The metabolic fate of 4-bromoaniline (4-BrA) was investigated following intraperitoneal administration to the rat at 50 mg kg(-1), using high-performance liquid chromatography/time-of-flight tandem mass spectrometry (HPLC/TOF-MS/MS). Up to five metabolites were detected in urine that correspond to isomeric pentose conjugates (possibly ribosides) of a hydroxysulfate of 4-BrA. This identification is supported by further studies where the water used in the reversed-phase solvent system was replaced with deuterated water in order to confirm that the number of exchangeable protons present in the metabolites was consistent with the proposed structures.
The urinary excretion of 4-bromoaniline and its (carbonyl-(13)C)-labelled N-acetanilide, together with their corresponding metabolites, have been investigated in the rat following i.p. administration at 50 mg kg(-1). Metabolite profiling was performed by reversed-phase HPLC with UV detection, whilst identification was performed using a combination of enzymic hydrolysis and directly coupled HPLC-NMR-MS analysis. The urinary metabolite profile was quantitatively and qualitatively similar for both compounds with little of either excreted unchanged. The major metabolite present in urine was 2-amino-5-bromophenylsulphate, but, in addition, a number of metabolites with modification of the N-acetyl moiety were identified (from both the ((13)C)-acetanilide or produced following acetylation of the free bromoaniline). For 4-bromoacetanilide, N-deacetylation was a major route of metabolism, but despite the detection of the acetanilide following the administration of the free aniline, there was no evidence of reacetylation (futile deacetylation). Metabolites resulting from the oxidation of the acetyl group included a novel glucuronide of an N-glycolanilide, an unusual N-oxanilic acid and a novel N-acetyl cysteine conjugate.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
暴露途径
该物质可以通过吸入其气溶胶和通过吞食被吸收进人体。
The substance can be absorbed into the body by inhalation of its aerosol and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
毒理性
吸入症状
嘴唇、手指甲和皮肤发蓝。头痛。恶心。
Blue lips, fingernails and skin. Headache. Nausea.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
毒理性
摄入症状
蓝色嘴唇、手指甲和皮肤。眩晕。头痛。呼吸困难。恶心。混乱。抽搐。昏迷。
Blue lips, fingernails and skin. Dizziness. Headache. Laboured breathing. Nausea. Confusion. Convulsions. Unconsciousness.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
/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 as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on 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. /Aniline and related compounds/
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
Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
申请人:Vertex Pharmaceuticals Incorporated
公开号:US20150231142A1
公开(公告)日:2015-08-20
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
An enantioselective alkoxycarbonylation-amination cascade process of terminalallenes with CO, methanol, and arylamines has been developed. It proceeds under mild conditions (room temperature, ambient pressure CO) via oxidative Pd(II) catalysis using an aromatic spiroketal-based diphosphine (SKP) as a chiral ligand and a Cu(II) salt as an oxidant and affords a wide range of α-methylene-β-arylamino
Synthesis and Anticonvulsant Activity of<i>N</i>-(Substituted)-1-methyl-2,4-dioxo-1,2-dihydroquinazoline-3(4<i>H</i>)-carboxamides
作者:Hemavathi N. Deepakumari、Bidarur K. Jayanna、Maralekere K. Prashanth、Hosakere D. Revanasiddappa、Bantal Veeresh
DOI:10.1002/ardp.201600024
日期:2016.7
A series of new N‐(substituted)‐1‐methyl‐2,4‐dioxo‐1,2‐dihydroquinazoline‐3(4H)‐carboxamides were designed, synthesized, and evaluated for their anticonvulsantactivity. Most of the synthesized compounds exhibited potent anticonvulsantactivities in the maximal electroshock (MES) and pentylenetetrazol (PTZ) test. The most promising compound 4c showed significant anticonvulsantactivity with a protective
Synthesis, anti-HIV-1 and antiproliferative evaluation of novel 4-nitroimidazole derivatives combined with 5-hydroxy-4-pyridinone moiety
作者:Pouria Shirvani、Afshin Fassihi、Lotfollah Saghaie、Siska Van Belle、Zeger Debyser、Frauke Christ
DOI:10.1016/j.molstruc.2019.127344
日期:2020.2
derivatives combined with 5-hydroxy-4-pyridinone moiety were designed by molecular docking studies, prepared and characterized by spectroscopic techniques. All the synthesized compounds were in vitro evaluated for their inhibitory effect against the HIV-1 replication in the MT-4 cells. Results showed that none of these synthesized compounds displayed any specific anti HIV-1 activity. Surprisingly, these
[EN] PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS<br/>[FR] PYRROLOTRIAZINES EN TANT QU'INHIBITEURS D'ALK ET DE JAK2
申请人:CEPHALON INC
公开号:WO2010071885A1
公开(公告)日:2010-06-24
The present invention provides a compound of formula (I) or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula (I) has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.