Metabolic pathway of butylate in rats proceeds as follows: thiocarbamate, thiocarbamate sulfoxide, S-(N,N-dialkylcarbamoyl)glutathione, D-(N,N-dialkylcarbamoyl)cysteine, S-(N,N-dialkylcarbamoyl)mercapturic acid, S-(N,N-dialkylcarbamoyl)mercaptoacetic acid, and N-(S-(N,N-dialkylcarbamoyl)mercaptoacetyl)glycine. S-(N-isobutylcarbamoyl)mercapturic acid is also formed. About 40% of the (14)CO-butylate administered is metabolized by ester cleavage and (14)CO2 liberation without going through the thiocarbamate sulfoxide as an intermediate.
When administered to rats, butylate yielded a glycine conjugate of the mercaptoacetic acid product that was not detected with EPTC; but the cysteine conjugate was not detected with butylate. An N-de-isobutylmercapturic acid was formed from butylate but the corresponding EPTC product was not seen.
来源:Hazardous Substances Data Bank (HSDB)
代谢
在哺乳动物中,口服给药后,主要代谢物是N,N-二烷基碳酰胺基共轭物。
In mammals, following oral administration, the major metabolite is the N,N-dialkylcarbamoyl conjugate.
The metabolism of the thiocarbamate herbicide SUTAN (butylate) was studied after administration of single oral doses of [isobutyl-1-(14)C]SUTAN to male and female rats. The radiolabelled dose was rapidly absorbed and excreted, with 79% of the dose excreted in the urine in 72 hr. The small percentages of radioactivity excreted in the feces and as (14)CO2 were significantly higher (P less than or equal to 0.05) in males than in females. SUTAN was extensively metabolized, and no unmetabolized SUTAN was found in the urine. A total of 18 of the 29 urinary metabolites were identified, and identified metabolites represented 83-88% of the urinary radioactivity. Diisobutylamine was the major urinary metabolite in both males and females, averaging 51% of the urinary radioactivity. Other significant urinary metabolites included primary hydroxylated and tertiary hydroxylated diisobutylamines and a series of mercapturic acid pathway metabolites, including an S-glucuronide and several hydroxylated and unhydroxylated mercapturates. Oxidations at the three alkyl groups produced a variety of minor urinary metabolites, and hydroxylation of the primary or tertiary carbon on the isobutyl groups, followed by an intramolecular reaction, generated a series of minor cyclized metabolites.
IDENTIFICATION AND USE: Butylate is a colorless liquid. It is a thiocarbamate compound used as a selective preplant incorporated herbicide. HUMAN STUDIES: Although limited, epidemiologic studies suggest possible associations between butylate use and cancer risk, specifically prostate cancer and non-Hodgkin lymphoma. ANIMAL STUDIES: Butylate was not carcinogenic in rats and dogs. Butylate was not teratogenic in rats and rabbits. Butylate was nonmutagenic in Salmonella typhimurium tester strains TA 1535, 1537, 1538, 98 and 100, with and without metabolic activation. ECOTOXICITY STUDIES: Not dangerous to bees when used as directed.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
癌症分类:E组 人类非致癌性证据
Cancer Classification: Group E Evidence of Non-carcinogenicity for 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
毒性数据
大鼠LC50 = 19,000毫克/立方米
LC50 (rat) = 19,000 mg/m3
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
Commercial and technical grades of 11 herbicides and 13 combinations of commercial grade herbicides were evaluated for their genotoxic properties with Salmonella typhimurium, Saccharomyces cerevisiae directly and following plant and animal activation, or with Zea mays. The herbicides were related by their use in commercial corn (maize) production. Commercial grade formulations of each herbicide and combination of herbicides were also evaluated in situ with the pollen waxy locus assay of Z. mays. Eradicane and bifenox were negative in all assays. Alachlor, propachlor, procyazine and SD50093 (a formulation of cyanazine plus atrazine) were positive in one assay. Cyanazine, dicamba and metolachlor were positive in 2 assays. Atrazine, simazine and butylate were tested only in situ. Atrazine and simazine were positive and butylate was negative. Of the combinations of herbicides evaluated with the 3 genetic assays, alachlor plus bifenox and procyazine plus metolachlor were positive in 1 assay and metolachlor plus atrazine was positive in 2 assays. Of the combinations of herbicides evaluated only in situ, butylate plus atrazine, eradicane plus atrazine, eradicane plus cyanazine and metolachlor plus cyanazine were positive while butylate plus cyanazine was negative.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
被根和胚芽鞘吸收,通过向顶运输。
Absorbed by the roots and coleoptiles, with translocation acropetally.
The metabolism of the thiocarbamate herbicide SUTAN (butylate) was studied after administration of single oral doses of [isobutyl-1-(14)C]SUTAN to male and female rats. The radiolabelled dose was rapidly absorbed and excreted, with 79% of the dose excreted in the urine in 72 hr. The small percentages of radioactivity excreted in the feces and as (14)CO2 were significantly higher (P less than or equal to 0.05) in males than in females. SUTAN was extensively metabolized, and no unmetabolized SUTAN was found in the urine. A total of 18 of the 29 urinary metabolites were identified, and identified metabolites represented 83-88% of the urinary radioactivity. Diisobutylamine was the major urinary metabolite in both males and females, averaging 51% of the urinary radioactivity. Other significant urinary metabolites included primary hydroxylated and tertiary hydroxylated diisobutylamines and a series of mercapturic acid pathway metabolites, including an S-glucuronide and several hydroxylated and unhydroxylated mercapturates. Oxidations at the three alkyl groups produced a variety of minor urinary metabolites, and hydroxylation of the primary or tertiary carbon on the isobutyl groups, followed by an intramolecular reaction, generated a series of minor cyclized metabolites.
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] 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.