RESUMO
My Little Smart Personal Assistant is a co-designed remote connected device with an interactive vocal assistant that provides a panel of social/medical services for the rural European elderly population. The aim is to create a new patient-centered solution to improve quality of life, self-autonomy, and integration within local community. This should improve aging-well at home in rural settings.
Assuntos
Envelhecimento , Serviços de Saúde Rural , Idoso , Humanos , Qualidade de Vida , População RuralRESUMO
BACKGROUND/OBJECTIVES: Malnutrition is associated with a high morbi-mortality in elderly populations and their institutionalization at an early stage. The incidence is well known despite being often under-diagnosed in primary care. General practitioners (GPs) have a key role in home care. What are the factors affecting malnutrition-screening implementation by French GPs? SUBJECTS/METHODS: We conducted a cross-sectional survey in two areas in the southeast of France (Savoie and Isère). In May 2008, an anonymized survey was sent by e-mail and/or post to all GPs with a large clinical practice. Two months later, reminder letters were sent. Potential barriers were measured by dichotomous scale. On GPs' characteristics (socio-demographic, medical training, geriatric practice and knowledge), multiple regression logistic was performed to identify others factors affecting malnutrition screening. RESULTS: In all, 493 GPs (26.85%) answered and 72.2% felt that malnutrition screening was useful although only 26.6% implemented it each year and 11.9% every 2-5 years. The main barriers to the implementation were patient selection (60.4%) and forgetting to screen (26.6%). Minor barriers were lack of knowledge (19.5%) or time (15%). New factors were identified: unsuitable working conditions (19.1%), insufficient motivation (6.8%) or technical support (7.2%). The quality of malnutrition information received was found to be the only promoter of annual screening (odds ratio=1.44 (1.087-1.919); P=0.011). CONCLUSIONS: This survey is the first in France to reveal GPs' factors affecting malnutrition implementation. New obstacles were identified in this survey. The hope of implementing regular malnutrition screening by GPs seems to lie with the quality of malnutrition information received.
Assuntos
Medicina Geral , Avaliação Geriátrica , Desnutrição/diagnóstico , Programas de Rastreamento , Avaliação Nutricional , Estado Nutricional , Padrões de Prática Médica , Idoso , Atitude do Pessoal de Saúde , Competência Clínica , Estudos Transversais , Feminino , França , Clínicos Gerais , Pesquisas sobre Atenção à Saúde , Humanos , Modelos Logísticos , Masculino , Memória , Motivação , Razão de ChancesRESUMO
A series of novel 7-substituted-1-tert-butyl-6-fluoronaphthyridone-3- carboxylic acids has been prepared. These derivatives are characterized by chiral aminopyrrolidine substituents at the 7 position. In this paper we report the full details of the asymmetric synthesis of this series of compounds. Structure-activity relationship studies indicate that the absolute stereochemistry at the asymmetric centers of the pyrrolidine ring is critical for maintaining good activity. Compounds 60 and 61 (3-amino-4-methylpyrrolidine enantiomers) were selected for preclinical evaluation.
Assuntos
Antibacterianos/síntese química , Naftiridinas/síntese química , Animais , Antibacterianos/farmacocinética , Antibacterianos/farmacologia , Cães , Feminino , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Naftiridinas/farmacocinética , Naftiridinas/farmacologia , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
A series of novel chiral 7-(1-, 3-, 4-, and 6-methyl-[(1R,4R)-2,5- diazabicyclo[2.2.1]heptan-2-yl]-substituted naphthyridines has been prepared with the aim of obtaining good in vitro and in vivo antibacterial agents with a decrease of the pseudoallergic type reaction when compared to that observed with 7[(1R,4R)-2,5-diazabicyclo[2.2.1]heptan-2-yl]-1-(1,1-dimethylethyl )1,4- dihydro-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid (1a) (BMY 40062). The derivatives 7-[(1R,4R,6S)-6-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]- 1-(1,1-dimethylethyl)-6-fluro-1,4-dihydro-4-oxo-1,8-naphthyridine- 3-carboxylic acid (41) and 7-[(1R,4R,6S)-6-methyl-2,5-diazabicyclo[2.2.1]heptan-2- yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxy lic acid (49) showed potent in vitro and in vivo antibacterial activity against Gram-positive and Gram-negative bacteria. The derivative 49 displayed a less marked decrease in blood pressure (MAP), compared to that of 1a, after intravenous infusion in dogs and was selected as a potential candidate for preclinical trials.
Assuntos
Anti-Infecciosos/síntese química , Pressão Sanguínea/efeitos dos fármacos , Fluoroquinolonas , Naftiridinas/farmacologia , Quinolonas/farmacologia , Animais , Anti-Infecciosos/farmacocinética , Anti-Infecciosos/farmacologia , Cães , Feminino , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Masculino , Camundongos , Naftiridinas/química , Naftiridinas/farmacocinética , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
A series of 5-substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8- naphthyridine-3-carboxylic acids have been prepared and tested for their in vitro and in vivo antibacterial activities. The 5-methyl group gave better in vitro activity with the 1-cyclopropyl appendage, but poorer activity with the 1-tert-butyl moiety. With the 1-(2,4-difluorophenyl) substitution, the influence of the 7-cycloalkylamino group was determinant: a (3S)-3-amino-pyrrolidine was shown to enhance greatly the in vitro and in vivo activity of the 5-methyl derivative. Compound 33 (BMY 43748) was selected as a promising candidate for an improved therapeutic agent.
Assuntos
Antibacterianos/síntese química , Bactérias/efeitos dos fármacos , Naftiridinas/síntese química , Animais , Antibacterianos/farmacocinética , Antibacterianos/farmacologia , Camundongos , Naftiridinas/farmacocinética , Naftiridinas/farmacologia , Relação Estrutura-AtividadeRESUMO
A series of novel N-1-(mono-,-(di- and -(trifluoro-tert-butyl)quinolones and -naphthyridines has been prepared. Structure-activity relationship (SAR) studies indicated that the in vitro antibacterial potency was the following order: 1-(1,1-dimethyl-2-fluoroethyl) greater than 1-[1-methyl-1-(fluoromethyl)-2-fluoroethyl] greater than 1-[1,1-(difluoromethyl)-2-fluoroethyl] substituents. In the quinolone series the monofluoro-tert-butyl derivatives were found to possess better in vitro antibacterial activity than the nonfluorinated-tert-butyl equivalents. In vivo PD50 values of the 1-fluoro-tert-butyl-substituted derivatives reflect pharmacokinetic behavior and incomplete oral absorption.
Assuntos
Anti-Infecciosos/síntese química , Naftiridinas/síntese química , 4-Quinolonas , Animais , Anti-Infecciosos/farmacocinética , Anti-Infecciosos/uso terapêutico , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Cães , Indicadores e Reagentes , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Naftiridinas/farmacologia , Naftiridinas/uso terapêutico , Relação Estrutura-AtividadeRESUMO
A number of 7-substituted-1-tert-butyl-6-fluoroquinolone-3-carboxylic acids and 7-substituted-1-tert-butyl-6-fluoro-1,8-naphthyridine-3-carboxylic acids have been prepared and tested for antibacterial activities. Among those the 7-aminopyrrolidinyl 20b and the 7-diazabicyclo naphthyridine 18b are the most potent compounds in vitro and in vivo. Physicochemical data and acute toxicity are also discussed. Compound 18b, BMY 40062, exhibits the most favorable overall properties, considering in vitro and in vivo microbiological activity, its low toxicity, and pharmacokinetic profile, and was selected for clinical evaluation.
Assuntos
Anti-Infecciosos/síntese química , Fluoroquinolonas , Naftiridinas , 4-Quinolonas , Animais , Anti-Infecciosos/farmacocinética , Anti-Infecciosos/farmacologia , Fenômenos Químicos , Química , Cães , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Taxa de Depuração Metabólica , Camundongos , Testes de Sensibilidade Microbiana , Relação Estrutura-AtividadeRESUMO
A series of novel 7-piperazinyl-1-substituted-6-fluoroquinolones and naphthyridines have been prepared and their antibacterial activities evaluated. These derivatives are characterized by having alkyl, alkenyl, arylalkyl, cycloalkyl, and cycloalkenyl groups at the 1-position. As a result of this study, derivatives 7 and 26, which are substituted with tert-butyl groups at N-1, were found to possess excellent in vitro and in vivo potency, particularly against Staphylococcus aureus, comparable to that of norfloxacin or ciprofloxacin. Structure-activity relationships of N-1 substituted alkyls and cycloalkyls are also discussed.
Assuntos
Antibacterianos/síntese química , Naftiridinas/síntese química , 4-Quinolonas , Animais , Antibacterianos/farmacologia , Fenômenos Químicos , Química , Cães , Bactérias Gram-Negativas/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Naftiridinas/farmacologia , Staphylococcus/efeitos dos fármacos , Relação Estrutura-AtividadeRESUMO
Using about 100 blood samples of dairy goats selected for their high level of milk production, the authors determined the enzymic activities of CPK, LDH, ICDH and SDH. The limits of the practical values of these parameters are (expressed in IU/l): CPK: 14-62; LDH pregnancy: 217-417, lactation: 300-586; ICDH: 2.3-14.8; SDH: 2.6-11.6.