Metabolism of rimsulfuron in plants and other animals (poultry and ruminants) appears to be similar to its metabolism in rats. Metabolism involves either the contraction or cleavage of the sulfonylurea bridge. While the cleavage of the bridge to form the pyridinesulfonamide metabolite is expected, the contraction reaction is not. The major residue found in plants is the parent compound, rimsulfuron.
The metabolism of (14)C-labeled rimsulfuron was studied in male and female rats. The low dose groups were treated once by oral gavage with 25 mg/kg (14)C -pyridine-labeled compound and the high dose groups with 250 mg/kg of either (14)C -pyridine- or (14)C-pyrimidine-labeled compound. The repeat dose groups were gavaged orally with unlabeled test compound (25 mg/kg) for 14 consecutive days, followed on the 15th day by 25 mg/kg of (14)C -pyridine-test compound. ... The metabolic profiles were determined using pooled urinary and fecal samples. The highest percentage of the urinary (42 to 55%) and fecal (5 to 16%) radioactivity was attributed to unmetabolized parent compound. The parent compound is metabolized by cleavage or contraction of the sulfonylurea bridge, leading to the formation of 3- (ethylsulfonyl)-2-pyridinesulfonamide (IN-E9260) or N-(4, 6-dimethoxy-2-pyrimidinyl)-N-((3-ethylsulfonyl)-2-pyridinyl) urea (IN-70941). IN-70941 is deamidated to form IN-70942, which is sequentially demethylated and hydroxylated.
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).
/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 the 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/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
解毒与急救
/SRP:/ 高级治疗：对于无意识、严重肺水肿或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。使用气囊面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿……。对于严重的支气管痉挛，考虑给予β激动剂，如沙丁胺醇……。监测心率和必要时治疗心律失常……。开始静脉输注D5W /SRP: "保持开放"，最低流量/。如果出现低血容量的迹象，使用0.9%生理盐水（NS）或乳酸林格氏液。对于伴有低血容量迹象的低血压，谨慎给予液体。注意液体过载的迹象……。使用地西泮或劳拉西泮治疗癫痫……。使用丙美卡因氢氯化物协助眼部冲洗……。 /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 /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's 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 or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/
/GENOTOXICITY/ /In a/ structural chromosome aberration /assay/, human Lymphocytes /were exposed to/ rimsulfuron (DPX-E9636-22, purity: 98.8%) /at concentrations of/ 0, 0.1, 0.6, 1.0, and 1.3 mg/mL (high dose based on peak solubility) 3 hr exposure. No change in the number of aberrations/cell, % aberrant cells, % of cells with greater than 1 aberration, or mitotic index was observed at any rimsulfuron concentration in the absence or presence of S9-mediated metabolic activation. /The/ positive controls, mitomycin C (-S9) increases the number of aberrations/cell over negative controls by 16.5-42-fold, the % abnormal cells by 10-32-fold, and the % of cells with greater than 1 aberration from 0 to 8-16%. Cyclophosphamide (+S9) generated increases in number of aberrations/cell of 8.7-26-fold, % of abnormal cells of 8-22-fold, and the % of cells with greater than 1 aberration from 0 to 2-8%. No effect on any type of aberration was detected /and/ both positive controls showed increases in various types of chromosomal aberrations (particularly chromatid gaps). Rimsulfuron does not elicit clastogenic changes under the conditions tested.
In rats, rimsulfuron is excreted within the first 72 hours following dosing in the urine (64%) and the feces (30%). Low, but detectable amounts of radioactivity were found in the heart, lung, liver, kidney, and muscle...
The metabolism of (14)C-labeled rimsulfuron was studied in male and female rats. The low dose groups were treated once by oral gavage with 25 mg/kg (14)C -pyridine-labeled compound and the high dose groups with 250 mg/kg of either (14)C -pyridine- or (14)C-pyrimidine-labeled compound. The repeat dose groups were gavaged orally with unlabeled test compound (25 mg/kg) for 14 consecutive days, followed on the 15th day by 25 mg/kg of (14)C -pyridine-test compound. Excretion accounted for 93 to 96% of the administered radioactivity, with 58 to 67% appearing in the urine and 20 to 33% in the feces. Tissue distribution of labeled residues was low. Males showed slightly higher hepatic accumulation than females within each test group. Animals in the repeat dose groups also showed a slight accumulation in the spleen. ...
[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.
