The major metabolites were a variety of polar and non-polar compounds resulting from aromatic hydroxylations and heteroaromatic N-demethylation. The parent compound was the primary fecal component over the 1st 72 hr.
Most of the radioactivity was found to be in the form of fluridone or 4-hydroxyfluridone (1-methyl-3-(4-hydroxyphenyl)-5-(3-trifluoromethyl phenyl)-4(1H)-pyridinone) ... in tissues of fish exposed to /fluridone/ ...
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：人类非致癌性证据E组
Cancer Classification: Group E Evidence of Non-carcinogenicity for Humans
来源:Hazardous Substances Data Bank (HSDB)
毒理性
毒性数据
LC50 (大鼠) > 2130000 毫克/立方米/小时
LC50 (rat) > 2,130,000 mg/m3/1h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Dose levels of 2 mL/kg of water (5 male(M)/5 female (F)), 20% (6M/4F), 40% (5M/5F), and 80% (5M/5F) fluridone 4AS; (% 4AS doses = 192 (20%), 384 (40%), and 768 (80%) mg/kg fluridone); six hours exposure, occluded patch; dermal treatments were performed five days a week for three consecutive weeks; moderate to severe erythema and slight edema, epidermal fissures, slight decrease in relative kidney weights in male treated rabbits; NOEL = 2 mL/kg of 20% fluridone 4AS.
/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Fluridone Technical (EL-171) (purity: 98.6%); 5 animals/sex/group; Doses: 0, 1000 mg/kg, 6 hours/day, applied under a damp gauze pad. No mortality. Clinical Observations: sign of mild erythema at application site, no treatment-related systemic signs or effect upon body weights or food consumption; No treatment-related effect upon hematology or serum chemistry. Necropsy: no treatment-related lesions or effect upon organ weights. Histopathology: no treatment-related lesions. ...NOEL: 1000 mg/kg/day. /98.6% pure technical fluridone/
/In a rat metabolism study/... Preliminary study: Group A, 2 male (M)/2 female (F) exposed to a single oral dose of [14C]fluridone (...radiopurity 99.8%; for test solutions [14C]fluridone was mixed w/[12C]fluridone, ...100% purity; test substance was suspended in 1% sodium carboxymethyl cellulose [CMC]) at ~10 mg/kg. Group B, 1M/1F exposed to a single oral dose at ~1000 mg/kg. Urine, feces and cage rinses were collected daily for 7 days (because expired (trapped) 14CO2 accounted for <1% of the dose after 24 hr, further 14CO2 measurements were discontinued). Definitive study: Group C, vehicle controls, 2M/2F exposed to a single oral dose of 1% CMC. Group D, 5M/5F exposed to a single oral dose at ~7.4 mg/kg. Group E, 7M/7F exposed to ~10 mg/kg unlabeled fluridone once daily for 14 days, then 5M/5F exposed on day 15 to ~10 mg/kg [14C]fluridone. Group F, 5M/5F exposed to a single oral dose at ~900 mg/kg. ...Clinical signs (lack of mobility, abnormal and rapid head movement, squinting, loss of balance and cage biting) occurred only at the HD (Groups B and F), clearing within 24 hr. Results, Group A: by 7 days, 12.52%/12.89% (M/F) was excreted in urine and 72.76%/81.79% in feces. Group B: by 7 days 4.83%/3.43% was excreted in urine and 86.43%/86.31% in feces. Group D: by 24 hr 11.14%/10.44% was excreted in urine and 72.46%/77.72% in feces. By 7 days 11.61%/10.93% was excreted in urine and 79.19%/84.62% in feces. Combined excretion (including cage rinse) by 7 days was 92.93%/98.74%. Group E: by 24 hr 9.54%/8.51% was excreted in urine and 70.69%/69.90% in feces. By 7 days 10.11%/9.14% was excreted in urine and 79.80%/81.79% in feces. Combined excretion (including cage rinse) by 7 days was 92.81%/94.21%. Group F: by 24 hr 2.40%/2.43% was excreted in urine and 27.16%/27.18% in feces (thus, a relative delay in fecal excretion at the HD). By 7 days 8.30%/8.07% was excreted in urine and 91.58%/90.09% in feces. Combined excretion (including cage rinse) by 7 days was 101.02%/99.62%. Total tissue residues were always <1% of the dose (Groups D-F). Under all conditions, highest tissue levels occurred in the liver. The major metabolites were a variety of polar and non-polar compounds resulting from aromatic hydroxylations and heteroaromatic N-demethylation. The parent compound was the primary fecal component over the 1st 72 hr.
In a metabolism study in rats, fluridone was rapidly and almost completely absorbed into the systemic circulation and eliminated in both the male and female rats within 3 days. The total radioactivity recovered within 3 days after dosing in the urine and feces were 78-90% and 87- 97% of administered dose in males and females, respectively. The majority (approximately 70%) of the radioactivity was eliminated via feces. No tissue accumulation was observed.
The rates of uptake of ... (14C) fluridone (1-methyl-3-phenyl-5-(3-trifluoromethylphenyl)-4-(1H)-pyridinone) from water by rainbow trout and Chironomus tentans (4th Instar) larvae were much lower than those for more hydrophobic compounds tested under similar conditions ... Uptake and clearance of fluridone ... by chironomid larvae were more rapid than for rainbow trout. /BCF/ for chironomid larvae /was/ estimated to be 128 for fluridone ... Liver, intestine, and pyloric caeca of adult rainbow trout accumulated the highest residues of (14C)-fluridone ... Most of the radioactivity was found to be in the form of fluridone or 4-hydroxyfluridone (1-methyl-3-(4-hydroxyphenyl)-5-(3-trifluoromethyl phenyl)-4(1H)-pyridinone) ... in tissues of fish exposed to /fluridone/ ...
The bioconversion of 5-deoxystrigol to sorgomol by the sorghum, Sorghum bicolor (L.) Moench
摘要：
Strigolactones, important rhizosphere signalling molecules and a class of phytohormones that control shoot architecture, are apocarotenoids of plant origin. They have a structural core consisting of a tricyclic lactone connected to a butyrolactone group via an enol ether bridge. Deuterium-labelled 5-deoxystrigol stereoisomers were administered to aquacultures of a high sorgomol-producing sorghum cultivar, Sorghum bicolor (L) Moench, and conversion of these substrates to sorgomol stereoisomers was investigated. Liquid chromatography-mass spectrometry analyses established that 5-deoxystrigol (5-DS) and ent-2'-epi-5-deoxystrigol were absorbed by sorghum roots, converted to sorgomol and ent-2'-epi-sorgomol, respectively, and exuded out of the roots. The conversion was inhibited by uniconazole-P, implying the involvement of cytochrome P450 in the hydroxylation. These results provide experimental evidence for the postulated biogenetic scheme for formation of strigolactones, in which hydroxylation at C-9 of 5-DS can generate sorgomol. (C) 2013 Elsevier Ltd. All rights reserved.
[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.
