Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Pyrazolones”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 541 records · Page 30Linked to original sources
PubMed2002

Determination of oligosaccharides in Pompe disease by electrospray ionization tandem mass spectrometry.

BACKGROUND: The development of therapies for lysosomal storage disorders has created a need for biochemical markers to monitor the efficacy of therapy and methods to quantify these markers in biologic samples. In Pompe disease, the concentration of a tetrasaccharide, consisting of four glucose residues, is reputedly increased in urine and plasma, but faster and more sensitive methods are required for the analysis of this, and other oligosaccharides, from biologic fluids. METHODS: We optimized the derivatization of storage oligosaccharides with 1-phenyl-3-methyl-5-pyrazolone for the measurement, by electrospray ionization tandem mass spectrometry, of oligosaccharide concentrations in urine (n = 6), plasma (n = 11), and dried-blood spots (n = 17) from Pompe-affected individuals. Age-matched control samples of urine (n = 10), plasma (n = 28), and blood spots (n = 369) were also analyzed. RESULTS: The mean tetrasaccharide concentration was increased in urine from infantile-onset (0.69-12 mmol/mol of creatinine) and adult-onset (0.22-3.0 mmol/mol of creatinine) Pompe individuals compared with age-matched controls. In plasma samples, an increased tetrasaccharide concentration was observed in some infantile patients (up to 22 micromol/L) compared with age-matched controls (mean, 2.2 micromol/L). The method developed was sensitive enough to determine oligosaccharide concentrations in a single 3-mm blood spot, but no differences were observed between blood spots from control and Pompe-affected individuals. CONCLUSIONS: Measurements of oligosaccharide concentrations in urine by this new method have potential application for the diagnosis and monitoring of patients with Pompe disease. Plasma analysis may have limited application for infantile patients, but analysis of blood spots does not discriminate between controls and affected individuals.

Adolescent↗
PubMedDate not supplied

Effect of antirheumatic drugs on neutral protease from human leucocyte granules.

The inhibitory effect of 38 antirheumatic and other agents on purified neutral protease from human polymorphonuclear leucocytes has been studied by determining the decrease in enzyme activity on Z-Ala-NPH as substrate. Analgesics, salicylates, cytostatic agents and steroids, as well as D-penicillamine, colchicine, allopurinol, chlorzoxazone and chlorpromazine, either had no effect on neutral protease or inhibited it only to a very small extent. Typical antirheumatic agents like gold and pyrazolone derivatives suppressed the activity of the enzyme at a concentration of 10(-5)M. The two sulphonated polysaccharides Arteparon and pentosan polysulphate (SP 54) were the most potent inhibitors of neutral protease (inhibition down to 10(-8)M). Increasing concentrations of various inorganic salts gradually suppressed the effect of some otherwise effective drugs on neutral protease. The drugs were completely ineffective at a salt concentration of 0.5 M. At physiological concentrations, however, this effect was insignificant. Inhibition of neutral protease may be one way in which some antirheumatic drugs exert a therapeutic effect in rheumatic diseases.

Anti-Inflammatory Agents↗
PubMed1992

Influence of mofebutazone in comparison to phenylbutazone on the adenosine triphosphate level of polymorphonuclear cells and their migration.

Two pyrazolon derivatives--mofebutazone (CAS 2210-63-1) and phenylbutazone (CAS 50-33-9)--were compared as to their effects on the adenosine triphosphate (ATP) level of polymorphonuclear cells (PMNs) and their response to the migration of these cells. In the range of 10(-8) to 10(-3) mol/l neither mofebutazone nor phenylbutazone significantly changed the ATP level of PMNs. Compared to the untreated PMNs only phenylbutazone reduced the migration of PMNs significantly (chemotactic index (CI) 0.46) at a concentration of 10(-3) mol/l. On the other hand with mofebutazone no statistically significant abnormality on PMN migration was found. Direct statistical comparisons of the migration between specific concentrations of the two pharmaceuticals did not indicate a different migration behavior even at 10(-3) mol/l. These results show that in contrast to the chemical and pharmacological differences of mofebutazone and phenylbutazone their effect on the ATP level and the migration of PMNs is comparable.

Adenosine Triphosphate↗
PubMed2003

[The determination of konjac glucomannan in konjac refined powder and monosaccharide compositions by HPLC].

OBJECTIVE: To establish a quantitative method for the content determination and monosaccharide composition analysis of Konjac glucomannan (KGM) in Konjac refined powder by pre-column derivatization high performance liquid chromatographic method (HPLC). METHOD: The two derivatives combined reducing monosaccharides with 1-phenyl-3-methyl-5-pyrazolone (PMP) were separated by reverse-phase HPLC using a developed fragment gradient elution process, and monitored by ultraviolet detector at 250 nm. The broad reagent peak of PMP was separated very well from all the PMP-sugars, and good separation was achieved for derivatives of mannose and glucose. The quantitative methods of two reducing monosaccharides were studied by the method combined internal and external standard; while the KGM content in Konjac refined powder was determined. RESULT: Linearity of glucose was good (r = 0.9990) in range of 1.002-8.016 nmol; while mannose (r = 0.9994) in range of 1.001-8.008 nmol. The average recovery of this method was 98.1%, RSD of repeatability was 1.72%. KGM content in Konjac refined powder was 79.5%, ratio of glucose to mannose in KGM was 1:1.51. CONCLUSION: This method is a sample, convenient and rapid method that can determine KGM content and analyze monosaccharide compositions in KGM, which will be helpful to quality assessment of Konjac refined powder.

Amorphophallus↗
PubMed2004

Synthesis of some new annulated pyrazolo-pyrido (or pyrano) pyrimidine, pyrazolopyridine and pyranopyrazole derivatives.

The bifunctional pyrazolopyridine (2) and pyrano-pyrazole (3) derivatives were prepared by the reaction of 2-(2,4-dinitrophenyl)-5-methyl-2,4-dihydro-3H-pyrazol-3-one (1) with p-methoxybenzaldehyde, malononitrile in the presence of ammonium acetate or piperidine, respectively. Compound 2 was used as the key intermediate to prepare the pyrazolo-pyrido-pyrimidine derivatives through its reaction with formic acid, formamide-formic acid-DMF, ammonium thiocyanate or reaction with triethyl orthoformate followed by cyclization with hydrazine hydrate. Reaction of 3 with triethyl orthoformate followed by cyclization with hydrazine hydrate gave the pyrazolo-pyrano-pyrimidine derivative 11. Reaction of ethyl-3-oxo-2-[2-phenyl-diazenyl]butanoate and ethyl 2-[2-(4-chlorophenyl)diazenyl]-3-oxobutanoate with 1 to give the pyrazolone derivatives 13a and 13b, was also considered.

Anti-Infective Agents↗
PubMed2004

[The allergic and other side effects of non-steroid antiinflammatory drugs and gold salts].

UNLABELLED: The wider usage of non steroid antiinflammatory drugs (NSAIDs) raises the significance of their side effects. The discovery of the two different cyclo-oxygenases (COX 1 and COX-2) led to the incorporation of more selective enzyme inhibitors into the therapeutic tools against disorders with pain and inflammation, in order to minimize the frequency of the side effects. Selective COX-2 inhibitors are well tolerated by most of the patients with a history of sensitivity against classical NSAIDs. The well-known gastrointestinal side effects (ulcers, bleedings) are much less frequent in the case of selective COX-2 inhibitors in comparison with non-selective COX inhibitors. However, the lack of "healing" prostaglandins as an effect of COX-2 antagonism may prevent the improvement of existing ulcers. In addition almost all other organs have been found to be affected in COX-2 knockout mice (COX-2 paradoxon). Hepatotoxicity is usually rare, its reason is most probably idiosyncrasy. Persistent nephropathy can be worsened by the inhibition of COX-2, however normal renal functions have not been changed in humans using selective COX-2 inhibitors. Authors' registry consists of 1000 patients with a history of suspected drug-allergy, during a 15 years' period. Approximately 30% of the cases have been connected with NSAIDs and with antirheumatic drugs. Because of functional similarities gold salts, proved suitable for the treatment of juvenile rheumatoid arthritis (JRA) and of osteoarthritis (OA) were included as well. Besides rheumatologic applications the second most common indication for these drugs was pain and/or fever. Among cutaneous symptoms intolerance was present at a relatively low frequency--as salicylates had not been taken into consideration. Next to salicylates the most frequent side effects were caused by pyrazolon derivates. Urticaria and angioedema were the most frequently observed symptoms on the skin--our observations are in accordance with other publications. CONCLUSIONS: Non-selective NSAIDs show a mixed effect of inhibitions of COX-1 and COX-2. The most important indications of modern selective COX-2 inhibitors are: 1. Prevention of the gastrointestinal side effects 2. Avoidance of cross-sensitivity against non-selective NSAIDs.

Adult↗
PubMed1978

[Lyell' syndrome: a review with special regard to the form caused by drugs (author's transl)].

The clinical evolution of Lyell' syndrome (LS), its complications, the histological findings, the nosological position and the differentiation from erythema exsudativum multiforme are dealt with. There are at least two etiological forms of LS: the LS caused by staphylococci, and the LS caused by drugs. The former mainly occurs in children, and is caused by staphylococci of the phagous group II, while the latter is mainly caused by sulfonamides, pyrazolones, penicillines, barbiturates and salicylates. The causative responsibility of a certain drug can be proved by three criteria: 1. Relapse of LS after exposure to the same drug. 2. Allergy to the drug taken before the onset of LS. 3. Positive allergy tests. The hypothesis concerning the pathogenesis of LS caused by drugs, the differential diagnosis and therapeutical guidelines are dealt with.

Acute Kidney Injury↗
PubMed1979

A review of spontaneously reported adverse drug reactions with diclofenac sodium (Voltarol).

The author reviews the worldwide picture of adverse reactions reported with diclofenac during the four-year period ending in December 1977, at which point he estimates that some ten million patients had received treatment with the drug. A total of 447 unwanted effects were reported in 194 patients, the most frequently reported side-effects being gastrointestinal in nature, followed by dermatological and central nervous system effects. Thirteen cases of liver function abnormality were reported, although there was reason to believe that 11 of these were not ascribable to diclofenac. Twenty haematological effects were reported, including two cases of agranulocytosis and two cases of fatal aplastic anaemia; one patient in each of these groups was taking concomitant pyrazolone compounds. Evaluation of adverse reactions reported with diclofenac suggest a profile in which gastrointestinal side-effects predominate; however, the risk of serious side-effects of this nature is slight, and the impression of good tolerability which emerges from this review is confirmed by the findings of comparative clinical trials.

Adult↗
PubMedDate not supplied

[Neurocysticercosis--pathogenesis and clinical aspects].

Neurocysticercosis is an infestation of the central nervous system with the larval cysts of the pork tapeworm (Taenia solium), when a man is paratenic host of the parasite. The infection results from ingestion of food or water contaminated with human feces containing the parasitic eggs. Much rarely, the infection is caused by autoinoculation, when the mature parasites are present in the small intestines, and reversed peristalsis gives rise to regurgitation of gravid proglottides (internal auto-infestation), or by ingestion of the eggs from one's own feces (external auto-infestation). The embryos (oncospheres) develop from the eggs, penetrating the small intestine mucosa and entering the circulation and subsequently different tissues and organs where cysticerci, small tissue larvae, are developed. Cysticerci have specific affinity for the central nervous system, eyes and striated muscles what is accounted for high concentration of glucose or glycogen in these organs. Neurocysticercosis is the most frequent parasitic disease of the central nervous system and the most common cause of convulsions and hydrocephalus in the adults in endemic regions, where the seroprevalence of disease is about 4% of population. Neurocysticercosis is classified into six clinical syndromes: asymptomatic, parenchymal, subarachnoid, intraventricular, spinal and ocular forms. Albendazole (benzimidazole) of 15 mg/kg/BW during 8-28 days or praziquantel (pyrazolone quinoline) of 50-60 mg/kg/BW during 15 days (or 100 mg/kg/BW only one day) are applied for treatment of neurocysticercosis.

Humans↗
PubMedDate not supplied

[The molecular bases of the pathogenesis of malaria and their potential uses in developing a combined therapy for the infection].

Molecular mimicry of a host is essential malaria parasite invasion and spreading in a host and it makes self-advantage for the parasite affecting vital organs and systems of the latter. It is tempting to assume that monoclonal antibody (MA) blocking specific (such as IMAM-I or CD36) and some unspecific (such as C3b) receptors of the blood stages of P. falciparum may prevent the malignant course of the infection. In our experience pyrazolone derivative not only suppressed schizont P. vivax infection but parasitemia too. After ceasing the drug administration, fever and parasitemia reappeared. It is of interest to study whether MA to the parasite hsp75 kD are able to suppress blood schizogony in P. falciparum infection. The prevention with MA to IFN-ů the development of experimental cerebral malaria has been reported. Principally new approach in advancing the therapy of malignant malaria might be inducing agents of TNF inhibitors production. The suppressing of the parasite activity by blocking its receptors in a host seems to be perspective in the therapy of malignant malaria.

Animals↗
PubMedDate not supplied

[New pyridazine compounds with possible physiological action].

The methods of obtaining and the physicochemical and spectral characterization of eight new pyridazine derivatives are presented. Thus, the reaction of chlorine-hydrazino-pyridazine with pyruvic and alpha-ketoglutaric acids resulted in the corresponding hydrazones. Using the indications in the literature the tetrazolic, triazolic, pyrazolonic and phenyl-thiocarbazidic derivatives of hydrazino-pyridazine were synthetized. The structure of the new compounds was confirmed by carbon, hydrogen and nitrogen analyses and spectral ones in infrared.

Chemical Phenomena↗
PubMed1990

Principles of managing chronic rheumatic diseases.

The principles of treating chronic rheumatic diseases are to be conceived as a complex care of the patient. Medication is just one part of the treatment, be it a very important one. Its possibilities are, however, restricted. In spite of the explosive appearance of new antirheumatic drugs we are sticking to the classical forms of treatment (salicylates, gold, antimalaric drugs). Pyrazolone derivatives and corticoids are still holding their place in the therapeutic design. They should be administered, however, wisely and one must be aware of what is to be expected of their effect. A special therapeutic problem appears to be osteoarthrosis, which has recently become more actual among the other rheumatic diseases. The therapeutic effort must be completed by social care of the patient suffering from a chronic rheumatic disease, at least in cases when the patient depends on the help of another person.

Arthritis, Rheumatoid↗
PubMed1990

The pharmacokinetics of pirazolac in human subjects.

Pirazolac (PAA) is a new non-steroidal anti-inflammatory drug (NSAID) belonging to the subgroup of heterocyclic acetic acids. PAA is rapidly and completely absorbed and bioavailable at all dose levels tested. Plasma level curves after oral administration of capsule-shaped tablets were no different from those after administration of a crystalline suspension. The drug is highly (greater than 99%) bound to plasma albumins and penetrates easily into the synovial fluid. Plasma levels obey first-order pharmacokinetics over the whole therapeutic dose range. PAA is entirely conjugated with glucuronic acid before leaving the body, mainly in the urine. It has an intermediate elimination half-life of 17 h which does not depend on age or sex. Under twice-daily administration, fairly constant plasma levels are achieved, thus avoiding the high fluctuation observed with short half-life NSAIDs like indomethacin or diclofenac, and also avoiding the excessive accumulation observed with long half-life NSAIDs like pyrazolones and oxicams. This pharmacokinetic property makes pirazolac highly appropriate for long-term therapy of rheumatic diseases.

Absorption↗
PubMedDate not supplied

[Adverse reactions to food preservatives].

We relate our experiences about the number of exacerbations that certain food preservatives such as sorbic acid, benzoic acid, sodium benzoate, metabisulfite and sodium nitrate can provoke in 62 patients affected with ASA-triad in steroid dependent intrinsic asthma with nasal polyps and acute bronchospasm caused by aspirin ingestion, and in 80 patients with chronic urticaria (C.U.) as well as the first assays of the possible usefulness of the HRT (Histamine release test automatized using whole blood) for the etiologic diagnosis process. In the cases of ASA-triad, and after the ingestion of aspirin (alternating with lactose in identical capsule), we consider the result as positive when the reduction of FEV1 is superior to 20% from its baseline value. Regarding the cases of C.U., the symptoms always exacerbate twice as much with the same substance within 24 hours of its administration. We have performed the HRT on 59 patients (14 with ASA-triad, 11 with steroid dependent intrinsic asthma; 20 with C.U. were negative to oral intake of analgesics/additives and 14 with C.U. showed positive results). Successive dilutions were incubated for 30 minutes using: pyrazolones, acetylsalicylate of lysine, sodium salicylate, sodium benzoate and 4-hydroxybenzoic acid which did not produce liberation of histamine in 100 controlled individuals. All the determinations were done in duplicate, considering positive those superior to 20% of the difference between total and basal histamine. We have not observed any significant descent of the FEV1 with benzoate and salicylate in our group of 62 patients with ASA-triad, nor any manifestations presented with sodium metabisulfite, sodium nitrate and sorbic acid.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1989

[Use of non-steroidal antiinflammatory drugs in specialty polyclinic practice].

A retrospective investigation of the prescription of nonsteroidal antiinflammatory drugs (NSA) was performed in the Rheumatologic out-patient-institute in Zagreb, including 1000 patients of both sexes, aged 20-70 years. 500 outpatients were treated by NSA during 1987 and 1989 respectively for lumbosacral syndrome, rheumatoid arthritis, ankylosing spondylitis and coxarthrosis. The kind of NSA as well as the registered side-effects were analysed from case histories. During 1987, NSA were applied to 365 (73%) and during 1989 to 390 (78%) of the 500 patients. In both groups a phenyl-acetic acid derivative (diclophenac) was most often applied, followed by propionic acid derivatives and oxycams. The most rarely applied drugs were indol-acetic acid derivatives. Pyrazolones were given only to 2 patients with an acute flare of ankylosing spondylitis in 1987. A gastro-duodenal ulcer was the absolute counterindication for this kind of treatment. The number of side-effects in this investigation was relatively small (6.5% in 1987 and 5% in 1989), probably because this investigation was a retrospective one. The most common among them appeared in the gastro-intestinal tract.

Adult↗
PubMed1989

Non-surgical synovectomy (basic principles).

Non-surgical synovectomy is an important therapeutical method, the spreading of which is due to intensive research in the ways of treatment, particularly in rheumatoid arthritis. Various procedures have been worked out to settle pathological changes first on the synovial membrane (synoviorthesis) by intraarticular administration of pharmacological substances. From this point of view, we report on cortisonoids, chloroquine, cytostatic drugs, pyrazolone derivates and antiproteolytic substances. Special attention is paid to osmic acid and radioactive colloids as possible. It is a matter of the physician's skill and further research to find the optimal drug for synoviorthesis so as to introduce it into the long-term and systematic therapeutical programme necessarily required by rheumatoid arthritis.

Arthritis, Rheumatoid↗
PubMed1989

[The quantitative determination of cyanide by FTD-GC].

In recent buildings, new materials containing chemical goods, chemical fibers and the like are in common use. Some of them evolve hydrogen cyanide (HCN) when burning. When a person meets a fire, therefore, it is necessary to measure his blood concentration of HCN as well as that of CO-Hb%. The blood concentration of HCN can be measured by colorimetry such as pyridine-pyrazolone method, gas-chromatography, electrode method, or the like. However, these methods require much time in pretreatment and the preparation of the reagent. We have investigated to find a new measurement method free from the above demerits, so that we have found the method by FTD-GC (Flame Thermionic Detecter Gas-chromatograph) is convenient and can be effected in a short time in comparison with the aforementioned method. GC-7AG made by Shimadzu Co. is employed as gas-chromatography and the headspace method is used in the quantitative determination. Samples are employed as solutions of potassium cyanide (KCN) either in distilled water or in fresh blood. The concentration of KCN is gradient in the range of 0.5-6 micrograms/ml. The quantitative conditions is investigated by a solution in distilled water as standard. Using this method, the concentration of HCN in the blood sample is determined slightly lower than that in the distilled water; however, this method is advantageous in convenience and the saving of time. Therefore, the method is useful in practice for the determination of the concentration of HCN.(ABSTRACT TRUNCATED AT 250 WORDS)

Chromatography, Gas↗
PubMed1989

[Glucocorticoid receptors as targets for pharmacologic action].

Experimental data demonstrate the influence of certain drugs on the interaction of Type II and III glucocorticoid receptors of the liver cytosol and labelled natural and synthetic glucocorticoids. Preparations of the phenothiazine (aminazine, tizercine) and pyrazolone (amidopyrine, analginum) series and non-steroid anti-inflammatory drugs (acetylsalicylic acid, sodium salicylate) exert a significant effect on the glucocorticoid-receptor interplay. Certain drugs (tizercine, analginum) have an anti-stress effect by lowering the level of Type II glucocorticoid receptors of liver cytosol and corticosterone concentration in the blood plasma of rats. The phenothiazine and no-spa derivatives inhibit the matrix activity of the thymocyte DNA in adrenalectomized rats. Pyracetam, caffeine, adrenaline, noradrenaline, verapamil, digoxin, and streptomycin do not influence the thymocyte DNA matrix activity in the presence of triamcinolone acetonide. Based on the literature data and original research findings, the problem of glucocorticoid receptors employment as targets for medication to control the glucocorticoid effect and stress is discussed.

Analgesics↗