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Non-steroidal anti-inflammatory drugs (NSAIDs) act by preventing prostaglandin production. In recent years, research on non-steroid dual inhibitors of prostaglandin and leukotriene biosyntheses has been developed. These compounds should represent a new class of anti-inflammatory drugs, with a wider spectrum of activity than classical NSAIDs. The present paper reports the synthesis of hydrazone derivatives. The effect of various substitutions is studied on platelet cyclooxygenase (i.e. prostaglandin synthesis) and on leukocyte 5-lipoxygenase (i.e. leukotriene synthesis). Among the 50 tested compounds, 2 hydrazone derivatives were selected for their significant dual inhibitory potency: 2-acetylthiophene-2-thiazolylhydrazone 5g, and N-phenyl benzamidrazone 6c.  相似文献   

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Because of metabolic changes due to ageing, malnutrition is accompanied by a preferential loss of fat free mass in the elderly and it exaggerates the physiological loss of body cell mass, muscle mass and muscle function observed in the aged. Exercise training has positive anabolic effects even in the frail elderly and may improve the effect of renutrition in malnourished elderly patients.  相似文献   

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BackgroundIn France, vaccination coverage against seasonal influenza for risk groups was inadequate: 55.2% of people aged 65 and older, and 33% of the16–64 year group with chronic targeted disorders were vaccinated in March 2012. Three quarters of general practitioners were vaccinated. Our objective was to estimate the influence of the vaccination status of general practitioners on vaccine coverage of their patients at risk.MethodsA questionnaire was sent in March 2012 to a sample of 500 general practitioners. Their professional characteristics, vaccination status against seasonal influenza and the determinants of these vaccinations were collected and compared to the vaccine coverage of their patients obtained from the French healthcare fund.ResultsSelf-reported vaccination coverage of the 225 general practitioners respondents was 81.3%. There was a positive correlation with age greater than 50 years, high activity level, rural practice and the absence of particular mode of exercise. The doctors wanted to be vaccinated to protect themselves and protect their patients or their family. Of the 42 doctors unvaccinated, 42.5% feared the side effects of the vaccine, 40% considered influenza to be a benign illness and 32.5% considered low risk of catching or spreading it. The vaccination rate for patients aged 65 and older was 62.3% among 147 doctors vaccinated versus 58.3% in unvaccinated 31 physicians (P < 0.0001). These rates were 39% versus 36.7% (P = 0.29) for patients with chronic targeted disorders.ConclusionThis study shows a positive association between the reported vaccination of general practitioners and effective influenza vaccination of their patients aged 65 years and older. This result is less clear for patients with chronic targeted disorders. All this findings argue in favor of promoting seasonal influenza vaccination among general practitioners.  相似文献   

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Analogs of nipecotic acid, substituted at positions 2, 3, 4, 5, or 6 with a methyl or phenyl group were prepared and their affinities for the GABA transport protein and the GABA receptor sites were measured. The expected beneficial increase in lipophilicity was however counteracted by conformationnal effects (predominance of the inactive conformer presenting an axial carboxylic group) and/or electronic effects (proportion of the zwitterionic population).  相似文献   

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IntroductionTwenty million cases of typhoid and paratyphoid fever (TF) are observed annually worldwide with more than 200,000 deaths. These fevers occur in areas where hygiene is precarious, mainly in developing countries. The objective of this study was to describe epidemiological patterns of TF in Meknes, Morocco in order to improve preventive measures.MethodsWe conducted a case series study based on data from 2013 to 2016 in the Meknes TF surveillance system. Data collected included socio-demographic variables, place of residence, season, mode of water supply, and food consumed. Diagnosis of TF was confirmed with the Widal test. Data were analyzed with Epi-info version 7 and mapping was done with Qgis version 2.18.1.ResultsThree hundred and twenty-two cases were reported with a male/female sex ratio of 0.9. Average age was 26 ± 20 years. Incidence increased from 13 per 100.000 inhabitants in 2013 to 8 per 100.000 inhabitants in 2016. Two hundred and seventy-nine (87%) cases occurred in urban areas and 174 (54%) cases developed in summer. One death was recorded.ConclusionPublic awareness campaigns on health education for hygiene are needed. Focus should be placed on transmission by food handlers.  相似文献   

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