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Androgen-independent induction of prostate-specific antigen gene expression via cross-talk between the androgen receptor and protein kinase A signal transduction pathways. (1/748)
Transcription of the prostate-specific antigen (PSA) gene escapes regulation by androgens in advanced prostate cancer. To determine the molecular mechanism(s) of androgen-independent regulation of the PSA gene, the possibility that the androgen receptor (AR) is activated in the absence of androgen by stimulation of protein kinase A (PKA) was investigated. Activation of PKA by forskolin resulted in elevated expression of the PSA gene in androgen-depleted LNCaP cells, an effect that was blocked by the antiandrogen, bicalutamide. Further evidence that induction of PSA gene expression was dependent on AR was obtained from experiments using PC3 cells devoid of AR. Neither PSA, PB, nor ARR3 androgen-responsive reporters could be induced by activation of PKA in the absence of transfected AR. In addition, when nuclear AR from forskolin-treated LNCaP cells was incubated with oligonucleotides encoding an androgen response element of the PSA promoter and examined by electromobility shift assay, an increase in AR-androgen response element complex formation was observed. Lastly, cotransfection of an expression vector for a chimeric protein encoding the amino-terminal domain of the human AR linked to Gal4 and a 5xGal4UAS reporter gene construct resulted in activation of the amino-terminal domain of the AR by stimulation of PKA activity. These results demonstrate androgen-independent induction of PSA gene expression in prostate cancer cells by an AR-dependent pathway. (+info)Effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and secretions of apolipoprotein B-containing lipoprotein and bile acids in HepG2. (2/748)
We studied the effect of NTE-122 (trans-1,4-bis[[1-cyclohexyl-3-(4-dimethylamino phenyl) ureido]methyl]cyclohexane), a novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, on intracellular cholesterol esterification and the secretion of apolipoprotein B100 (apoB)-containing lipoprotein and bile acids in the human hepatoma cell line HepG2. NTE-122 markably inhibited [3H]oleate incorporation into cholesteryl esters in HepG2 cells incubated with 5 microg/ml 25-hydroxycholesterol as a stimulus for ACAT (IC50=6.0 nM). On the other hand, NTE-122 did not affect [3H]oleate incorporation into triglycerides and phospholipids and [14C]acetate incorporation into cholesterol. The stimulation of ACAT by 25-hydroxycholesterol caused significant increases in the secretion of radiolabeled cholesteryl esters, radiolabeled triglycerides and apoB mass. NTE-122 pronouncedly inhibited the secretion of radiolabeled cholesteryl esters in proportion to the inhibition of cellular cholesterol esterification, and it significantly reduced the secretion of radiolabeled triglycerides and apoB mass in HepG2 cells incubated with 25-hydroxycholesterol. Furthermore, NTE-122 increased the secretion of bile acids synthesized from [14C]-cholesterol. These results suggest that NTE-122 is capable of exhibiting anti-hyperlipidemic effects by reducing both the cholesterol content and the amount of secreted very low-density lipoprotein and enhancing the excretion of bile acid from the liver. (+info)Metabolism of aminoacyl-p-nitroanilides by rat mammary tissue. (3/748)
We have examined the metabolism of aminoacyl-p-nitroanilides by rat mammary tissue isolated from rats during late pregnancy, peak lactation and late lactation. The rate of hydrolysis depended upon the chemical nature of the aminoacyl-p-nitroanilide compound and the physiological state of the donor animals. Thus, mammary tissue isolated from rats during late pregnancy and peak lactation hydrolysed aminoacyl-p-nitroanilides in the order L-met-p-nitroanilide=L-leu-p-nitroanilide>L-lys-p-nitroanilide>gamma- glu-p-nitroanilide. The order of activity was the same for mammary tissue taken from rats during late lactation except that L-lys-p-nitroanilide was hydrolysed at the same rate as the neutral aminoacyl-p-nitroanilides. Mammary tissue from peak lactating rats also hydrolysed alpha-L-glu-p-nitroanilide and alpha-L-asp-p-nitroanilide but to a lesser extent than the other compounds tested. The anionic aminoacyl-p-nitroanilides were able to trans-stimulate D-aspartate efflux from mammary tissue explants and the perfused mammary gland via the high-affinity anionic amino acid carrier. The clearance of gly-L-phe by the perfused mammary gland was markedly inhibited by L-phe. The results suggest that mammary tissue expresses a variety of dipeptidases at the basolateral aspect of the mammary epithelium which are capable of hydrolysing peptides extracellularly. These enzymes may be important for providing amino acids for milk protein synthesis and/or inactivating signal peptides. (+info)Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. (4/748)
The role of androgen receptor (AR) mutations in androgen-independent prostate cancer (PCa) was determined by examining AR transcripts and genes from a large series of bone marrow metastases. Mutations were found in 5 of 16 patients who received combined androgen blockade with the AR antagonist flutamide, and these mutant ARs were strongly stimulated by flutamide. In contrast, the single mutant AR found among 17 patients treated with androgen ablation monotherapy was not flutamide stimulated. Patients with flutamide-stimulated AR mutations responded to subsequent treatment with bicalutamide, an AR antagonist that blocks the mutant ARs. These findings demonstrate that AR mutations occur in response to strong selective pressure from flutamide treatment. (+info)Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system. (5/748)
Advanced prostate cancer is treated by androgen ablation and/or androgen receptor (AR) antagonists. In order to investigate the mechanisms relevant to the development of therapy-resistant tumours, we established a new tumour model which closely resembles the situation in patients who receive androgen ablation therapy. Androgen-sensitive LNCaP cells were kept in androgen-depleted medium for 87 passages. The new LNCaP cell subline established in this manner, LNCaP-abl, displayed a hypersensitive biphasic proliferative response to androgen until passage 75. Maximal proliferation of LNCaP-abl cells was achieved at 0.001 nM of the synthetic androgen methyltrienolone (R1881), whereas 0.01 nM of this compound induced the same effect in parental cells. At later passages (> 75), androgen exerted an inhibitory effect on growth of LNCaP-abl cells. The non-steroidal anti-androgen bicalutamide stimulated proliferation of LNCaP-abl cells. AR protein expression in LNCaP-abl cells increased approximately fourfold. The basal AR transcriptional activity was 30-fold higher in LNCaP-abl than in LNCaP cells. R1881 stimulated reporter gene activity in LNCaP-abl cells even at 0.01 nM, whereas 0.1 nM of R1881 was needed for induction of the same level of reporter gene activity in LNCaP cells. Bicalutamide that acts as a pure antagonist in parental LNCaP cells showed agonistic effects on AR transactivation activity in LNCaP-abl cells and was not able to block the effects of androgen in these cells. The non-steroidal AR blocker hydroxyflutamide exerted stimulatory effects on AR activity in both LNCaP and LNCaP-abl cells; however, the induction of reporter gene activity by hydroxyflutamide was 2.4- to 4-fold higher in the LNCaP-abl subline. The changes in AR activity were associated neither with a new alteration in AR cDNA sequence nor with amplification of the AR gene. Growth of LNCaP-abl xenografts in nude mice was stimulated by bicalutamide and repressed by testosterone. In conclusion, our results show for the first time that the nonsteroidal anti-androgen bicalutamide acquires agonistic properties during long-term androgen ablation. These findings may have repercussions on the natural course of prostate cancer with androgen deprivation and on strategies of therapeutic intervention. (+info)Investigation of the quantitative metabolic fate and urinary excretion of 3-methyl-4-trifluoromethylaniline and 3-methyl-4-trifluoromethylacetanilide in the rat. (6/748)
The urinary metabolites of 3-methyl-4-trifluoromethylaniline in the rat were characterized and quantified using a combination of (19)F NMR, HPLC-NMR ((1)H and (19)F), and HPLC-mass spectrometry techniques. The major routes of metabolism were amine N-acetylation and methyl group C-oxidation to the benzyl alcohol (with subsequent glucuronide conjugation) and further to the corresponding benzoic acid derivative. Quantitatively only a small proportion of the urinary metabolites contained the free amino group, and these were products of ortho-hydroxylation (2 and 6 position) with additional conjugation to form the ether sulfates and glucuronides. An N-glucuronide of the parent compound was also identified. 3-Methyl-4-trifluoromethylacetanilide ((13)C-labeled in the acetyl group) gave virtually the same overall metabolite profile as 3-methyl-4-trifluoromethylaniline; however, a significant level of futile N-deacetylation and reacetylation occurred as ca. 50% of the excreted N-acetylated major metabolites contained no (13)C-label at the acetyl, having been replaced by an endogenous (12)C-acetyl source. This level of futile deacetylation is the highest yet reported for a substituted aniline/acetanilide and indicates a high degree of electronic activation of the amino group toward the acetyltransferase enzymes in vivo. (+info)Bicalutamide monotherapy versus flutamide plus goserelin in prostate cancer patients: results of an Italian Prostate Cancer Project study. (7/748)
PURPOSE: To compare the efficacy of bicalutamide monotherapy to maximal androgen blockade (MAB) in the treatment of advanced prostatic cancer. PATIENTS AND METHODS: Previously untreated patients with histologically proven stage C or D disease (American Urological Association Staging System) were randomly allocated to receive either bicalutamide or MAB. After disease progression, patients treated with bicalutamide were assigned to castration. The primary end point for this trial was overall survival. Secondary end points included response to treatment, disease progression, treatment safety, quality-of-life (QOL), and sexual function. RESULTS: A total of 108 patients received bicalutamide and 112 received MAB. There was no difference in the percentage of patients whose prostate-specific antigen returned to normal levels. At the time of the present analysis (median follow-up time, 38 months; range, 1 to 60 months), 129 patients progressed and 89 died. There was no difference in the duration of either progression-free survival or overall survival. However, a survival trend favored bicalutamide in stage C disease but MAB in stage D disease. Overall and subgroup trends were confirmed by multivariate analysis. Serious adverse events and treatment discontinuations were more common in patients receiving MAB (P =.08 and P =.04, respectively). Fewer patients in the bicalutamide group complained of loss of libido (P =. 01) and of erectile dysfunction (P =.002). Significant trends favored bicalutamide-treated patients also with respect to their QOL, namely relative to social functioning, vitality, emotional well-being, and physical capacity. CONCLUSION: Bicalutamide monotherapy yielded comparable results relative to standard treatment with MAB, induced fewer side effects, and produced a better QOL. (+info)Stimulation of bradykinin B(1) receptors induces vasodilation in conductance and resistance coronary vessels in conscious dogs: comparison with B(2) receptor stimulation. (8/748)
BACKGROUND: Constitutive bradykinin B(1) receptors have been identified in dogs; however, their physiological implications involving the coronary circulation remain to be determined. This study examined, in conscious dogs, the coronary response to des-Arg(9)-bradykinin (a B(1) receptor agonist) and the mechanisms involved. METHODS AND RESULTS: Eleven dogs were instrumented with a left ventricular micromanometer, a circumflex coronary catheter, a cuff occluder, a Doppler flow probe, and ultrasonic crystals to measure coronary blood flow velocity (CBFv) and coronary diameter (CD). Intracoronary des-Arg(9)-bradykinin (3 to 100 ng/kg) and bradykinin (0.1 to 10 ng/kg) did not modify systemic hemodynamics but dose-dependently increased CBFv and CD. Des-Arg(9)-bradykinin was less potent than bradykinin. Hoe 140 (a B(2) antagonist, 10 microg/kg) abolished the effects of bradykinin but did not influence the effects of des-Arg(9)-bradykinin. When CBFv increase was prevented by the cuff occluder, CD responses to bradykinin and des-Arg(9)-bradykinin were maintained. Intracoronary lisinopril (0. 75 mg) increased the CD response to bradykinin, with only minimal effect on CBFv, and extended the duration of the effect. Lisinopril did not alter des-Arg(9)-bradykinin responses. Intracoronary N(omega)-nitro-L-arginine (2 mg/kg) decreased the CD effect of bradykinin and prevented the CBFv and CD effects of des-Arg(9)-bradykinin. The relaxing effect of des-Arg(9)-bradykinin on isolated coronary rings was prevented by des-Arg(9), [Leu(8)]-bradykinin. CONCLUSIONS: In the conscious dog, B(1) receptors are present in coronary vessels, and their stimulation produces vasodilation in conductance and resistance vessels, which is mediated essentially by NO but not modulated by angiotensin-converting enzyme. However, the coronary vasodilation induced by B(1) receptor stimulation is not as great as that produced by B(2) receptor stimulation. (+info)
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Tocainide
1. Primary alpha-amino anilides". Journal of Medicinal Chemistry. 22 (10): 1171-6. doi:10.1021/jm00196a005. PMID 513064. Burton ...
Hydrocodone/paracetamol
Anilide analgesic. Clinical data. Trade names. Lorcet, Norco, Vicodin, others. Synonyms. Hydrocodone/acetaminophen, hydrocodone ...
Oxycarboxin
It is an anilide. Oxycarboxin is used to control rust diseases (e.g. soybean rust). Oxycarboxin has been commercially available ...
Aniline
Main article: Anilide. Aniline reacts with acyl chlorides such as acetyl chloride to give amides. The amides formed from ... At high temperatures aniline and carboxylic acids react to give the anilides.[17] ... aniline are sometimes called anilides, for example CH3-CO-NH-C6H5 is acetanilide. ...
Toxic oil syndrome
None of the in vivo or in vitro studies performed with toxic-oil-specific components, such as fatty acid anilides, and esters ... Similar results were obtained after administration of fatty acid anilides. Data discrepancies combined with both a high level ...
LiMAx test
Analgesic potency and acute toxicity of substituted anilides and benzamides. Toxicology and Applied Pharmacology 1971;19(1):20- ...
2,5-Furandicarboxylic acid
Screening studies on FDCA-derived anilides showed their important anti-bacterial action. The diacid itself is a strong ...
Bicalutamide
It is a bicyclic compound (has two rings) and can be classified as and has variously been referred to as an anilide (N- ... First-generation NSAAs including bicalutamide, flutamide, and nilutamide are all synthetic, nonsteroidal anilide derivatives ... C]linically relevant antiandrogens currently are nonsteroidal anilide derivatives. Antiandrogens used for prostate cancer ...
Naphthol AS
It is the anilide of 3-hydroxy-2-carboxynaphthalene. Many analogous compounds are known, designated with a differing suffix. ...
Aza-Cope rearrangement
Primary amines, aromatic amines, or lithium anilides can also be used as nucleophiles. Protective O-methylation often follows ...
Salicylanilide
It is classified as both a salicylamide and an anilide. Derivatives of salicylanilide have a variety of pharmacological uses. ...
Portmanteau inhibitor
"Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5". Bioorganic & Medicinal ...
Discovery and development of antiandrogens
... share an anilide ring structure. The structures can be seen in figure 7, where the anilide ring is coloured red. These three ... Replacing the anilide with an alkene gives weakly active compounds, which can be attributed to the lack of intramolecular ...
PMDTA
The effect of PMDTA on lithium anilide is illustrative of PMDTA's complexing power. The complex, [{PhN(H)Li}3·2PMDTA], is ... ISBN 978-3-527-29390-2. Barr, D.; Clegg, W.; Cowton, L.; Horsburgh, L.; Mackenzie, F. M.; Mulvey, R. (1995). "Lithium Anilide ...
Meta-selective C-H functionalization
In 2009, Gaunt's group reported a copper catalyzed meta-selective C-H arylation reaction on anilide derivatives. Despite the ... It is compatible with a spectrum of substituted anilide as well as different bisaryliodonium salts. However, the meta- ... selectivity is lost when highly ortho/para-directing methoxy group substitutes one of the meta-hydrogen of the anilide, which ... the arylation occurs exclusively on the meta position on a variety of anilide substrates. Remarkably, the regioselectivity is ...
Phenampromide
US 3016382, "N-substituted anilides and method of preparing the same" Lenz GR, Evans SM, Walters DE, Hopfinger AJ (1986). ...
Arsanilic acid
... as arsenic acid anilide. Also biologist, physician, and pharmacist, Béchamp reported it 40 to 50 times less toxic as a drug ... "de l'action de la chaleur sur l'arseniate d'analine et de la formation d'un anilide de l'acide arsenique". Compt. Rend. 56: ...
Bechamp reaction
M. A. Bechamp (1863). "de l'action de la chaleur sur l'arseniate d'analine et de la formation d'un anilide de l'acide arsenique ...
Zaleplon
The anilide nitrogen is then alkylated by means of sodium hydride and ethyl iodide to give 3. The first step in the ...
AA560
It is an anilide derivative and analogue of the NSAA flutamide, and shows greater in vivo antiandrogenic potency than does ...
3-Hydroxy-2-naphthoic acid
... is a precursor to many anilides, such as Naphthol AS, which are reactive toward diazonium salts to ...
Acetanilide
ISBN 978-0-85404-182-4. N-Phenyl derivatives of primary amides are called 'anilides' and may be named using the term 'anilide' ...
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Subsequently, the rate of chemical change was studied in the case of the formation of amides and anilides by the action of ...
Vorinostat
... (rINN) also known as suberanilohydroxamic acid (suberoyl+anilide+hydroxamic acid abbreviated as SAHA) is a member of ...
Naphthol Red
... anilide ("Naphtol AS-PH" dye precursor). In the solid state the hydrazo tautomer forms and several crystal structures exist. In ...
Avizafone
2-benzoyl-4-chloro-N-methyl-N-lysylglycin anilide), as adjunct antidotes in the treatment of organophosphorus intoxication in ...
Conrad-Limpach synthesis
... leading to the thermodynamically preferred β-keto acid anilide product (albeit in less than ideal yields). Continuation of this ...
Aryl-acylamidase
In enzymology, an aryl-acylamidase (EC 3.5.1.13) is an enzyme that catalyzes the chemical reaction an anilide + H2O ⇌ {\ ... displaystyle \rightleftharpoons } a carboxylate + aniline Thus, the two substrates of this enzyme are anilide and H2O, whereas ...
List of fungicides
... acid fungicides acypetacs aldimorph aliphatic nitrogen fungicides allyl alcohol amide fungicides ampropylfos anilazine anilide ...
Anilide - Wikipedia
Anilides (or phenylamides) are a class of chemical compounds which are acyl derivatives of aniline. Aniline reacts with acyl ... Media related to Anilides at Wikimedia Commons v t e. ... aniline and carboxylic acids react to give anilides. Herbicides ... "Anilide herbicides". Pesticide Target Interaction Database. East China University of Science & Technology. Archived from the ... chlorides or carboxylic anhydrides to give anilides. For example, reaction of aniline with acetyl chloride provides acetanilide ...
pMe-anilide anion
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
Browsing Technical documents by Subject "Anilides"
Ferrocene-based anilides: synthesis, structural characterization and inhibition of butyrylcholinesterase - Dalton Transactions ...
Twenty-three compounds in two series of ferrocene-based anilides, with the general formula C5H5-Fe-C5H4-C6H4-NH-CO-C6H4-R ( ... Twenty-three compounds in two series of ferrocene-based anilides, with the general formula C5H5-Fe-C5H4-C6H4-NH-CO-C6H4-R ( ... Ferrocene-based anilides: synthesis, structural characterization and inhibition of butyrylcholinesterase A. A. Altaf, M. ...
Medical Subject Headings - Anilides - Classes | NCBO BioPortal
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Poly (N-Alkyl-O-Nitro Anilides)
Hydractinia echinata test system. II. SAR toxicity study of some anilide derivatives of Naphthol-AS type
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The changing structural chemistry of lithium anilide on solvation by pyridine, 4-methylpyridine or 4-tert-butylpyridine -...
A family of crystalline lithium anilide solvates, [{PhN(H)Li .(pyr)(2)}(2)] 1, [{PhN(H)Li .(4-Me-pyr)(2)}(2)] 2 and [{PhN(H)Li ... The changing structural chemistry of lithium anilide on solvation by pyridine, 4-methylpyridine or 4-tert-butylpyridine ... The changing structural chemistry of lithium anilide on solvation by pyridine, 4-methylpyridine or 4-tert-butylpyridine. ...
Binding of Anilide-type Local Anesthetics in Human Plasma:I. Relationships between Binding, Physicochemical Properties, and...
Binding of Anilide-type Local Anesthetics in Human Plasma: I. Relationships between Binding, Physicochemical Properties, and ... Binding of Anilide-type Local Anesthetics in Human Plasma: I. Relationships between Binding, Physicochemical Properties, and ... Binding of Anilide-type Local Anesthetics in Human Plasma: I. Relationships between Binding, Physicochemical Properties, and ... Geoffrey T. Tucker, Robert N. Boyes, Phillip O. Bridenbaugh, Daniel C. Moore; Binding of Anilide-type Local Anesthetics in ...
β</em>-Oxo Anilides in Heterocyclic Synthesis: Novel Synthesis of Substituted Pyridazinones, Pyridine, Pyrimidines and...
The reaction of anilide 4 with aromatic aldehydes yielded 10a,b. Also, when anilide 4 was reacted with a mixture of aromatic ... Hussein, A. H. M. , El-Gaby, M. S. A. A. , El-Maged, A. A. H. A. , El-Sharief, A. M. and Ammar, Y. A. (2015). β-Oxo Anilides in ... Similarly, anilide 1 was reacted with cyanoacetamide under the same reaction conditions to yield 4-methyl-2-oxo-6-p-tolylamino- ... Microwave-Assisted Synthesis of New Substituted Anilides of Quinaldic Acid. A QUICK VIEW ON METHODS OF SYNTHESIS OF PYRIMIDINES ...
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ATP gamma-anilide. Known as: Adenosine 5-(trihydrogen diphosphate), monoanhydride with phenylphosphoramidic acid, adenosine ... Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) ... Slow hydrogen atom self-exchange between Os(IV) anilide and Os(III) aniline complexes: relationships with electron and proton ... The interaction of heparin with human alpha-thrombin: effect on the hydrolysis of anilide tripeptide substrates. ...
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The absolute antipodal activity of analgesics in the basic anilide series<...
Portoghese, P. S. (1962). The absolute antipodal activity of analgesics in the basic anilide series. Journal of Pharmaceutical ... Portoghese, Philip S. / The absolute antipodal activity of analgesics in the basic anilide series. In: Journal of ... Portoghese, PS 1962, The absolute antipodal activity of analgesics in the basic anilide series, Journal of Pharmaceutical ... The absolute antipodal activity of analgesics in the basic anilide series. Journal of Pharmaceutical Sciences. 1962 Dec;51(12): ...
Esposizione ambientale e professionale a pesticidi propionanilidici e dicarbossimidici<...
Fingerprint Dive into the research topics of Occupational and environmental exposure to anilide and dicarboximide pesticides ... and anilide herbicides (AH) such as diuron, linuron, propanil are used to control weeds on hard surfaces, such as, roads, ... and anilide herbicides (AH) such as diuron, linuron, propanil are used to control weeds on hard surfaces, such as, roads, ... and anilide herbicides (AH) such as diuron, linuron, propanil are used to control weeds on hard surfaces, such as, roads, ...
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Toxic response of linoleic acid anilide in female rats
- UTMB Health Research Expert Profiles
title = "Toxic response of linoleic acid anilide in female rats",. abstract = "The toxicity of linoleic acid anilide (LAA) and ... The toxicity of linoleic acid anilide (LAA) and heated linoleic acid anilide (HLAA) was studied in female rats. Female Sprague- ... N2 - The toxicity of linoleic acid anilide (LAA) and heated linoleic acid anilide (HLAA) was studied in female rats. Female ... AB - The toxicity of linoleic acid anilide (LAA) and heated linoleic acid anilide (HLAA) was studied in female rats. Female ...
Countercation effect on CO<sub>2</sub> binding to oxo titanate with bulky anilide...
Countercation effect on CO2 binding to oxo titanate with bulky anilide ligands. Albert Paparo, Jared S. Silvia, Thomas P. ... Countercation effect on CO2 binding to oxo titanate with bulky anilide ligands. / Paparo, Albert; Silvia, Jared S.; Spaniol, ... Countercation effect on CO2 binding to oxo titanate with bulky anilide ligands. Chemistry - A European Journal. 2018 Nov 16;24( ... This work focuses on nucleophilic activation of CO2 at the anionic terminal oxo titanium tris(anilide) complexes [(Solv)nM][OTi ...
Patent US8156718 - Method of preparing a packaged antimicrobial medical device - Google Patents
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Cinnamic Anilides as New Mitochondrial
Permeability
Transition Pore Inhibitors Endowed with Ischemia-Reperfusion Injury...
Cinnamic Anilides as New Mitochondrial Permeability Transition Pore Inhibitors Endowed with Ischemia-Reperfusion Injury ... cinnamic anilides attenuate opening novel class compound Cinnamic Anilides cinnamic anilide mPTP inhibitors mPTP opening ... In this account, we report the development of a series of substituted cinnamic anilides that represents a novel class of ... The activity of the cinnamic anilide mPTP inhibitors turned out to be additive with that of CsA, suggesting for these ...
Derivatives5
- Anilides (or phenylamides) are a class of chemical compounds which are acyl derivatives of aniline. (wikipedia.org)
- Highly enantioselective synthesis of atropisomeric anilide derivatives through catalytic asymmetric N-arylation: conformational analysis and application to asymmetric enolate chemistry. (semanticscholar.org)
- Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. (semanticscholar.org)
- Substitution in the anilide ring affords a series of Naphthol AS derivatives although only a limited number is commercially recognized [ 3 , 4 ]. (hindawi.com)
- Charge transfer complexes of some anilides with nitrobenzene derivatives as pi-electron acceptors. (biomedsearch.com)
Aniline4
- Aniline reacts with acyl chlorides or carboxylic anhydrides to give anilides. (wikipedia.org)
- At high temperatures, aniline and carboxylic acids react to give anilides. (wikipedia.org)
- Slow hydrogen atom self-exchange between Os(IV) anilide and Os(III) aniline complexes: relationships with electron and proton transfer self-exchange. (semanticscholar.org)
- Preparation of 3-Alkylated Oxindoles from N-Benzyl Aniline via a Cu(II)-Mediated Anilide Cyclization Process. (york.ac.uk)
Pharmacology1
- Khan, MF , Kaphalia, BS & Ansari, GAS 1992, ' Toxic response of linoleic acid anilide in female rats ', Research Communications in Chemical Pathology and Pharmacology , vol. 77, no. 2, pp. 241-244. (utmb.edu)
Analgesics1
- Portoghese, PS 1962, ' The absolute antipodal activity of analgesics in the basic anilide series ', Journal of Pharmaceutical Sciences , vol. 51, no. 12, pp. 1197-1198. (umn.edu)
Herbicides1
- The use of N,N-diallyl-2-chloroacetamide (German Printed Application DAS 1,014,380) and O-(isopropylaminosulfonyl)-glycolic acid-N-butyn-1-yl anilide (German Laid-Open Application DOS 2,201,432) as selective herbicides in various crops is known. (freepatentsonline.com)
Alkylation2
Aromatic4
- The reaction of anilide 4 with aromatic aldehydes yielded 10a,b. (oalib.com)
- Also, when anilide 4 was reacted with a mixture of aromatic aldehydes, urea or thiourea afforded the pyrimidines 11a,b. (oalib.com)
- This compound belongs to the class of organic compounds known as aromatic anilides. (drugbank.ca)
- These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. (drugbank.ca)
COMPOUND1
- The reference compound of Naphthols AS is the anilide of 2-hydroxy-3-naphthoic acid. (hindawi.com)
Toxicity3
- In this paper, a toxicity study for a series of anilides of Naphthol-AS type is presented. (ad-astra.ro)
- The toxicity of linoleic acid anilide (LAA) and heated linoleic acid anilide (HLAA) was studied in female rats. (utmb.edu)
- These results further support that hemopoietic system is an early target of fatty acid anilide toxicity. (utmb.edu)
Compounds1
- Twenty-three compounds in two series of ferrocene-based anilides, with the general formula C 5 H 5 -Fe-C 5 H 4 -C 6 H 4 -NH-CO-C 6 H 4 -R (where R = H, F, Cl, CH 3 and OCH 3 ), have been successfully synthesized. (rsc.org)
Acid1
- In the organic phase the azo-coupling reaction between 4-nitrobenzenediazonium chloride and 3-hydroxy-2-carboxylic acid 2-methyl-anilide (Naphthol AS-D) takes place as coupling component. (hindawi.com)
Pyridine1
- Similarly, anilide 1 was reacted with cyanoacetamide under the same reaction conditions to yield 4-methyl-2-oxo-6-p-tolylamino-1,2-dihydro-pyridine-3-carbonitrile 13 in quantitative yield. (oalib.com)
Reaction2
- The reaction of anilide 1 with active methylene reagents was also investigated. (oalib.com)
- Iodine mediated Diels-Alder reaction of the axially chiral N-acryl anilide with cyclopentadiene or isoprene proceeded with high diastereoselectivity. (elsevier.com)
Series1
- In this account, we report the development of a series of substituted cinnamic anilides that represents a novel class of mitochondrial permeability transition pore (mPTP) inhibitors. (figshare.com)
Effects1
- Further studies of metyrapone effects upon anilide hydroxylation. (cdc.gov)
Give1
- The copper mediated radical cyclisation of anilides to give oxindoles was also investigated. (warwick.ac.uk)
Study1
- Crystallographic study of the binding of a trifluoroacetyl dipeptide anilide inhibitor with elastase. (semanticscholar.org)