... In feces intact (14)C-cymoxanil (< 1%) and IN W3595 was detected, but the majority of radioactivity was (14)C-glycine (about 9 - 13%). Based on the data, the metabolic pathway involves hydrolysis of cymoxanil to IN W3595, which is then degraded to glycine, which in turn is incorporated into natural constituents or further metabolized.
... IN-U3204 (1-ethyl-5,6-di-2,4(1H,3H) pyridinedione) was detected in pooled 0-48 hr urine samples, both sexes, from animals treated with 120 mg/kg DPX-3217 and in pooled 0-24 hr samples, both sexes, from animals treated with 2.5 mg/kg in an ongoing low dose biliary fistula study. The latter group was included to ensure that the presence of IN-U3204 was not an artifact of storage; IN-U3204 was detected in both groups, though at apparently low levels.
/2-(14)C-DPX-T3217/ was administered /to rats/ in corn oil to/ single dose groups: 2.5 & 120 mg/kg, 0.5 & 2 mL/animal (~10 & ~20 uCi/animal, groups D & E, respectively) and a multiple dose group: daily administration at 2.5 mg/kg for 14 days followed by labeled dose at 2.5 mg/kg (group F). /In a/ 5/sex/dose regimen, the primary metabolites detected by HPLC and TLC in excreta were IN-W3595 (2-cyano-2-methoxyimino acetic acid) and polar components (glycine and other amino acid conjugates); In group D males, 24 hr: 58% of /administered dose (AD)/ in urine (8.6% as IN-W3595, 46.5% as polars), 21.9% in feces (14% extractable, <1% IN-W3595, 13.1% polars). In /group D/ females, 64.2% of AD /appeared/ in urine (16.1% IN-W3595, 45.2% polars), 16.3% in feces (10.1% extractable, <1% IN-W3595, 8.7% polars). In group E males, 70.3% of AD /appeared/ in urine (26.3% IN-W3595, 40.3% polars), 16.1% in feces (11.3% extractable, <1% IN-W3595, 8.6% polars). /In group E/ females, 73% of AD in urine (33% IN-W3595, 36.7% polars), 17.1% in feces (11.5% extractable, <1% IN-W3595, 8.5% polars). In group F males, 66.2% of AD /appeared/ in urine (6.5% IN-W3595, 55% polars), 14.5% in feces (9% extractable, <1% IN-W3595, 8.9% polars). In group F females, 63.1% of AD /appeared/ in urine (11.1% IN-W3595, 46.6% polars), 19.4% in feces (12.3% extractable, <1% IN-W3595, 12.2% polars). /IN-W3595 metabolite/
Organic nitriles are converted into cyanide ions through the action of cytochrome P450 enzymes in the liver. Cyanide is rapidly absorbed and distributed throughout the body. Cyanide is mainly metabolized into thiocyanate by either rhodanese or 3-mercaptopyruvate sulfur transferase. Cyanide metabolites are excreted in the urine. (L96)
Organic nitriles decompose into cyanide ions both in vivo and in vitro. Consequently the primary mechanism of toxicity for organic nitriles is their production of toxic cyanide ions or hydrogen cyanide. Cyanide is an inhibitor of cytochrome c oxidase in the fourth complex of the electron transport chain (found in the membrane of the mitochondria of eukaryotic cells). It complexes with the ferric iron atom in this enzyme. The binding of cyanide to this cytochrome prevents transport of electrons from cytochrome c oxidase to oxygen. As a result, the electron transport chain is disrupted and the cell can no longer aerobically produce ATP for energy. Tissues that mainly depend on aerobic respiration, such as the central nervous system and the heart, are particularly affected. Cyanide is also known produce some of its toxic effects by binding to catalase, glutathione peroxidase, methemoglobin, hydroxocobalamin, phosphatase, tyrosinase, ascorbic acid oxidase, xanthine oxidase, succinic dehydrogenase, and Cu/Zn superoxide dismutase. Cyanide binds to the ferric ion of methemoglobin to form inactive cyanmethemoglobin. (L97)
来源:Toxin and Toxin Target Database (T3DB)
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).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
副作用
皮肤致敏剂 - 一种可以诱导皮肤产生过敏反应的制剂。
Skin Sensitizer - An agent that can induce an allergic reaction in the skin.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
毒性数据
LCLo(大鼠)= 4,980 毫克/立方米/4小时
LCLo (rat) = 4,980 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Cymoxanil is rapidly absorbed and maximum concentrations in the blood and plasma is reached within 4 hours after dosing. Rapid and almost complete elimination of the administered radioactive dose was observed in urine and feces within 48 hours. Excretion is primarily by urine (64 - 75%), fecal (16 - 24%) and expired air (< 5%) of the administered dose. There is no significant difference in residue profiles or elimination rates between sexes, dose levels, or single or multiple dosing. No evidence of bioaccumulation was detected. DPX-T3217 is metabolized extensively and only trace level of the administered (14)C-cymoxanil was detected in the urine and feces. ...
Five SD rats/sex with cannulated bile ducts were dosed orally with 2.5 mg/kg of (14)C-Cymoxanil (radiochemical purity = 98%; 14.09 uCi/mg) as a corn oil suspension. Urine, feces, and bile were collected over a 48 h period, after which the animals were terminated and whole blood, liver, kidneys, and residual carcass were collected for measurement of radiolabel. ...More than 85% of the test compound was eliminated in urine ( approximately 65%), feces (approximately 14%), and bile (approximately 7%) within 48 hr in both sexes, with most elimination occurring with the first 24 hr; polar amino acid conjugates comprised the major class of metabolites found in both urine (approximately 45-50%) and bile (approximately 4-6%); Metabolite A (unknown) and IN-W3595 /(2-cyano-2-methoxyimino acetic acid)/ were found at much lower concentrations (< 10%) in urine. IN-W3595 was found at higher concentrations in the urine of females (7.7%) as compared to males (2.8%); Metabolite A was not found in bile.
/To study the absorption, distribution, metabolism, and excretion of 2-(14)C-DPX-T3217 in rats, doses of/ 2.5 & 120 mg/kg in corn oil /at/ 0.5 & 2 mL/animal, /were administered. Radioactivity amounted to/ ~10 & ~20 uCi/animal, respectively. /High dose/ set by expectation of slight toxicity. /With/ single gavage administration: 3/sex/dose - blood pharmacokinetics, 5/sex/dose - elimination/distribution, 8/sex/dose - tissue distribution; multiple administration (cold dosing at 2.5 mg/kg for 14 days followed by labeled dose): 5/sex; no significant differences between groups in blood/plasma and tissue residue profiles. Max. blood concentrations were attained by 4 hr; with the possible exception of a somewhat decreased relative fecal excretion at the high dose (both sexes) and at the multiple low dose (males only). No significant differences in excretion time or route were seen when comparing sexes, doses, or single vs. multiple dosing regimens. Including all dose groups, 57-65% of the administered dose (AD) recovered in urine & 5-17% in feces by 24 hr, 63-75% in urine & 16-24% in feces by 96 hr; at 96 hr <1% of AD remained in tissues (highest levels found in kidney, liver, & skin).
(14)C-Cymoxanil was applied to either the root system or to the foliage of tomato plants and its uptake, translocation and degradation was followed using autoradiography, combustion and thin-layer chromatographic analyses of water or methanolic extracts. Cymoxanil was taken up by the root system within 1 hr and translocated to cotyledons, stem and leaves within 16 hr. The compound was degraded, mostly to glycine, within 16-44 h, in the root and all parts of the shoot. When applied to the surface of leaf 2 of five-leaf plants, enhanced uptake, translocation and degradation (mainly to glycine) of (14)C-cymoxanil was observed in plants treated with a mixture of oxadixyl and (14)C-cymoxanil, compared with plants treated with (14)C-cymoxanil alone. Root application data confirm that cymoxanil is a systemic compound with a short persistence in tomato plants. Foliage application data suggest that the well-documented synergistic interaction between cymoxanil, oxadixyl and mancozeb in controlling plant diseases caused by Peronosporales does not result from a delayed degradation of cymoxanil in the presence of the other fungicides; the mechanism of synergism has not yet been elucidated.
[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.