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1.
Res Q Exerc Sport ; 79(2): 166-73, 2008 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-18664041

RESUMO

General socioeconomic conditions as well as the physical environment have undergone remarkable changes in Hungary during the past 30 years. Unfortunately, these positive processes have resulted in a reduction of habitual physical activity along with unfavorable changes in dietary habits. Therefore, the purpose of the present study was to compare some selected morphological and functional parameters of 7-14-year-old Hungarian schoolboys living in the middle of the 1970s and at the beginning of the new millennium. It was hypothesized that there would be significant differences in morphological and functional characteristics of the Hungarian schoolboy populations, because they were assessed 30 years apart. Means of height, body mass, body mass index (BMI), the sum of five skinfold tests, percentage of body fat, and two running performance times (400 m and 1,200 m) of the boys (N = 3,672) studied in 1975 were compared to those of the boys (N = 3,758) in 2005. Data were analyzed using two-tailed independent samples t tests (p < .05). We observed significant secular changes in body mass and height. In addition, boys in 2005 had significantly more subcutaneous fat compared to 1975. The running times for the two distances were significantly poorer at the time of the second investigation. The remarkable and unfavorable changes in body composition and cardiorespiratory performance were attributed to the continuously decreasing intensity of habitual physical exercise and a lifestyle that had become more sedentary (watching TV playing computer games, etc.). Radical interventions are necessary to reduce these risks associated with the high prevalence of cardiovascular disease in Hungary, and the challenge to resolve the problem requires combined efforts at the educational, societal, corporate, and governmental levels.


Assuntos
Composição Corporal , Estilo de Vida , Aptidão Física , Adolescente , Índice de Massa Corporal , Criança , Intervalos de Confiança , Meio Ambiente , Humanos , Hungria , Masculino , Vigilância da População , Dobras Cutâneas , Fatores Socioeconômicos
2.
Acta Physiol Hung ; 94(3): 191-8, 2007 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-17853771

RESUMO

The prevalence of overweight or fat children and adolescents has markedly increased in Hungary during the past three decades. Among the possible factors insufficient physical activity and a relative or absolute excess of calorie intake associated to it can be regarded as the most important ones. The aim of the study was to analyse the effects of a 20-week aerobic exercise on body composition and on the exercise tested cardio-respiratory functions in 10-year-old obese boys. Obesity was defined by a BMI greater than the cut-off value reported by Cole and co-workers (5) and a relative body fat content above 30% (13). Of the study group 21 volunteer children completed the program; the contrast group contained 28 obese boys. Mean calendar age was 10.03 +/- 0.26 in the study group (S) and 9.88 +/- 0.29 in the control group (C). The members of group S had two curricular physical education (PE) classes a week and three extracurricular aerobic physical activity sessions of 60 min net time in the afternoon, on Mondays (swimming and water games), Wednesdays (folk dance) and Fridays (soccer). Group C had only 2 PE classes a week. Anthropometric and spiroergometric data were collected in the middle of January and June of 2004. Relative body fat content and BMI did not increase during the observation period in contrast to the significant increase of both in the control group. Peak minute ventilation, aerobic power, oxygen pulse, and running distance (performed on a treadmill) increased in group S, and did not change in group C. The program was considered successful despite that the changes in the observed physiological and physical indicators appeared to be slight. However, the 5-month elevated level of physical activity brought about such development in the physical status of the obese subjects that might be an appropriate basis for regular training. Fortunately, the cardio-respiratory functions of the investigated boys were not affected yet by obesity, consequently the really dramatic change in their further lifestyle exclusively depends on their decision.


Assuntos
Distribuição da Gordura Corporal , Terapia por Exercício , Frequência Cardíaca , Obesidade/terapia , Consumo de Oxigênio , Ventilação Pulmonar , Corrida , Estatura , Índice de Massa Corporal , Peso Corporal , Estudos de Casos e Controles , Criança , Humanos , Masculino , Obesidade/fisiopatologia , Espirometria , Resultado do Tratamento
3.
Acta Physiol Hung ; 94(3): 267-70, 2007 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-17853778

RESUMO

Increasing prevalence of overweight and obesity is a serious social and health problem both in the economically developed and developing countries. Despite this fact the nation-wide growth studies completed in Hungary during the past 30 years had not categorised the children either by body fat content or nutritional status. The aim of the study was to estimate the prevalence of overweight and obese boys in the country at the beginning of the new millennium. Height, body mass and four skinfold thicknesses were measured in 7173 volunteer boys aged between 7 and 10 and living in various urban and rural settlements of Hungary between 2003 and 2005. Nutritional status was qualified by the BMI and relative body fat content. The significantly increasing prevalence with age of overweight and obesity ranged between 10.3 and 23.4%. The results showed the joint effects of a secular trend of growth and of a remarkably changed lifestyle. Of these the consequences of the lifestyle are the more important ones. The high and possibly further increasing prevalence of child-age overweight and obesity reminds one of the observations of Kopp and associates (5), namely that of the increased prevalence of chronic childhood diseases during the past 15 years. More intense habitual physical activity and dramatic changes in dietary habits still promise some solution. No one should reckon, however, with the efficiency of physical education at the schools with its very few classes.


Assuntos
Obesidade/epidemiologia , Sobrepeso , Distribuição da Gordura Corporal , Estatura , Índice de Massa Corporal , Peso Corporal , Criança , Humanos , Hungria/epidemiologia , Estilo de Vida , Masculino , Estado Nutricional , Obesidade/fisiopatologia , Vigilância da População , Prevalência
4.
Heart ; 91(9): 1164-6, 2005 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-16103548

RESUMO

OBJECTIVES: To examine the hypothesis that glyceryl trinitrate (GTN) may cause headache in patients with normal coronary arteries more often than in patients with obstructive coronary artery disease (CAD). This simple assessment may aid clinicians in the initial evaluation of chest pain syndrome and possible CAD. PATIENTS AND METHODS: 118 patients (66 men and 52 women) with new onset of chest pain were enrolled in this study. Patients were excluded from the study if they had a history of chronic headache, long term nitrates use, or any coronary artery procedures. Mean age of the patients was 62.5 years. Coronary angiography was performed within one month of GTN administration with the usual clinical indications such as recurrent chest pain, abnormal ECG, or abnormal results of stress tests. Thirty patients had normal coronary arteries or minimal or non-obstructive CAD. Eighty eight patients had obstructive CAD defined as luminal narrowing greater than 50% in any one or more of the left or right coronary arteries or their major branches. All the patients had a varying degree of relief of chest pain with GTN administration within 10 minutes. 36% of patients reported significant headache after GTN administration. RESULTS: In patients with normal coronary arteries or minimal CAD, 73% had significant headache caused by sublingual GTN. In patients with obstructive CAD, only 23% had significant headache after GTN use (p < 0.001). There were no differences in patients' sex and vascular risk factors concerning the frequency of headache in patients with or without obstructive CAD. CONCLUSIONS: GTN causes significantly more frequent headache episodes in patients with normal coronary arteries or minimal CAD than in patients with obstructive CAD. This unique finding may provide clinicians with an additional tool for the differential diagnosis of patients with chest pain syndrome.


Assuntos
Estenose Coronária/diagnóstico , Cefaleia/induzido quimicamente , Nitroglicerina/efeitos adversos , Vasodilatadores/efeitos adversos , Idoso , Dor no Peito/etiologia , Angiografia Coronária , Estenose Coronária/complicações , Estenose Coronária/tratamento farmacológico , Feminino , Cefaleia/complicações , Humanos , Masculino , Pessoa de Meia-Idade , Nitroglicerina/uso terapêutico , Vasodilatadores/uso terapêutico
5.
Orv Hetil ; 142(34): 1851-4, 2001 Aug 26.
Artigo em Húngaro | MEDLINE | ID: mdl-11681232

RESUMO

This is a case history of a 24-year-old female patient in whom two rare pulmonary diseases occurred: Langerhans cell histiocytosis and four years later lymphangioleiomyomatosis were diagnosed. Both diseases were verified by the examination of the lung tissue removed by the surgery for pneumothorax. The patient's symptoms were characterised by coughing, dyspnoe, repeated pneumothorax. The authors summarised the characteristics and treatment of these diseases. This case history is worth of reporting for its unique rareness.


Assuntos
Histiocitose de Células de Langerhans/complicações , Histiocitose de Células de Langerhans/diagnóstico , Neoplasias Pulmonares/complicações , Neoplasias Pulmonares/diagnóstico , Linfangioleiomiomatose/complicações , Linfangioleiomiomatose/diagnóstico , Adulto , Diagnóstico Diferencial , Dispneia/etiologia , Feminino , Histiocitose de Células de Langerhans/patologia , Humanos , Neoplasias Pulmonares/patologia , Linfangioleiomiomatose/patologia , Prognóstico
7.
Neurobiology (Bp) ; 8(2): 215-23, 2000.
Artigo em Inglês | MEDLINE | ID: mdl-11061216

RESUMO

Recent data suggest that elevated serum semicarbazide-sensitive amine oxidase activity (SSAO) may cause endothelial injury. Formation of cytotoxic metabolites (especially formaldehyde) and increased oxidative stress might lead to initiation or progression of atherosclerosis. Effective and selective inhibitors of human SSAO might exert cytoprotective effect on endothelial cells. To compare the inhibitor sensitivity of human serum and vascular tissue SSAO enzyme, the inhibitory effect of semicarbazide and MDL 72974A was investigated. Serum and vascular SSAO activity has been determined using 14C-benzylamine as a substrate. The IC50 values of semicarbazide were estimated to be 5x10(-3) M and 5x10(-4) M for SSAO from human serum and saphenous vein, respectively. MDL 72974A amine oxidase inhibitor was more than thousand times more effective than semicarbazide. The IC50 values were 10(-7) M and 10(-8) M for SSAO from human serum and saphenous vein, respectively. This finding supports the hypothesis that soluble and membrane-bound vascular SSAO enzymes might have similar structure.


Assuntos
Amina Oxidase (contendo Cobre)/antagonistas & inibidores , Amina Oxidase (contendo Cobre)/sangue , Endotélio Vascular/enzimologia , Músculo Liso Vascular/enzimologia , Compostos Alílicos/farmacologia , Arteriosclerose/sangue , Butilaminas/farmacologia , Diabetes Mellitus Tipo 2/sangue , Angiopatias Diabéticas/sangue , Humanos , Monoaminoxidase/sangue , Inibidores da Monoaminoxidase/farmacologia , Veia Safena/enzimologia , Solubilidade
8.
Am Heart J ; 139(1 Pt 1): 101-5, 2000 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-10618569

RESUMO

BACKGROUND: Mitral valve prolapse syndrome (MVPS), a term applied to patients who have a variety of symptoms, has been associated with autonomic or neuroendocrine dysfunction. Recent evidence suggests that effects of angiotensin II mediated by the angiotensin II type 1 (AT(1)) receptor are involved in modulation of cardiovascular autonomic control in human beings. Association of a genetic polymorphism (A-C(1166)) of the AT(1) gene with abnormal vasomotion and low blood pressure related to autonomic control has been reported recently. Because the role of this genetic variant in MVPS has not been studied, we performed a case-control study of the A-C(1166) variant in a group of 76 white subjects with MVPS. METHODS AND RESULTS: All patients were genotyped by use of a mismatch polymerase chain reaction/Afl II restriction fragment length polymorphism analysis. Frequency of the C(1166) allele was 0.4 in patients with MVPS and 0.26 in control patients. The difference in genotype (chi square = 6.5; P <.05) and allele (chi square = 5.9; P =.02) frequencies between the groups was significant. The odds ratio in favor of carrying the C allele was 4 times greater for patients with MVP than for control patients (95% confidence interval 1.4 to 12.1). CONCLUSIONS: The current results indicate that the A-C(1166) polymorphism of the angiotensin II type 1 receptor gene is associated with MVPS in the white population.


Assuntos
Prolapso da Valva Mitral/genética , Polimorfismo Genético , Receptores de Angiotensina/genética , Adulto , Alelos , Pressão Sanguínea , DNA/análise , Feminino , Frequência do Gene , Marcadores Genéticos , Genótipo , Humanos , Masculino , Prolapso da Valva Mitral/sangue , Prolapso da Valva Mitral/fisiopatologia , Razão de Chances , Reação em Cadeia da Polimerase , Polimorfismo de Fragmento de Restrição , Receptor Tipo 1 de Angiotensina , Receptor Tipo 2 de Angiotensina , Síndrome , Vasodilatação
9.
Metabolism ; 48(1): 113-7, 1999 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-9920154

RESUMO

Previous clinical studies reported elevated semicarbazide-sensitive amine oxidase (SSAO) activity in insulin-dependent diabetes mellitus (IDDM), but there are not sufficient data about SSAO in non-insulin-dependent diabetes mellitus (NIDDM). The present study was conducted to investigate serum SSAO activity in NIDDM patients compared with nondiabetic and IDDM patients. Serum SSAO activity in 61 patients with diabetes (n = 34 NIDDM and n = 27 IDDM) and 36 controls was determined using 14C-benzylamine as a substrate. NIDDM and IDDM patients exhibited higher SSAO activity compared with controls ([mean +/- SD] NIDDM, 164.60+/-69.43 pmol/mg protein/h, P<.0001; IDDM, 143.91+/-72.45 pmol/mg protein/h, P<.002; control, 91.46+/-28.11 pmol/mg protein/h). There was a significant positive correlation between serum SSAO activity and the body mass index (BMI), body weight, hemoglobin A1c (HbA1c), fasting plasma glucose, and triglycerides. Within the control group, SSAO correlated with total cholesterol levels. The progression and severity of diabetic complications such as angiopathy may be exacerbated by cytotoxic metabolites (e.g., formaldehyde and hydrogen peroxide) formed by SSAO. These results reveal the possibility that elevated serum SSAO activity in association with obesity and hyperlipidemia may be a cardiovascular risk factor in diabetes mellitus.


Assuntos
Amina Oxidase (contendo Cobre)/sangue , Índice de Massa Corporal , Diabetes Mellitus Tipo 2/enzimologia , Triglicerídeos/sangue , Adulto , Idoso , Colesterol/sangue , Diabetes Mellitus Tipo 2/etiologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Obesidade/complicações , Obesidade/enzimologia
10.
Eur J Drug Metab Pharmacokinet ; 24(4): 299-302, 1999.
Artigo em Inglês | MEDLINE | ID: mdl-10892891

RESUMO

Semicarbazide-sensitive amine oxidase (SSAO) is present in the plasma membrane of several human tissues, e.g. vascular smooth muscle cell adipocytes, and is also found in human serum. Some previous studies on cultured endothelial cells indicate that cytotoxic metabolites (e.g. hydrogen peroxide, formaldehyde, acrolein) formed by serum SSAO may cause endothelial injury and subsequently induce atherosclerosis. To investigate the role of this enzyme in the pathogenesis of macrovascular complications in diabetes, a simple and sensitive radiometric procedure was adapted for human serum measurements. Serum SSAO activity of 35 patients with non-insulin dependent diabetes mellitus (NIDDM) and that of 30 controls was determined using [14C]-benzylamine as substrate. The severity of atherosclerosis was assessed by carotid sonography. Diabetic patients with atherosclerosis exhibited a higher SSAO activity compared to diabetic patients without complications (212.91 +/- 90.54 pmol/mg protein/h versus 133.17 +/- 65.40 pmol/mg protein/h, P <0.04). In diabetic patients without complications, serum SSAO activity was elevated compared to control subjects (133.17 +/- 65.40 pmol/mg protein/h versus 91.79 +/- 31.70 pmol/mg protein/h, P <0.01). These results suggest that determination of human serum SSAO activity might be a useful marker in the prognostic evaluation of diabetic angiopathy and atherosclerosis.


Assuntos
Amina Oxidase (contendo Cobre)/metabolismo , Arteriosclerose/enzimologia , Adulto , Idoso , Arteriosclerose/etiologia , Biomarcadores , Diabetes Mellitus Tipo 2/enzimologia , Angiopatias Diabéticas/enzimologia , Angiopatias Diabéticas/etiologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Fatores de Risco
11.
J Neural Transm Suppl ; 52: 79-85, 1998.
Artigo em Inglês | MEDLINE | ID: mdl-9564610

RESUMO

In order to study the putative monoamine oxidase (MAO) inhibitory side effect of neuroleptics and simultaneous changes in platelet serotonin content both MAO-B activity and serotonin (5-HT) content in platelets of 30 healthy volunteers and 50 schizophrenic patients treated with neuroleptics were investigated. Our results have shown significantly lower MAO-B activity (15.26 +/- 6.81 S.D. vs. 8.63 +/- 3.82 mmol/hour/10(9) platelets) and higher platelet 5-HT content (906.19 +/- 285.33 vs. 1,727.85 +/- 947.40 ng/10(9) platelets) in the schizophrenic group. Platelet MAO-B activity was considerably lower in paranoid and residual schizophrenics compared with other patients, however, no difference was found in platelet 5-HT content between different subtypes of schizophrenia. Various neuroleptic treatments did not produce different effects either on platelet serotonin content or platelet MAO-B activity.


Assuntos
Antipsicóticos/uso terapêutico , Plaquetas/metabolismo , Inibidores da Monoaminoxidase/uso terapêutico , Monoaminoxidase/sangue , Esquizofrenia/sangue , Esquizofrenia/tratamento farmacológico , Serotonina/sangue , Plaquetas/efeitos dos fármacos , Clozapina/uso terapêutico , Quimioterapia Combinada , Haloperidol/farmacologia , Humanos , Isoenzimas/sangue , Probabilidade , Valores de Referência
12.
Neurochem Res ; 23(6): 863-8, 1998 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-9572675

RESUMO

This study aimed at determining the effect of drug therapy, age and type of dementia on biological markers. Both platelet monoamine oxidase type B (MAO-B) activity and serotonin content of 57 demented patients and 20 control subjects were determined. Platelet MAO-B activity was measured using [14C]tyramine as substrate. Serotonin content was determined by HPLC-EC method. Increased platelet serotonin content and platelet count was found in patients with dementia compared to controls. A positive correlation was experienced between platelet MAO-B activity, platelet serotonin content and age. Platelet MAO-B activity was higher in the haloperidol treated group, compared with patients treated with anxyolitics. The main original finding of the present study is that platelet serotonin content is increased in demented patients with delusions compared to dementia without complications (p = 0.006). It seems, that platelet MAO-B activity is influenced mainly by drug therapy, while serotonin content rather reflects clinical characteristics in dementia.


Assuntos
Plaquetas/enzimologia , Plaquetas/metabolismo , Demência/sangue , Monoaminoxidase/sangue , Serotonina/sangue , Fatores Etários , Idoso , Idoso de 80 Anos ou mais , Alcoolismo/sangue , Alcoolismo/complicações , Alcoolismo/tratamento farmacológico , Antipsicóticos/uso terapêutico , Biomarcadores/sangue , Plaquetas/efeitos dos fármacos , Delusões/sangue , Delusões/complicações , Delusões/tratamento farmacológico , Demência/complicações , Demência/tratamento farmacológico , Feminino , Humanos , Doença de Huntington/sangue , Doença de Huntington/complicações , Doença de Huntington/tratamento farmacológico , Masculino , Pessoa de Meia-Idade , Doença de Parkinson/sangue , Doença de Parkinson/complicações , Doença de Parkinson/tratamento farmacológico , Contagem de Plaquetas , Fatores Sexuais
13.
Acta Chir Hung ; 37(1-2): 85-93, 1998.
Artigo em Inglês | MEDLINE | ID: mdl-10196616

RESUMO

The performance of ipsilateral mediastinal blockdissection as a routine in every non-small cell lung cancer (NSCLC) operation gives us a chance to judge the accuracy of the preoperative CT examination. The accuracy rate of the CT in our 316 cases was 70.6%, the false positive rate was 69.6%, the false negative rate was 18.2%. Taking into account the 18.2% false negative rate and the slightly better survival of patients operated with routine blockdissection compared to the survival of a group of patients who had mediastinal blockdissection only if suspicion of tumour spread arose, we consider the procedure reasonable in every NSCLC operation.


Assuntos
Carcinoma Pulmonar de Células não Pequenas/cirurgia , Neoplasias Pulmonares/cirurgia , Excisão de Linfonodo , Metástase Linfática/patologia , Adenocarcinoma/diagnóstico por imagem , Adenocarcinoma/secundário , Adenocarcinoma/cirurgia , Carcinoma Pulmonar de Células não Pequenas/diagnóstico por imagem , Carcinoma Pulmonar de Células não Pequenas/secundário , Carcinoma de Células Escamosas/diagnóstico por imagem , Carcinoma de Células Escamosas/secundário , Carcinoma de Células Escamosas/cirurgia , Reações Falso-Negativas , Reações Falso-Positivas , Humanos , Neoplasias Pulmonares/diagnóstico por imagem , Linfonodos/diagnóstico por imagem , Metástase Linfática/diagnóstico por imagem , Mediastino , Planejamento de Assistência ao Paciente , Pneumonectomia , Taxa de Sobrevida , Tomografia Computadorizada por Raios X
14.
Acta Physiol Hung ; 84(4): 403-4, 1996.
Artigo em Inglês | MEDLINE | ID: mdl-9328613

RESUMO

Platelet rich plasma serotonin contents were examined using HPLC-EC method in patients suffering from different anxiety states and compared to age matched healthy controls. We have found significant increase of PRP serotonin level in the group of schizophrenic patients and in patients suffering from dementia compared to controls. PRP serotonin content was significantly lower in heavy drinkers but in patients suffering from panic disorder did not differ significantly from the controls.


Assuntos
Plaquetas/metabolismo , Transtornos Mentais/sangue , Serotonina/sangue , Alcoolismo/sangue , Cromatografia Líquida de Alta Pressão , Demência/sangue , Humanos , Transtorno de Pânico/sangue , Esquizofrenia/sangue
15.
Orv Hetil ; 131(40): 2205-7, 1990 Oct 07.
Artigo em Húngaro | MEDLINE | ID: mdl-2234911

RESUMO

The authors report the case of a young female patient in whose lung they found a hollow, infiltrating lesion characteristic of tuberculosis which was removed by operation. Histologically, the lesion proved to be choriocarcinoma. Elsewhere tumour could not be detected.


Assuntos
Coriocarcinoma/diagnóstico , Neoplasias Pulmonares/diagnóstico , Tuberculose Pulmonar/diagnóstico por imagem , Adulto , Coriocarcinoma/patologia , Diagnóstico Diferencial , Feminino , Humanos , Neoplasias Pulmonares/diagnóstico por imagem , Neoplasias Pulmonares/patologia , Radiografia
18.
J Med Chem ; 27(10): 1253-9, 1984 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-6148420

RESUMO

The weak antiallergic activity of 6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-3-carbox yli c acid (1) in the rat reaginic passive cutaneous anaphylaxis test was enhanced by the introduction of an (arylamino)methylene moiety into position 9 of the pyridopyrimidine ring. Compound 34, (+)-6(S)-methyl-9-[(m-methylphenyl)-hydrazono]-4-oxo-4H-pyrido[1,2 -a] pyrimidine-3-carboxylic acid, displayed about 10 000 times the activity of the starting compound 1. A structure-activity relationship study of 9-[(arylamino)methylene]tetrahydropyridopyrimidine-3-carb ox ylic acids resulted in conclusions similar to those found for the 9-(arylhydrazono)tetrahydro-and 9-(arylamino)dihydropyridopyrimidine series. Replacement of the 3-carboxy group of 9-(phenylhydrazono)-tetrahydropyridopyrimidin-4-ones with an acrylic acid moiety caused slight increases in potency. In the 6-methyl-substituted series, a high stereospecificity was observed between the enantiomers with 6S and 6R absolute configurations, the former being responsible for the antiallergic activity. The effects of some 9-[(arylamino)-methylene]tetrahydropyridopyrimidine-3-car box ylic acids on the rat passive peritoneal anaphylaxis test were also investigated.


Assuntos
Antagonistas dos Receptores Histamínicos H1/síntese química , Pirimidinonas/síntese química , Anafilaxia , Animais , Avaliação Pré-Clínica de Medicamentos/métodos , Feminino , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Masculino , Rotação Ocular , Anafilaxia Cutânea Passiva , Pirimidinonas/farmacologia , Ratos , Ratos Endogâmicos , Relação Estrutura-Atividade
19.
J Med Chem ; 26(10): 1494-9, 1983 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-6137567

RESUMO

The weak antiallergic activity of 6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-3-carboxylic acid (4) on the rat reaginic passive cutaneous anaphylaxis test was enhanced by the introduction of appropriate functional groups into position 9 of the pyridopyrimidine ring. The most active 9-substituted pyridopyrimidinecarboxylic acids contained an oxime, a phenylamino, or a (phenylamino)thioxomethyl group in position 9. The 9-phenylcarboxamido and 9-phenylhydrazono moieties may be regarded as bioisosteric groups in the pyridopyrimidinone series. In the series of 9-(arylamino)dihydropyridopyrimidines, the structure-activity relationship study revealed similar relationships as found for the 9-(arylhydrazono)tetrahydropyridopyrimidines. The biological activity was due to the 6S enantiomers. A monosubstituted arylamino moiety in position 9 was necessary for the intravenous activity. The most active compound, 9-[(3-acetylphenyl)amino]-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H- pyrido[1,2-a]pyrimidine-3-carboxylic acid (40) was three times as active as the reference sodium chromoglycate (DSCG) in the passive cutaneous anaphylaxis (PCA) test.


Assuntos
Antagonistas dos Receptores Histamínicos H1/síntese química , Anafilaxia Cutânea Passiva/efeitos dos fármacos , Pirimidinonas/síntese química , Animais , Avaliação Pré-Clínica de Medicamentos , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Pirimidinonas/uso terapêutico , Ratos , Relação Estrutura-Atividade
20.
J Med Chem ; 26(8): 1126-30, 1983 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-6876080

RESUMO

A series of 9-hydrazono-4H-pyrido[1,2-a]pyrimidin-4-ones was prepared. The compounds were evaluated in the rat passive cutaneous anaphylaxis test for antiallergic activity. Structure-activity relationship studies revealed that the presence of a monosubstituted hydrazone moiety in position 9 and an unsubstituted 2-position are necessary for the intravenous activity.


Assuntos
Hipersensibilidade/tratamento farmacológico , Pirimidinonas/síntese química , Animais , Hidrazonas/síntese química , Hidrazonas/uso terapêutico , Anafilaxia Cutânea Passiva/efeitos dos fármacos , Pirimidinonas/uso terapêutico , Ratos , Relação Estrutura-Atividade
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