In studies of metabolism in rats, ... cyprodinil was primarily metabolized by hydroxylation of the phenyl and pyrimidine rings and methyl group, and excreted mainly as glucuronide or sulfate conjugates in urine, feces and bile. Approximately 3-8% of the parent compound was detected in the feces. Excretion, distribution and metabolite profiles were essentially independent of dose, pretreatment and site of radiolabel, although there were some quantitative sex-dependent differences in urinary metabolites.
来源:Hazardous Substances Data Bank (HSDB)
代谢
代谢途径与性别、预处理或给药剂量水平无关。
The metabolic pathways are independent of sex, pre-treatment or dose level administered.
来源:Hazardous Substances Data Bank (HSDB)
代谢
在番茄中，CGA 219417的代谢主要通过嘧啶环6-甲基组的羟基化以及苯环和嘧啶环的羟基化进行。
In tomatoes, the metabolism of CGA 219417 proceeded mainly via hydroxylation of the 6-methyl group of the pyrimidine ring as well as hydroxylation of the phenyl & pyrimidine ring.
IDENTIFICATION AND USE: Cyprodinil is a fine beige powder. It is used as a foliar fungicide in cereals, grapes, pome fruits, stone fruits, strawberries, and vegetables and as a seed dressing on barley; it controls a wide range of pathogens, including Pseudocercosporella herpotrichoides, Erysiphe spp., Pyrenophora teres, Rhynchosporium secalis, and Septoria nodorum. HUMAN EXPOSURE AND TOXICITY: Cyprodinil acts as an aryl hydrocarbon receptor activator, a potential endocrine disrupter, and an extracellular signal-regulated kinase disrupter. Weak androgen receptor binding was shown for cyprodinil. Cyprodinil was genotoxic for HepG2 cells at concentrations 20 uM. ANIMAL STUDIES: In a 28 day gavage study in rats, the LOEL is 100 mg/kg bw/day for rats, based on increased liver weights and abnormalities in liver morphology. In a two-generation reproduction study in rats, the LOEL for maternal systemic toxicity is 4000 (about 326 mg/kg/day) based on lower body weights in the F0 females during the pre-mating period. The NOEL for maternal systemic toxicity is 1000 ppm (about 81 mg/kg/day). The LOEL for reproductive/developmental toxicity is 4000 ppm (about 326 mg/kg/day) based on decreased pup weights (F1 and F2). The NOEL for reproductive toxicity is 1000 ppm (about 81 mg/kg/day). In an 18-month carcinogenicity study in mice, the LOEL is 2000 ppm (males- 212.4 mg/kg/day) based on a dose-related increase in the incidence of focal and multifocal hyperplasia of the exocrine pancreas in males. The NOEL is 150 ppm (males- 16.1 mg/kg/day). This study was tested to adequate levels based on signs of toxicity in males at 2000 ppm and females at 5000 ppm. There was no indication of carcinogenic potential at any dose level. ECOTOXICITY STUDIES: In plants, cyprodinil promoted a copious increase in exudate secretion and caused the most severe collapse of stigmatic cells of all the fungicides evaluated.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类：不太可能对人类致癌
Cancer Classification: Not 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
毒理性
毒性数据
LC50 (大鼠) > 1,200 mg/m³/4小时
LC50 (rat) > 1,200 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
... In rats, radiolabelled cyprodinil administered by gavage as a single dose of 0.5 or 100 mg/kg bw, or as repeated doses of 0.5 mg/kg bw per day for 14 days, was rapidly absorbed from the gastrointestinal tract and excreted. Approximately 75% (range, 71-85%) of an orally administered dose was absorbed over 48 hr. At a dose of 0.5 and 100 mg/kg bw, two plasma level maxima of radioactivity were observed at approximately 0.5-1 hr and 8-12 hr, probably caused by reabsorption of material excreted in the bile. Approximately 92-97% of the administered dose was eliminated within 48 hr in the urine (48-68%), feces (29-47%), and bile (accounting for up to 35.4% of the dose in cannulated rats), with elimination being almost complete by day 7. Seven days after single or repeated oral administration at the lower dose, total tissue residues accounted for 0.15-0.60% of the administered dose. ... Excretion, distribution and metabolite profiles were essentially independent of dose, pretreatment and site of radiolabel, although there were some quantitative sex-dependent differences in urinary metabolites.
After oral administration, CGA 219417 is rapidly absorbed and also rapidly and almost completely eliminated with urine and feces. ... Residues in tissues were generally low and there was no evidence for accumulation or retention of radioactivity.
Microbial Transformations of the Fungicide Cyprodinil (CGA-219417)
摘要：
A collection of 12 microbial cultures, known to contain cytochrome P-450 monooxygenase or other degradative enzymes, was screened for their ability to degrade the Novartis Crop Protection Inc. developmental fungicide cyprodinil (CGA-219417; 4-cyclopropyl-6-methyl-N-phenyl-2-pyrimidinamine). Ten of the 12 cultures produced a monohydroxylated metabolite in yields ranging from 1.2 to 35.6%. The filamentous fungus, Beauveria bassiana ATCC 7159, produced a methoxylated glycoside of the monohydroxylated metabolite with a yield of 80%. Dihydroxylated metabolites and a molecular cleavage product, 4-cyclopropyl-6-methyl-2-pyrimidamine, were also detected in certain cultures. The overall results of the study indicated that cyprodinil was readily metabolized by a variety of microbial species. Metabolites generated by these cultures can potentially be used as analytical reference standards to support animal, plant, and soil metabolism studies.
[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] BICYCLYL-SUBSTITUTED ISOTHIAZOLINE COMPOUNDS<br/>[FR] COMPOSÉS ISOTHIAZOLINE SUBSTITUÉS PAR UN BICYCLYLE
申请人：BASF SE
公开号：WO2014206910A1
公开（公告）日：2014-12-31
The present invention relates to bicyclyl-substituted isothiazoline compounds of formula (I) wherein the variables are as defined in the claims and description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
The present invention relates to azoline compounds of formula (I) wherein A, B1, B2, B3, G1, G2, X1, R1, R3a, R3b, Rg1 and Rg2 are as defined in the claims and the description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
[EN] SUBSTITUTED QUINAZOLINES AS FUNGICIDES<br/>[FR] QUINAZOLINES SUBSTITUÉES, UTILISÉES EN TANT QUE FONGICIDES
申请人：SYNGENTA PARTICIPATIONS AG
公开号：WO2010136475A1
公开（公告）日：2010-12-02
The present invention relates to a compound of formula (I) wherein wherein the substituents have the definitions as defined in claim 1or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
