites appear to undergo significant sequestration. Tissue burden data following compound administration did not suggest a specific target beyond those tissues, namely liver and kidney, which are associated with absorption and elimination of orally administered xenobiotics.[EPA 40 CFR Part 180
[EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
申请人：GILEAD APOLLO LLC
公开号：WO2017075056A1
公开（公告）日：2017-05-04
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
[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.
