Samples ... extracted and analyzed for the presence of metabolites using techniques including thin-layer chromatography and mass spectroscopy. Absorbed quinclorac was metabolized to only a limited extent, with unchanged parent compound representing approximately 80% of the excreted radiolabel. The major biotransformation product was quinclorac-glucuronide conjugate, representing approximately 5% of the administered dose. The pattern of metabolism was similar across sexes, dose levels and administration of repeated doses. A number of metabolites each representing less than 5% of the administered dose were not identified. The metabolism of quinclorac is so limited that a metabolic pathway is considered unnecessary.
IDENTIFICATION AND USE: Quinclorac is a herbicide. HUMAN STUDIES: It induced chromosomal aberrations in cultured human lymphocytes. ANIMAL STUDIES: It produced no sensitization reactions in a guinea-pig maximization test. Quinclorac was fed to groups of Beagle dogs in the diet at a dose of 0, 1,000, 3,000, 9,000 or 27,000 ppm for 28 days. At 27,000 ppm, feed consumption was reduced in females, and there was body weight loss over the duration of the study in both sexes. Kidney lesions were present at the top dose level. In mice Quinclorac was administered in a diet, at dose levels of 0, 4,000, 8,000, or 16,000 ppm. At 8000 and 16000 ppm there was an increase in water intake in males and females and blood urea nitrogen in males. There was decreased kidney weight in males and females and relative kidney weight in males in the 16,000 ppm group. At 4000 ppm there was decreased body weight gain in males and females. In rats given Quinclorac at dose levels of 0, 1,000, 4,000, or 12,000 ppm in a diet, noted decreases in body weight gain, food consumption and an increase in water intake in males and females, and decrease in monocytes in female, increases in liver enzymes in males, and pathological changes in kidneys of males. Quinclorac did not induce tumors in mice, rats or dogs. In rabbits the developmental toxicity observed at 600 mg/kg/day consisted of increased rate of resorption and post-implantation loss, a decrease in the number of live fetuses, and reduced fetal body weight. No structural anomalies were observed in rats in a 2-generation reproduction study. There were no effects noted for neuropathology or brain weight determinations in rats. Bacterial reverse gene mutation test was negative with or without metabolic activation in Salmonella typhimurium strains TA98, TA100, TA1535, TA1537. ECOTOXICITY STUDIES: When tested in fingerlings of the silver catfish (Rhamdia quelen), acetylcholinesterase (AChE) activity was evaluated in brain and muscle tissue of fish exposed to different herbicide concentrations. Quinclorac caused increases in enzyme activity in the brain and inhibitions in muscle tissue. In fish species Cyprinus carpio exposed to the quinclorac herbicide the levels of antioxidant enzymes and oxidative stress were increased.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
对人类无致癌性(未列入国际癌症研究机构IARC清单)。
No indication of carcinogenicity to humans (not listed by IARC).
/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W TKO /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) or lorazepam (Ativan) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/
The extent of oral absorption was high (> 90%), based on urinary and biliary data, with most of the biliary component reabsorbed and excreted in urine. The biliary component increased disproportionately with increasing dose from 15 to 600 mg/kg bw. Absorption of radiolabel was rapid, with maximal blood concentrations achieved between 0.25 and 1 hour for single doses of 600 mg/kg bw and below. Quinclorac was widely distributed in the body, with highest concentrations present in the blood, plasma and kidneys. Tissue levels were generally higher (< 2-fold) in females than in males. The labelled material was rapidly excreted, primarily via urine (50-90% in 24 hours). Initial plasma half-lives were calculated to be approximately 3-4 hours. Clearance from the blood was slower following repeated dosing with 600 mg/kg bw and with single doses of 1200 mg/kg bw, resulting in non-proportionate increases in the area under the concentration-time curve (AUC). The excretion pattern and tissue distribution of radioactivity were similar across administered dose levels and when the administration of radiolabelled quinclorac was preceded by 7 or 14 days of administration of the labelled or unlabelled material.
The metabolism of quinclorac ((2,3,4-(14)C)3,7-dichloro-8-quinolinecarboxylic acid) following oral administration was studied extensively in male and female CD rat. The compound was rapidly absorbed and eliminated in the urine following administration of single oral doses of (14)C quinclorac at 15 or 600 mg/kg and at 15 mg/kg after the animals were dosed with unlabeled quinclorac at 15 mg/kg/day for 14 days. Elimination in the urine 5 days after dosing accounted for 91 to 98% of the dose with only 1 to 4% eliminated in the feces. No radioactivity was detected in expired air. Biliary excretion was significant (11.5 to 14.5% of the dose) in animals receiving 600 mg/kg. However, most of this radioactivity was reabsorbed from the intestines and eliminated in the urine. Most of the radioactivity in the bile is associated with the glucuronide conjugate of quinclorac. The conjugate is apparently hydrolyzed in the intestines and reabsorbed. Almost all the radioactivity in the urine is unchanged quinclorac. Radioactive tissue residue levels 5 days after dosing were dose-dependent. Results from these and other (whole-body autoradiography and time-course) studies indicate that quinclorac may accumulate in the adrenal glands, bone marrow, thyroid, squamous epithelium of the non-fundic stomach, and ovaries.
In 7-day time-course studies (oral gavage at 15 mg/kg/day or dietary at about 1,000 mg/kg/day) maximum (14)C residue levels were detected 30 minutes after the final dose; thereafter, residue levels decreased with time. Mean (14)C residues in plasma were also detected at 30 minutes in animals receiving single oral doses of 15, 100, or 600 mg/kg or 15 mg/kg/day for 7 days. Elimination was biphasic with half-lives of 3 to 4 hours for the rapid phase at the low doses and a half-life of about 13 hours at 600 mg/kg. Peak plasma levels of radioactivity in animals receiving higher doses (1200 mg/kg or 600 mg/kg/day for 7 days) were noted for 7 to 48 hours postdosing: saturation kinetics were also noted at these higher doses.
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
[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] 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.