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1.
Polymers (Basel) ; 11(9)2019 Sep 06.
Artículo en Inglés | MEDLINE | ID: mdl-31500164

RESUMEN

A novel (E)-5-(2-(5-alkylthiothiophen-2-yl)vinyl)thien-2-yl (TVT)-comprising benzo[1,2-b:4,5-b']dithiophene (BDT) derivative (BDT-TVT) was designed and synthetized to compose two donor-acceptor (D-A) typed copolymers (PBDT-TVT-ID and PBDT-TVT-DTNT) with the electron-withdrawing unit isoindigo (ID) and naphtho[1,2-c:5,6-c']bis[1,2,5]thiadiazole (NT), respectively. PBDT-TVT-ID and PBDT-TVT-DTNT showed good thermal stability (360 °C), an absorption spectrum from 300 nm to 760 nm and a relatively low lying energy level of Highest Occupied Molecular Orbital (EHOMO) (-5.36 to -5.45 eV), which could obtain a large open-circuit voltage (Voc) from photovoltaic devices with PBDT-TVT-ID or PBDT-TVT-DTNT. The photovoltaic devices with ITO/PFN/polymers: PC71BM/MoO3/Ag structure were assembled and exhibited a good photovoltaic performance with a power conversion efficiency (PCE) of 4.09% (PBDT-TVT-ID) and 5.44% (PBDT-TVT-DTNT), respectively. The best PCE of a PBDT-TVT-DTNT/PC71BM-based device mainly originated from its wider absorption, higher hole mobility and favorable photoactive layer morphology.

2.
Eur J Med Chem ; 180: 509-523, 2019 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-31336309

RESUMEN

A series of novel xanthine derivatives 2a-l incorporating benzoic acid moieties were rapidly generated by using strategy of scaffold-hopping from our previously reported scaffold uracil to xanthine, a scaffold of approved drug linagliptin. After systematic structure-activity relationship (SAR) study around benzoic acid moieties, 5 novel DPP-4 inhibitors with low picomolar potency range (IC50 < 1 nM) and excellent selectivity against various DPP-4 homologues were identified, in which the best one, compound 2f, with the IC50 value of 0.1 nM for DPP-4, showed 22-fold improvement in inhibitory activity compared to lead compound uracil 1, its activity was 45-fold more potent than alogliptin. 2e, 2f, 2i and 2k were selected for pharmacokinetic evaluation, and 2f and 2i showed the better pharmacokinetic profiles after iv administration, but poor oral bioavailability. To improve the oral pharmacokinetic profile, prodrug design approach was performed around 2f and 2i. Esters of 2f and 2i were synthesized and evaluated for stability, toxicity and pharmacokinetics. Compound 3e, the methyl ester of compound 2f, was identified to demonstrate good stability, low toxicity and improved oral bioavailability, with 3-fold higher blood concentration compared to 2f in rats. The following in vivo evaluations revealed 3e provided a sustained pharmacodynamics effect for 48h, and robustly improved glucose tolerance in normal ICR and db/db mice in dose-dependent manner. Chronic treatments investigations demonstrated that 3e achieved more beneficial effects on fasting blood glucose levels and glucose tolerance than alogliptin in type 2 diabetic db/db mice. The overall results have shown that compound 3e has the potential to efficacious, safety and long-acting treatment for T2DM.


Asunto(s)
Ácido Benzoico/farmacología , Dipeptidil Peptidasa 4/metabolismo , Inhibidores de la Dipeptidil-Peptidasa IV/farmacología , Hipoglucemiantes/farmacología , Profármacos/farmacología , Xantina/farmacología , Animales , Ácido Benzoico/química , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Inhibidores de la Dipeptidil-Peptidasa IV/síntesis química , Inhibidores de la Dipeptidil-Peptidasa IV/química , Relación Dosis-Respuesta a Droga , Humanos , Hipoglucemiantes/síntesis química , Hipoglucemiantes/química , Masculino , Ratones , Ratones Endogámicos C57BL , Ratones Endogámicos ICR , Modelos Moleculares , Estructura Molecular , Profármacos/síntesis química , Profármacos/química , Relación Estructura-Actividad , Xantina/síntesis química , Xantina/química
3.
Polymers (Basel) ; 10(7)2018 Jun 25.
Artículo en Inglés | MEDLINE | ID: mdl-30960628

RESUMEN

In recent years, ternary organic photovoltaic cells (OPVs) have been dedicated to improving power conversion efficiency (PCE) by broadening optical absorption spectra. Ternary OPVs with different poly[thieno[3,2-b]thiophene-2,5-diyl-alt-4,9-bis(4-(2-decyltetradecyl)thien-2-yl)naphtho[1,2-c:5,6-c']bis[1,2,5]thiadiazole-5,5'-diyl] (PTT-DTNT-DT) doping concentrations were designed and the effect of PTT-DTNT-DT as a complementary electron donor on the performance of OPVs was investigated. The optimized PCE of OPVs was increased from 3.42% to 4.66% by doping 20 wt % PTT-DTNT-DT. The remarkable improvement in the performance of the ternary device is mainly attributed to the sharp increase in the short-circuit current density and fill-factor. The major reasons have been systematically studied from atomic force microscopy, electrochemical impedance spectroscopy, surface energy, space charge limited current and photocurrent behavior. It has been found that the separation of excitons and the transportation of charge are enhanced while light absorption is increased, and the charge recombination also decreases due to the optimization of the cascade energy level and the morphology of the ternary active layer. The results show that it is feasible to improve the performance of ternary OPVs by their complementary absorption.

4.
Neurorehabil Neural Repair ; 27(8): 684-94, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-23757295

RESUMEN

BACKGROUND: Neurologic music therapy has demonstrated improved walking performance in persons with neurologic disease; however, little evidence supports the use of music with functional resistance exercise to improve motor capacity and daily functions for children with cerebral palsy. OBJECTIVE: To investigate the effect of additional patterned sensory enhancement (PSE) music combined with exercise for children with spastic diplegia. METHODS: An assessor-blind, randomized controlled trial with 6- and 12-week follow-ups was carried out. Thirty-six children with spastic diplegia, aged 5 to 13 years, were assigned to a PSE group (n = 18) or a no-music group (n = 18). Both groups received 6-week, home-based, loaded sit-to-stand exercise, but only the PSE group exercised with prerecorded PSE music. The primary outcome was Gross Motor Function Measure (GMFM). Secondary outcomes included Pediatric Evaluation of Disability Inventory (PEDI) mobility and self-care domains, 1-repetition maximum of sit-to-stand, and walking speeds. RESULTS: Three children did not complete the program. Intention-to-treat analysis showed both groups improved in GMFM D, E, and Goal dimensions; Functional Skills Scales of PEDI mobility domain; and 1-repetition maximum of sit-to-stand at posttest and follow-ups (P ≤ .005). The PSE group improved significantly greater than the no-music group in the GMFM D and Goal dimensions (P < .005) after training, and the improvement persisted for at least 6 or 12 weeks (P ≤ .013). No significant improvements in the rest PEDI scales and walking speeds were found. CONCLUSIONS: Adding neurologic music therapy to functional resistance exercise could induce greater improvements in gross motor capacity for children with cerebral palsy.


Asunto(s)
Parálisis Cerebral/rehabilitación , Musicoterapia , Entrenamiento de Fuerza , Caminata/fisiología , Adolescente , Niño , Preescolar , Femenino , Visita Domiciliaria , Humanos , Masculino
5.
Clin Rehabil ; 26(7): 664-71, 2012 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-22080526

RESUMEN

UNLABELLED: OBJECTIVE To investigate the psychometric properties of the five-repetition sit-to-stand test, a functional strength test, in children with spastic diplegia. DESIGN: Methodology study. SETTINGS: Hospital, laboratory or home. PARTICIPANTS: In total, 108 children with spastic diplegia and 62 with typical development aged from five to 12 years were tested. For test-retest reliability, 22 children with spastic diplegia were tested twice within one week. INTERVENTIONS: Not applicable. MAIN MEASURES: The five-repetition sit-to-stand test measures time needed to complete five consecutive sit-to-stand cycles as quickly as possible. The higher the rate of five-repetition sit-to-stand (repetitions per second), the more strength a person has. RESULTS: The intraclass correlation coefficients of intra-session reliability and test-retest reliability were 0.95 and 0.99 respectively. The minimal detectable difference was 0.06 rep/sec. The convergent validity of the five-repetition sit-to-stand test was supported by significant correlation with one-repetition maximum of the loaded sit-to-stand test, isometric muscle strength, scores of Gross Motor Function Measure, and gait function (r or rho = 0.40-0.78). For known group validity, children with typical development and children classified as Gross Motor Function Classification System level I performed higher rates of five-repetition sit-to-stand than children classified as level II, and children classified as level II performed higher rates than level III. CONCLUSION: The five-repetition sit-to-stand test was a reliable and valid test to measure functional muscle strength in children with spastic diplegia in clinics.


Asunto(s)
Parálisis Cerebral/fisiopatología , Extremidad Inferior/fisiología , Fuerza Muscular/fisiología , Estudios de Casos y Controles , Niño , Preescolar , Femenino , Humanos , Contracción Isométrica , Masculino , Músculo Esquelético/fisiología , Psicometría , Reproducibilidad de los Resultados , Estudios Retrospectivos
6.
Gait Posture ; 33(2): 274-8, 2011 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-21185725

RESUMEN

The effects of patterned sensory enhancement (PSE) music on muscle power and movement control in children with spastic diplegia (SD) during loaded sit-to-stand (LSTS) were investigated. Twenty-three children with SD aged 5 to 12 years were recruited. Individualized PSE was composed by a music therapist based on each subject's sit-to-stand (STS) movement with 50% 1-repetition maximum load. Each subject performed LSTS continuously for eight repetitions under randomly assigned music or no-music (Control) conditions while the kinematic and kinetic data were measured simultaneously. For the music condition, PSE music was played only during the first five repetitions (PSE condition), and the following three repetitions were referred to as the Continuation condition. Paired t- or Wilcoxon signed rank tests were used to compare the variables between the PSE and Control conditions, and between the Continuation and Control conditions. Compared to the Control condition, greater peak knee extensor power (P=0.009), greater total extensor power (P=0.015), and better center-of-mass smoothness (P=0.01), but less movement time (P=0.003) were found in the PSE condition. Significant effects of the PSE music on the above variables were also found for Continuation condition. The current results showed that individualized PSE music helped improve the performance of LSTS in children with SD. The associated biomechanical features also continued to exist in subsequent movement cycles after the music had ceased. These findings suggest that therapy using LSTS combined with PSE music may be beneficial for rehabilitating children with SD.


Asunto(s)
Parálisis Cerebral/terapia , Movimiento/fisiología , Musicoterapia , Fenómenos Biomecánicos , Parálisis Cerebral/fisiopatología , Niño , Preescolar , Femenino , Humanos , Masculino , Músculo Esquelético/fisiopatología
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