Thidiazuron (N-phenyl-N'-1,2,3-thiadiazol- 5-ylurea) cotton defoliant was administered for 10 consecutive days to lactating goats and laying hens. The vast majority of the radioactive material (> 70%) was eliminated in goat urine and feces; less than 1.5% of the administered radioactivity was in the milk. Hens excreted 72% of the total consumed radioactive material during the 10-day feeding period. In addition to the parent compound, which was present in low levels in goat milk and in chicken excreta, eggs, liver, and kidney, N-4-hydroxyphenyl- N'-1,2,3-thiol-5- ylurea or 4-hydroxyphenyl thidiazuron and phenylurea were detected. 4-Hydroxyphenyl thidiazuron was the major thidiazuron metabolite and was present in the free and/or conjugated form in goat and hen excreta, milk, eggs, and certain tissues. Phenylurea was detected only in goat urine. Other unidentified compounds also were present.
/In/ an oral metabolism study in rats ... identification of urinary metabolites indicated the presence of oxidative metabolite (4-hydroxy thidiazuron) in urine and the presence of sulfate and glucuronide conjugates of 4-hydroxy thidiazuron. In feces, the major metabolites identified were 4-hydroxy thidiazuron at the low dose and unmetabolized thidiazuron at the high dose.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
毒性总结
美国环保局没有发现任何信息表明噻二唑隆与其他物质有共同的毒性作用机制。
The US EPA has found no information indicating thidiazuron shares a common mechanism of toxicity with other substances. (L2080)
来源:Toxin and Toxin Target Database (T3DB)
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).
Relatively few incidents of illness have been reported due to thidiazuron. Since 1992, OPP IDS has only reported 5 incidents as a result of thidiazuron exposure, which all show similar symptoms such as skin rash, nausea, and weakness. However, no medical treatment was required. (L2080)
[(14)C-aniline] thidiazuron was fed at a dose exaggeration of 1.9x to a lactating cow at a rate of 10 ppm for seven days. The animal was sacrificed within 24 hours of administration of the final dose. Parent equivalent radioactivity found was 0.05 ppm, 0.1 ppm, 1.5 ppm, and 1.0 ppm in fat, muscle, kidney and liver, respectively. Radioactivity reached a plateau in milk on the second day (0.2 ppm). Analysis was performed using HPLC and TLC.
[(14)C-aniline] thidiazuron was fed once daily at a dose exaggeration of 100x to six hens for fourteen days at a rate of 8 ppm. Radioactivity did not plateau in eggs during this period. All tissues were first treated with protease and beta-glucuronidase prior to extraction. Parent equivalent radioactivity found was 0.02 ppm, 0.27 ppm, 1.11 ppm, 0.66 ppm, 0.10 ppm, 0.10 ppm and 0.34 ppm in fat, gastrointestinal tract, gastro-intestinal tract contents, liver, muscle, skin and blood, respectively.
In a metabolism study groups of male and female Sprague-Dawley CD rats were dosed with (14)C-thidiazuron [((14)C-aniline) thidiazuron or ((14)C-thiadizaole) thidiazuron (purity: >97% a.i.; batch No: 1695-3 and 1695-4)] at a single oral gavage dose (10 or 1000 mg/kg) or 14-day repeated oral doses of thidiazuron at 10 mg/kg followed by a single oral dose of (14)C-thidiazuron at 10 mg/kg ... The results of the pilot study showed that less than 0.2% of administered radioactivity was eliminated as (14)CO2 from administration of either ((14)C-aniline) thidiazuron or ((14)C-thiadizaole) thidiazuron. In addition, the study showed no significant differences in the percentages eliminated through urine or feces from administration of the two radiolabeled forms. Absorption of thidiazuron was rapid but incomplete at both doses, and appeared decreased at the high dose relative to the low dose. Elimination of thidiazuron was relatively rapid at the single low oral dose level. The major route of elimination was shown to be via urine. The single low, single high, and multiple low oral dose studies indicate that the total radioactivity recovered within 5 days after dosing in the urine and feces were 91-104% of administered dose. At the low dose, the radioactivity recovered in the urine and feces was 60-66% and 29-31% of the dose over a 5-day period, respectively. At the repeated low oral dose, the radioactivity recovered in the urine and feces was 73-75% and 26-28% of the dose over a 5-day period, respectively. At the high dose, the radioactivity recovered in the urine and feces was 41-47% and 56-60% of the dose over a 5-day period, respectively. Administration of a single high dose resulted in a decreased percentage of thidiazuron derived radioactivity eliminated in urine (approximately 20%), with concomitant rise in fecal elimination. This alteration is likely due to reduced absorption of test material at the high dose. Terminal tissue distribution data showed that highest concentrations of thidiazuron derived radioactivity at sacrifice were found in the liver, kidneys, thyroid, whole blood and adrenals at both low and high doses. Repeated oral dosing did not significantly affect distribution of thidiazuron derived radioactivity.
In a dermal penetration study Thidiazuron (99.9 %a.i., batch # OR 1844 (SEL/1098), [phenyl-U-(14)C]-thidiazuron) was administered to 5 male Sprague Dawley CD rats/dose to a 12 sq cm area of the back in a formulation and water dilution thereof at dose levels of 5.0, 0.04 and 0.004 mg/sq cm ... The mean total recoveries were in the range 88% and 99.54% dose for all groups. The amount in the stratum corneum was 0.73%, 10.68% and 8.14% at 24 hours for the high, middle and low dose groups respectively after a 24-hours exposure and 0.41%, 3.24% and 5.37% at 120 hours following 8-hours exposure for the high, middle and low dose groups respectively. However, the results showed that the majority of the radioactive material in the stratum corneum was lost by desquamation and upward renewal of the stratum corneum with time.
Thidiazuron (N-phenyl-N'-1,2,3-thiadiazol- 5-ylurea) cotton defoliant was administered for 10 consecutive days to lactating goats and laying hens. The vast majority of the radioactive material (> 70%) was eliminated in goat urine and feces; less than 1.5% of the administered radioactivity was in the milk. Hens excreted 72% of the total consumed radioactive material during the 10-day feeding period. In addition to the parent compound, which was present in low levels in goat milk and in chicken excreta, eggs, liver, and kidney, N-4-hydroxyphenyl- N'-1,2,3-thiol-5- ylurea or 4-hydroxyphenyl thidiazuron and phenylurea were detected. 4-Hydroxyphenyl thidiazuron was the major thidiazuron metabolite and was present in the free and/or conjugated form in goat and hen excreta, milk, eggs, and certain tissues. Phenylurea was detected only in goat urine. Other unidentified compounds also were present.
[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.
A tetrazolinone compound of formula (1):
wherein R
1
and R
2
each independently represents a hydrogen atom, etc.;
R
3
represents a C1-C6 alkyl group, etc.; R
4
, R
5
, and R
6
each independently represents a hydrogen atom, etc.; A represents a C6-C16 aryl group optionally having one or more atoms or groups selected from Group P, etc.; Q represents the following group Q1, etc.; and
X represents an oxygen atom or a sulfur atom, has excellent control activity against pests.
The present invention provides triazole compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
本发明提供了三唑化合物，可用作乙酰辅酶A羧化酶（ACC）的抑制剂，以及其组合物和使用方法。
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
申请人：Dow AgroSciences LLC
公开号：US20180279612A1
公开（公告）日：2018-10-04
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
