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1.
J Oral Sci ; 62(1): 89-92, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31996531

RESUMO

The oral hygiene and oral status of children with severe disabilities with both nutritional and respiratory complications who were institutionalized at Karugamonoie (KNI), a facility for children with disabilities, were investigated in this study. Their oral hygiene management was solely dependent on caregivers and nurses at the institution. Thirty children (13 females, 17 males; average age, 7.6 years) who had a tracheotomy and feeding tube (gastrostomy, nasogastric, or jejunostomy feeding tube) were included in the study. As for oral characteristics, poor control of tongue movement, anterior open-bite, abnormal strain of facial muscles, dry mouth, and swallowing dysfunction were found in 63.3%, 63.3%, 13.3%, 20.0%, and 100.0%, of the children, respectively. The mean ± standard deviation Decayed, Missing, Filled Teeth score was 0.13 ± 0.57. The Gingival Index (GI) showed that the children had mild (53.3%) to moderate (46.7%) gingivitis. The Simplified Oral Hygiene Index was excellent in 50.0% of the children, good in 23.3%, fair in 20.0%, and poor in 6.7% of the children. These indices were satisfactory in general except for GI management, which may have been hampered by abnormal oral functions and anterior open-bite. In conclusion, oral hygiene management of children with nutritional and respiratory complications at KNI was shown to be of high quality even without on-site intervention by dental specialists.


Assuntos
Cárie Dentária , Deficiência Intelectual , Criança , Criança Institucionalizada , Índice CPO , Feminino , Humanos , Masculino , Saúde Bucal , Higiene Bucal , Índice de Higiene Oral
2.
Anal Sci ; 23(8): 987-92, 2007 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-17690433

RESUMO

This research attempts to establish a method to measure 11 kinds of oxygenated volatile organic compound (OVOC) in ambient air by using the canister collection-gas chromatography/mass spectrometry (GC/MS) method. Since several compounds such as acetone exhibited high blank concentrations due to their laboratory use, stringent quality control was conducted for the VOC-free added water and the VOC-free nitrogen gas. In order to prevent the decline of recovery rates due to lack of sufficient relative humidity, it is necessary to add VOC-free water when pressurizing and diluting the air samples. Thus, all the target compounds in ambient air were obtained from the canisters at high recovery rates without significant contamination. Furthermore, the canister collection-GC/MS method makes it possible to apply simultaneous air monitoring of OVOCs as well as volatile hazardous air pollutants without additional sampling.

3.
Bioorg Med Chem ; 14(17): 5781-94, 2006 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-16762554

RESUMO

Conformationally restricted 3-anilino-4-(3-indolyl)maleimide derivatives were designed and synthesized aiming at discovery of novel protein kinase Cbeta (PKCbeta)-selective inhibitors possessing oral bioavailability. Among them, compounds having a fused five-membered ring at the indole 1,2-position inhibited PKCbeta2 with IC50 of nM-order and showed good oral bioavailability. One of the most potent compounds was found to be PKCbeta-selective over other 6 isozymes and exhibited ameliorative effects in a rat diabetic retinopathy model via oral route.


Assuntos
Maleimidas/química , Maleimidas/farmacologia , Proteína Quinase C/antagonistas & inibidores , Administração Oral , Animais , Disponibilidade Biológica , Diabetes Mellitus Experimental/tratamento farmacológico , Retinopatia Diabética/tratamento farmacológico , Relação Dose-Resposta a Droga , Maleimidas/farmacocinética , Maleimidas/uso terapêutico , Estrutura Molecular , Proteína Quinase C/metabolismo , Proteína Quinase C beta , Ratos , Relação Estrutura-Atividade
4.
J Med Chem ; 48(10): 3586-604, 2005 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-15887966

RESUMO

A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkeys, showed a dose-dependent antithrombotic effect at 0.1, 0.3, and 1 mg kg(-1) h(-1) in a rat model of venous thrombosis, and significantly reduced the size of brain infarction in a middle cerebral artery occlusion model at a dose of 0.1 mg kg(-1) h(-1). These results suggest that compound 2 (JTV-803) is likely to be useful as both a venous and arterial antithrombotic agent.


Assuntos
Inibidores do Fator Xa , Fibrinolíticos/síntese química , Isoquinolinas/síntese química , Piperidinas/síntese química , Piridinas/síntese química , Tetra-Hidroisoquinolinas/síntese química , Administração Oral , Animais , Arteriopatias Oclusivas/complicações , Infarto Encefálico/tratamento farmacológico , Infarto Encefálico/etiologia , Infarto Encefálico/patologia , Doenças Arteriais Cerebrais/complicações , Fator Xa/química , Fibrinolíticos/química , Fibrinolíticos/farmacologia , Humanos , Injeções Intravenosas , Isoquinolinas/química , Isoquinolinas/farmacologia , Macaca fascicularis , Artéria Cerebral Média , Modelos Moleculares , Piperidinas/química , Piperidinas/farmacologia , Piridinas/química , Piridinas/farmacologia , Ratos , Relação Estrutura-Atividade , Tetra-Hidroisoquinolinas/química , Tetra-Hidroisoquinolinas/farmacologia , Trombose Venosa/tratamento farmacológico
5.
Bioorg Med Chem Lett ; 15(1): 185-9, 2005 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-15582437

RESUMO

A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 (JTV-803) exhibited potent inhibitory activity against FXa and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkey, and showed a dose-dependent antithrombotic effect in a rat model of venous thrombosis.


Assuntos
Inibidores do Fator Xa , Inibidores de Serino Proteinase/farmacologia , Tetra-Hidroisoquinolinas/farmacologia , Animais , Ratos , Inibidores de Serino Proteinase/uso terapêutico , Tetra-Hidroisoquinolinas/uso terapêutico , Trombose Venosa/tratamento farmacológico , Trombose Venosa/enzimologia
6.
Nippon Ganka Gakkai Zasshi ; 108(10): 600-5, 2004 Oct.
Artigo em Japonês | MEDLINE | ID: mdl-15559312

RESUMO

OBJECTIVE: To investigate how the increase in survival rate in extremely low birth weight (a birth weight of 1,000 g or less) infants had affected the incidence of retinopathy of prematurity (ROP) and the frequency of laser treatment. METHODS: We retrospectively reviewed the medical records of 122 surviving premature infants with birthweights less than 1,000 g to determine the severity of ROP observed at 16 neonatal intensive care units in Tokyo between April and October 2002. RESULTS: The survival rate was 85.6%. The mean gestational age was 26.74 weeks and the mean birth weight was 782.25 g. One-hundred-and-five infants (86.1%) developed ROP, fifty (41.0%) received laser treatment, and six (4.9%) had retinal detachment. The median postmenstrual age (gestational age at birth plus chronological age in weeks, PMA) at the onset of ROP was 32.5 weeks, and the first laser treatment was performed at the median PMA of 35.7 weeks. CONCLUSIONS: In these extremely low birth weight infants, there was an increase in the survival rate and in the incidence of severe ROP that progressed to the stage that required treatment.


Assuntos
Recém-Nascido de muito Baixo Peso , Retinopatia da Prematuridade/epidemiologia , Peso ao Nascer , Idade Gestacional , Humanos , Incidência , Recém-Nascido , Unidades de Terapia Intensiva Neonatal/estatística & dados numéricos , Terapia a Laser , Retinopatia da Prematuridade/terapia , Estudos Retrospectivos , Taxa de Sobrevida , Fatores de Tempo , Tóquio/epidemiologia
7.
Bioorg Med Chem Lett ; 14(20): 5171-4, 2004 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-15380221

RESUMO

We report herein synthesis of PKCbeta-selective inhibitors possessing the novel pharmacophore of anilino-monoindolylmaleimide. Several compounds of this series exhibited IC50's as low as 50 nM against human PKCbeta2. One of the most potent compounds, 6l, inhibited PKCbeta1 and PKCbeta2 with IC50 of 21 and 5 nM, respectively, and exhibited selectivity of more than 60-fold in favor of PKCbeta2 relative to other PKC isozymes (PKCalpha, PKCgamma, and PKCepsilon).


Assuntos
Compostos de Anilina/síntese química , Indóis/síntese química , Maleimidas/síntese química , Proteína Quinase C/antagonistas & inibidores , Compostos de Anilina/química , Humanos , Indóis/química , Isoenzimas/antagonistas & inibidores , Isoenzimas/química , Maleimidas/química , Proteína Quinase C/química , Proteína Quinase C beta , Relação Estrutura-Atividade
8.
Bioorg Med Chem Lett ; 14(16): 4281-6, 2004 Aug 16.
Artigo em Inglês | MEDLINE | ID: mdl-15261287

RESUMO

A series of benzimidazole derivatives with the side chain on the nitrogen atom oriented to the prime site of factor Xa (FXa) were designed and synthesized. Compounds with substituted aminocarbonylmethyl groups as the side chain showed potent FXa inhibitory activity. Compounds 1 and 2 exhibited most potent inhibitory activity and were effective as anticoagulants in a DIC model.


Assuntos
Benzimidazóis/química , Inibidores do Fator Xa , Inibidores de Serino Proteinase/química , Inibidores de Serino Proteinase/farmacologia , Relação Estrutura-Atividade
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