André P Liesen,
Thiago M de Aquino,
Cristiane S Carvalho,
Vânia T Lima,
Janete M de Araújo,
José G de Lima,
Antônio R de Faria,
Edésio J T de Melo,
Antonio J Alves,
Elias W Alves,
Anselmo Q Alves and
Alexandre J S Góes
Abstract
We reported the synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities in vitro of three new compound series obtained from ethyl(5-methyl-1-H-imidazole-4-carboxylate): acylthiosemicarbazide analogues 3a-d, 4-thiazolidinone analogues 4a-d and 1,3,4-thiadiazole analogues 5a-d....
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PMID: 20541294
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Abstract
A fluorescence-enhanced chemodosimeter 1 based on coumarin thiosemicarbazide for Hg(2+) was developed via a Hg(2+)-induced desulfurization reaction. Spectroscopic results reveal that chemodosimeter 1 exhibits high sensitivity and selectivity for Hg(2+) in comparison to common interfering metal ions...
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PMID: 20392664
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Abstract
We depict the synthesis and characterization of copper(II) and zinc(II) coordination compounds of 4-(3',4'-dimethoxybenzaldehydene)2-3-dimethyl-1-phenyl-3-pyrazolin-5-semicarbazone (1a), 4-(3',4'-dimethoxybenzaldehydene)2-3-dimethyl-1-phenyl-3-pyrazolin-5-thiosemicarbazone (1b), 4-(3'-hydroxy-4'-nit...
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PMID: 20363662
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Abstract
Semicarbazide-formaldehyde resin (SFRs) was prepared by the condensation of semicarbazide with formaldehyde in an acidic medium and its polymer metal complexes were prepared with transition metal ions. All the synthesized polymers were characterized by elemental analysis, FTIR, (1)H NMR, (13)C NMR,...
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PMID: 20138409
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Abstract
The release of the substances from food packaging into food triggers the problem for food safety and is the matter of particular interest in the European Commission (EC) and Member States. The problems concerning the presence of these substances in the food which result from their mi...
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PMID: 21446113
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Abstract
New chelates of N(1)-[4-(4-X-phenylsulfonyl)benzoyl]-N(4)-butyl-thiosemicarbazide (X=H, Cl, Br) with Cu(2+) and UO(2)(2+) have been prepared and characterized by analytical and physico-chemical techniques such as magnetic susceptibility measurements, elemental and thermal analyses, e...
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PMID: 19356828
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Abstract
In Japan, N-nitrosodimethylamine (NDMA) formation associated with ozonation at a relatively high concentration has been reported only at a small number of water treatment plants (WTPs) in the western part of Japan for which the source water is the Yodo River. In the present study, the formation of r...
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PMID: 19708347
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Abstract
A series of 3-alkoxy(phenyl)thiophosphorylamido-2-(per-O-acetylglycosyl-1'-imino)thiazolidine-4-one derivatives were prepared by the reaction of 1-alkoxy(phenyl)thiophosphoryl-4-(per-O-acetylglycosyl) thiosemicarbazides with ethyl bromoacetate. (1)H/(13)C HMBC measurements corroborat...
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PMID: 19450796
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Abstract
A series of N-per-O-acetyl-glucosyl arylthiosemicarbazide and thiosemicarbazone derivatives have been synthesized and evaluated for their in vivo anti-dyslipidemic and in vitro antioxidant activities. Among 16 compounds tested, 3 compounds showed potent anti-dyslipidemic activity and 6 compounds sho...
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PMID: 19064319
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Abstract
In the reaction of hydrazide of 3,4-dimethoxyphenylacetic acid (1) with isothiocyanate the respective thiosemicarbazide derivatives (2) were obtained. Further cyclization with 2% NaOH led to the formation of 3-[(3,4-dimethoxyphenyl)methyl]-4-substituted-1,2,4-triazoline-5-thiones (3). The structures...
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PMID: 19226973
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Abstract
The reactions of 1,1-dimethyl-4-phenylthiosemicarbazide (LH) with Cu(II) and Sn(IV) have been investigated. If THF or methanol is used as solvent with Cu(II), oxidative cyclisation and coupling are observed, yielding a 1,2,4-thiadiazole or a 1,3,4-thiadiazolium salt. SnI(4) is also able to induce ox...
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PMID: 19180593
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Abstract
Various isonicotinoylhydrazinocarbothioamides were prepared by reacting isonicotinoyl hydrazide (INH) with appropriate potassium salt of substituted phenyl thiocarbamate and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H(37)R(v) and INH resistant M. tu...
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PMID: 18343086
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Abstract
We selected the natural products limonene and camphene as sources for the preparation of these new thiosemicarbazide derivatives. The compound N(4)-[2,2-dimethyl-3-methylnorbornane]-thiosemicarbazide (TIO C) showed an antifungal effect on Trichophyton mentagrophytes, with values of MIC = 55 mmol L(-...
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PMID: 19471200
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Abstract
These results are explained in terms of the binding of the outer N of the NHNH 2 group in semicarbazide to an active site residue with a relatively low p K a ( approximately 6). Heavy-atom isotope effects for both leaving groups have been determined. For the NHNH 2 side, (15) k obs = 1.0045, whereas...
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PMID: 18817416
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Abstract
We aimed to examine the extent to which the gabaergic mechanisms of this brain region are involved in conditioned fear using the fear-potentiated startle (FPS). Muscimol, a GABA-A receptor agonist, and semicarbazide, an inhibitor of the GABA synthesizing enzyme glutamic acid decarboxylase (GAD), wer...
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PMID: 18634894
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Abstract
We examine the effects of BLA inactivation with the GABA-(A) receptor agonist muscimol (MUS) on the unconditioned fear. We also investigated, through the CPA test, the effects of BLA and/or dPAG inactivation with MUS on the acquisition and the expression of the fear conditioned response. Our results...
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PMID: 18687375
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Abstract
The multifunctional ligand, thiosemicarbazide, was physically loaded on neutral alumina. The produced alumina-modified solid phase (SP) extractor named, alumina-modified thiosemicarbazide (AM-TSC), experienced high thermal and medium stability. This new phase was identified based on surface coverage...
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PMID: 18243533
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Abstract
A new inhibitor for human sirtuin type proteins 1 and 2 (SIRT1 and SIRT2) was discovered through virtual database screening in search of new scaffolds. A series of compounds was synthesized based on the hit compound (3-[[3-(4-tert-butylphenyl)1,2,4-oxadiazole-5-carbonyl]amino]-1-[3-(trifluoromethyl)...
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PMID: 18642893
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Abstract
An enzyme-linked immunosorbent assay (ELISA) method is described for the semi-quantitative determination of semicarbazide (SEM), the marker residue for the banned nitrofuran drug, nitrofurazone, in chicken eggs. The sample homogenate is subjected to acid hydrolysis and derivatisation with o-nitroben...
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PMID: 18608512
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Abstract
The synthetic, spectroscopic, and biological studies of Cu(II), Ni(II), Zn(II), Co(II), Mn(II), Fe(III) and Cr(III) complexes of N(4)-(7'-chloroquinolin-4'-ylamino)-N(1)-(2-hydroxy-benzylidene)thiosemicarbazone (HL) obtained by the reaction of N(4)-(7'-chloroquinolin-4'-ylamino)thiosemicarbazide wit...
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PMID: 18665996
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Abstract
Our aim was to state whether such weight gain limitation could occur in non-obese, non-diabetic rats and to extend these observations to other amine oxidase inhibitors. Prolonged treatment of non-obese rats with a high dose of S (900 micromol kg(-1) day(-1)) reduced body weight gain and limited whit...
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PMID: 18539478
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Abstract
The accumulation, depletion and partitioning of semicarbazide (SEM) and its parent compound nitrofurazone (NFZ) in eggs were studied using hens fed NFZ at therapeutic and sub-therapeutic levels. Dietary NFZ correlated strongly with NFZ and total SEM in eggs, while 28% of observed SEM was present in...
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PMID: 18484297
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Abstract
A novel series of 4-substituted 1-{[4-(10,15,20-triphenylporphyrin-5-yl)phenyl]methylidene}thiosemicarbazide, 4a-4n, was synthesized in 9-21% yield by the condensation of 4-(10,15,20-triphenylporphyrin-5-yl)benzaldehyde (3) with various substituted thiosemicarbazides in presence of c...
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PMID: 18493963
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Abstract
Nitrofuran antibiotic residues in food continue to be of international concern. The finding of sources of semicarbazide (SEM), other than through the misuse of nitrofurazone, present a challenge to the use of SEM as a definitive marker residue for this drug. Detection of intact (parent) nitrofurazon...
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PMID: 18473209
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Abstract
Azodicarbonamide, an approved food additive, is commonly used as a flour additive and dough conditioner in the United States and Canada. A number of researchers have clearly established a link between the use of azodicarbonamide and semicarbazide contamination in commercial bread products. However,...
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PMID: 18303820
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Abstract
The development of a direct competitive enzyme-linked immunosorbent assay (ELISA) based on polyclonal antibodies specific for semicarbazide (SEM) is described. Molecular modelling of the hapten mimics and other key components of the assay system was conducted to explain antibody properties in relati...
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PMID: 18206998
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Abstract
A series of 1-(1-arylethylidene)thiosemicarbazide compounds and their analogues were synthesized and characterized by 1H NMR, MS. Their tyrosinase inhibitory activities were investigated by an assay based on the catalyzing ability of tyrosinase for the oxidation of L-DOPA, comparing with 4-methoxyci...
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PMID: 18326070
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Abstract
New and more potent prodrugs of the 5-fluorouracyl family derived by hydroxymethylation or acyloxymethylation of 5-fluoro-1-(tetrahydro-2-furanyl)-2,4(1H,3H)-pyrimidinedione (tegafur, 1) are described. The anticancer activity of the butyroyloxymethyl-tegafur derivative 3 and not that of tegafur was...
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PMID: 18163551
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Abstract
A series of 5-amino-3-methyl-4-isoxazolecarboxylic acid semicarbazides and thiosemicarbazides (M1-M9) were obtained by reacting 5-amino-3-methyl-4-isoxazolecarboxylic acid hydrazide with isocyanate and isothiocyanate. In order to determine structure-activity relationships for the series of nine comp...
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PMID: 19051600
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Abstract
In the title Schiff base complex, [Zn(C15H12N7OS)2] x 3 C3H7NO x H2O, each Zn(II) atom is six-coordinated in a distorted octahedral environment by two ligands acting in a tridentate chelating mode through two N atoms and one S atom. The coordination mode of the ligand is nearly planar. There are thr...
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PMID: 18216439
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Abstract
SSAO/VAP-1 is not only involved in the metabolism of biogenic and xenobiotic primary amines and in the production of metabolites with cytotoxic effects or certain physiological actions, but also plays a role, for example, as an adhesion molecule, in leukocyte trafficking, in regulating glucose uptak...
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PMID: 18691041
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Abstract
Oscillating chemical reactions are complex systems involving a large number of chemical species. In oscillating chemical reactions, some species, usually reaction intermediates, exhibit fluctuations in their concentration. In this report, a novel slowly-damped oscillating chemiluminescence produced...
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PMID: 18452144
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Abstract
A series of 1-acyl-4-phenyl/(acridin-9-yl)thiosemicarbazides 3, including four new compounds, were prepared in order to study substituent effects on cyclization reactions with oxalyl chloride (producing imidazolidine-4,5-diones 4), dimethyl acetylenedicarboxylate (to give thiazolidin-4-ones 7 and 8)...
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PMID: 18463562
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Abstract
We synthesised 12 new thiadiazolic and triazolic derivatives in order to obtain new possible antituberculosis agents. Early tests on Mycobacterium tuberculosis indicate that 2 of the tested substances have clear antituberculosis activity in vitro for the tested concentrations....
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PMID: 20201282
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Abstract
The experimental electron density of the bis(thiosemicarbazide)zinc(II) dinitrate complex, [Zn(CH5N3S)2](NO3)2,was studied. The Hansen-Coppens multipole model was used to extract the electron density from high-resolution X-ray diffraction data collected at 100 K. Careful strategies were designed for...
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PMID: 18052044
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Abstract
We propose that P+S-induced reduction of fat deposition results from decreased food intake and from impaired MAO- and SSAO-dependent lipogenic and antilipolytic actions of endogenous or alimentary amines....
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PMID: 17977742
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Abstract
We suggest that a loop dPAG-LD-BLA-dPAG is activated during the panic disorder with agoraphobia....
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PMID: 17900567
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Abstract
A new series of first-row transition metal complexes with 1-acetylpyridinium chloride-4-benzoyl thiosemicarbazide (H2GPBzIT) have been prepared and characterized by elemental analysis, spectroscopic and magnetic measurements. The proton-ligand ionization constants were determined potentiometrically...
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PMID: 17317280
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Abstract
4-(N,N-diethylamino)benzaldehyde thiosemicarbazone(DEABT) is proposed as a sensitive and selective analytical reagent for the spectrophotometric determination of palladium(II). The reagent reacts with palladium (II) in a potassium hydrogen phthalate-hydrochloric acid buffer of pH 3.0, to form a yell...
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PMID: 18154003
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Abstract
Acetic acid hydrazide containing 5-methyl-2-benzoxazolinone (4) was synthesized by the condensation of 2-(5-methyl-2-benzoxazolinone-3-yl)acetate with hydrazine hydrate. Thiosemicarbazide derivatives (5a-5d) were afforded by the reaction of corresponding compound 4 with substituted isothiocyanates....
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PMID: 17587585
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Abstract
Nitrofuran antibiotics cannot be used in food production within the European Union because of their potential health risks to consumers. The recent discovery of their widespread use in global food industries and the finding of semicarbazide in baby food as a result of packaging contamination have fo...
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PMID: 17691006
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Abstract
The autonomic activities of mice were significantly inhibited by the volatile oil of Valeriana amurensis. The rate of falling sleep and the extension of sleeping time of mice were significantly increased by the synergic action of pentobarbital sodium with the volatile oil. The sleep phases of SWS2 a...
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PMID: 18074850
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Abstract
These results show that complete impairment of SSAO activity produced by AG-treatment in obese rats was likely responsible for a weak limitation of fat deposition. Previously proposed for prophylaxis in diabetes, AG may be useful for treating obesity via its SSAO blocking properties....
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PMID: 17548204
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Abstract
We now report the first production of antibodies against derivatised SEM. A novel carboxyphenyl SEM derivative was used to raise a polyclonal antibody that has been incorporated into a semi-quantitative microtitre plate ELISA, validated according to the criteria set out in Commission Decision 2002/6...
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PMID: 17499072
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Abstract
This paper reports on the formation and characterization of semicarbazide termination on aminated boron-doped diamond (BDD) surfaces, and further preparation of peptide microarray through site-specific alpha-oxo semicarbazone ligation. Hydrogen-terminated BDD electrodes were first aminated using NH3...
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PMID: 17367174
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Abstract
N-Hydroxythiosemicarbazide was prepared by two methods starting from 2,4-dimethoxy benzyl amine and hydroxylamine hydrochloride, which in turn was reacted with various aldehydes and ketones to obtain the titled compounds. Eighteen compounds were tested for their in vitro activity against Mycobacteri...
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PMID: 17276683
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Abstract
These results indicated that this kinetic method was reliable for serum ethanol assays with obvious advantages....
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PMID: 17420549
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Abstract
The reactions of N,N-substituted thiosemicarbazides with copper salts have been investigated and either copper(II) thiosemicarbazide complexes, 1,3,4-thiadiazolium salts or 1,3,5-thiadiazoles are obtained depending on the Cu(II) salt and solvent used.
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PMID: 17353950
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Abstract
Recently doubts have arisen on the usefulness of semicarbazide as marker residue for the illegal use of the antibiotic nitrofurazone (NFZ) in aquaculture and poultry production. Most notably azodicarbonamide (ADC) has been implicated as an alternative source of semicarbazide. ADC is used in some cou...
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PMID: 17386736
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Abstract
We report a novel method for the chemical micropatterning of polycarbonate based on the printing of functionalized silica nanoparticles. The semicarbazide groups present on the surface of the nanoparticles were used for the site-specific semicarbazone ligation of unprotected peptides derivatized by...
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PMID: 17226879
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Abstract
Three new derivatives of thiosemicarbazides, derived from the reactions of ethyl-, allyl- and phenyl isothiocyanates with Girard's T [(carboxymethyl) trimethylammonium chloride hydrazide] and P [1-(carboxymethyl) pyridinium chloride hydrazide], have been isolated and characterized by chemical analys...
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PMID: 16938486
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Abstract
We studied the effects of drugs modulating GABA content in the brain on communicative activity and sexual motivation of male mice. The effects of the drug depended on animal genotype and initial psychoemotional status. Aminooxyacetic acid elevating GABA content did not modulate communicative activit...
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PMID: 17970208
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Abstract
By the reaction of (5-arylidene-2,4-dioxothiazolidin-3-yl)acetyl chlorides with 4-phenylthiosemicarbazide, acylthiosemicarbazide derivatives 4-6 were obtained. The cyclization of 4-6 in acid medium led to 1,3,4-thiadiazole derivatives 7-9. The structure of the compounds was confirmed by elemental an...
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PMID: 17695145
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Abstract
Interactions of twelve new synthesized 1-N-substituted thiocarbamoyl-3-substituted phenyl-5-pyrolyl-2-pyrazoline derivatives with rat lung semicarbazide-sensitive amine oxidase (SSAO) were assessed. Pyrazoline derivatives were synthesized according to previous methods and SSAO was purified from the...
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PMID: 17385065
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Abstract
We developed an ex vivo model using human coronary artery bypass graft (CABG) blood vessels and a demonstrated acrolein precursor, allylamine. Allylamine induces hypercontraction in isolated rat coronary artery in a semicarbazide-sensitive amine oxidase activity (SSAO) dependent manner. Isolated hum...
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PMID: 17095030
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Abstract
To develop novel biologically active organic compounds possessing a sugar moiety, a series of 2-phenylsulfonylhydrazono-3-(2',3',4',6'-tetra-O-acetyl-beta-d-glucopyranosyl)thiazolidine-4-one were synthesized via reaction of the thiosemicarbazide with ethyl bromoacetate. Their chemical structures wer...
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PMID: 17027940
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Abstract
We have prepared 5-alkyl- and 5-aryl-2-amino-1,3,4-oxadiazoles in 78-99% yield....
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PMID: 17137395
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