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1.
Int J Biol Macromol ; 254(Pt 1): 127701, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37907179

RESUMO

3D-printing provides a feasible technique for realizing new materials into structural and intelligent parts. In this work, biomass furan-based polyesters poly (ethylene furanoate) (PEF), poly (trimethylene furanoate) (PTF), and poly (butylene furanoate) (PBF) were successfully synthesized in a 5 L reactor through the melt polycondensation process and fabricated into 3D-printing feedstocks. It was demonstrated that the three furan-based polyesters were additively-manufactured into complicated structures. Besides, the mechanical and thermal properties of furan-based polyesters could be tailored by the chain length of diol monomer. The mechanical performance of 3D-printed PEF, PTF and PBF were characterized and compared with commercial filaments. The tensile strength of PEF and PTF could reach 74.6 and 63.8 MPa respectively, which exhibited superior tensile property to poly(ether-ether-ketone) (PEEK), polyamide (PA) and polylactic acid (PLA). Meanwhile, the compression results demonstrated that the PEF and PTF possessed comparable energy absorption capacity with PEEK and PLA respectively, which indicated excellent mechanical properties of furan-based polyesters. It was interesting to find that the 3D-printed structures including solid cube, bionic flower and lattice structures were employed to prove that the PTF possessed excellent shape memory properties. Therefore, the proposed biomass furan-based polymers would offer more freedom in the field of 3D-printing.


Assuntos
Poliésteres , Polímeros , Biomassa , Éteres , Impressão Tridimensional
2.
Huan Jing Ke Xue ; 44(6): 3301-3308, 2023 Jun 08.
Artigo em Chinês | MEDLINE | ID: mdl-37309948

RESUMO

Urban domestic sewage is one of the important nitrate (NO-3) sources for surface water; however, their NO-3 concentrations and nitrogen and oxygen isotope values (δ15N-NO-3 and δ18O-NO-3) remain unclear, and the factors affecting NO-3 concentrations and δ15N-NO-3 and δ18O-NO-3 values of effluents in the waste water treatment plant (WWTP) are still unknown. Water samples in the Jiaozuo WWTP were collected to illustrate this question. Influents, clarified water in the secondary sedimentation tank (SST), and effluents of the WWTP were sampled every 8 h. The ammonia (NH+4) concentrations, NO-3 concentrations, and δ15N-NO-3 and δ18O-NO-3 values were analyzed to elucidate the nitrogen transfers through different treatment sections and illustrate the factors affecting the effluent NO-3 concentrations and isotope ratios. The results indicated that ① the mean NH+4 concentration was (22.86±2.16) mg·L-1 in the influent and decreased to (3.78±1.98) mg·L-1 in the SST and continuously reduced to (2.70±1.98) mg·L-1 in the effluent of the WWTP. The median NO-3 concentration was 0.62 mg·L-1 in the influent, and the average NO-3 concentration increased to (33.48±3.10) mg·L-1 in the SST and gradually increased to (37.20±4.34) mg·L-1 in the effluent of the WWTP. ② The mean values of δ15N-NO-3 and δ18O-NO-3 were (17.1±10.7)‰ and (19.2±2.2)‰ in the influent of the WWTP, the median values of δ15N-NO-3 and δ18O-NO-3 were 11.9‰ and 6.4‰ in the SST, and the average values were (12.6±1.9)‰ and (5.7±0.8)‰ in the effluent of the WWTP. ③ The NH+4 concentrations of influent had significant differences compared to those in the SST and the effluent (P<0.05). The reduction of NH+4 concentrations in the SST was due to the above nitrification during the aerobic treatment process, which transferred NH+4 to NO-3. The NH+4 concentrations in the SST had no significant differences with that in the effluent of the WWTP (P>0.05). ④ The NO-3 concentrations in the influent had significant differences with those in the SST and the effluent (P<0.05), and minor NO-3 concentrations but relatively high δ15N-NO-3 and δ18O-NO-3 values in the influent were probably due to denitrification during the pipe sewage transportation. The obviously increased NO-3 concentrations (P<0.05) but decreased δ18O-NO-3 values (P<0.05) in the SST and the effluent resulted from water oxygen incorporation during the nitrification. The above results confirmed the impacts of aerobic and anaerobic treatment processes on NO-3 concentrations and isotope ratios of effluent from the WWTP and provided scientific basis for the identification of sewage contributions to surface water nitrate via average δ15N-NO-3 and δ18O-NO-3 values.

3.
J Pers Med ; 12(11)2022 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-36579535

RESUMO

(1) Background: Laparoscopic sleeve gastrectomy (LSG) is widely performed in bariatric surgery. However, the prevalence and risk factors of gastroesophageal reflux disease (GERD) symptoms after LSG remain unclear to date. This study aimed to identify risk factors of GERD after LSG. (2) Methods: We conducted a retrospective study at Linkou Chang Gung Memorial Hospital and reviewed 296 patients who underwent LSG from 2016 to 2019. A total of 143 patients who underwent preoperative esophagogastroduodenoscopy and completed the 12-month postoperative follow-up were enrolled. Patients' demographic data, comorbidities, and postoperative weight loss results were recorded for analysis. The GerdQ questionnaire was used to assess GERD after LSG. (3) Results: There were eight surgical complications (5.6%) among the 143 studied patients (median age, 36 years; 56 (39.2%) men; median body weight 105.5 kg; median body mass index [BMI], 38.5 kg/m2). Twenty-three patients (16.1%) developed de novo GERD symptoms. GERD was significantly associated with older age (p = 0.022) and lower BMI (<35 kg/m2, p = 0.028). In multiple logistic regression analysis, age and BMI were significantly associated with GERD. (4) Conclusions: LSG is a safe and effective weight loss surgery. In our study, it led to 16.1% of de novo GERD symptoms, which were significantly related to older age and lower BMI (<35 kg/m2).

4.
Sensors (Basel) ; 22(1)2021 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-35009843

RESUMO

On-line fatigue crack evaluation is crucial for ensuring the structural safety and reducing the maintenance costs of safety-critical systems. Among structural health monitoring (SHM), guided wave (GW)-based SHM has been deemed as one of the most promising techniques. However, the traditional damage index-based method and machine learning methods require manual processing and selection of GW features, which depend highly on expert knowledge and are easily affected by complicated uncertainties. Therefore, this paper proposes a fatigue crack evaluation framework with the GW-convolutional neural network (CNN) ensemble and differential wavelet spectrogram. The differential time-frequency spectrogram between the baseline signal and the monitoring signal is processed as the CNN input with the complex Gaussian wavelet transform. Then, an ensemble of CNNs is trained to jointly determine the crack length. Real fatigue tests on complex lap joint structures were carried out to validate the proposed method, in which several structures were tested preliminarily for collecting the training dataset and a new structure was adopted for testing. The root mean square error of the training dataset is 1.4 mm. Besides, the root mean square error of the evaluated crack length in the testing lap joint structure was 1.7 mm, showing the effectiveness of the proposed method.


Assuntos
Aprendizado de Máquina , Redes Neurais de Computação , Distribuição Normal , Análise de Ondaletas
5.
Biotechnol Biofuels ; 13: 117, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32636923

RESUMO

BACKGROUND: Mannitol is a C(6) polyol that is used in the food and medical sector as a sweetener and antioxidant, respectively. The sustainable production of mannitol, especially via the direct conversion of CO2 by photosynthetic cyanobacteria, has become increasingly appealing. However, previous work aiming to achieve mannitol production in the marine Synechococcus sp. PCC7002 via heterologous expression of mannitol-1-phosphate-5-dehydrogenase (mtlD) and mannitol-1-phosphatase (m1p, in short: a 'mannitol cassette'), proved to be genetically unstable. In this study, we aim to overcome this genetic instability by conceiving a strategy to stabilize mannitol production using Synechocystis sp. PCC6803 as a model cyanobacterium. RESULTS: Here, we explore the stabilizing effect that mannitol production may have on cells faced with osmotic stress, in the freshwater cyanobacterium Synechocystis sp. PCC6803. We first validated that mannitol can function as a compatible solute in Synechocystis sp. PCC6803, and in derivative strains in which the ability to produce one or both of the native compatible solutes was impaired. Wild-type Synechocystis, complemented with a mannitol cassette, indeed showed increased salt tolerance, which was even more evident in Synechocystis strains in which the ability to synthesize the endogenous compatible solutes was impaired. Next we tested the genetic stability of all these strains with respect to their mannitol productivity, with and without salt stress, during prolonged turbidostat cultivations. The obtained results show that mannitol production under salt stress conditions in the Synechocystis strain that cannot synthesize its endogenous compatible solutes is remarkably stable, while the control strain completely loses this ability in only 6 days. DNA sequencing results of the control groups that lost the ability to synthesize mannitol revealed that multiple types of mutation occurred in the mtlD gene that can explain the disruption of mannitol production. CONCLUSIONS: Mannitol production in freshwater Synechocsytis sp. PCC6803 confers it with increased salt tolerance. Under this strategy, genetically instability which was the major challenge for mannitol production in cyanobacteria is tackled. This paper marks the first report of utilization of the response to salt stress as a factor that can increase the stability of mannitol production in a cyanobacterial cell factory.

6.
Opt Express ; 25(18): 21342-21348, 2017 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-29041433

RESUMO

We theoretically investigate the dipolar whispering-gallery modes (WGMs) with different mode orders supported by spherical hyperbolic metamaterial (HMM) cavities consisting of alternating metal and dielectric layers. Associated with the excitations of the WGMs with the highest and the second highest mode orders, the HMM cavities are capable of creating highly enhanced and uniformly distributed local fields in the entire dielectric core region. Variation on the metal filling ratio allows for easily tuning the resonant wavelengths of WGMs over a wide spectral range. By integrating a nonlinear nanocrystal into the HMM cavities, we show enhancements of intensity of second harmonic generation up to a factor of 3.9 × 1010, which is two orders of magnitude higher than the largest enhancement achieved in the single-layer plasmonic core-shell cavities.

7.
Sci Rep ; 7(1): 32, 2017 02 17.
Artigo em Inglês | MEDLINE | ID: mdl-28196968

RESUMO

We theoretically investigate light absorption by a graphene monolayer that is coated on the outside of dielectric-metal core-shell resonators (DMCSRs). We demonstrate that light absorption of graphene can be greatly enhanced in such multi-layered core-shell architectures as a result of the excitation of the hybridized bonding plasmon resonance supported by the DMCSRs. We also demonstrate that the absorption enhancement in graphene can be easily tuned over a wide range from the visible to the near-infrared, and particularly the enhancement factor can be optimally maximized at any selective wavelength, by simultaneously varying the dielectric core size and the metal shell thickness. Our results suggest that the graphene-wrapped DMCSRs with strong and highly wavelength-tunable absorption enhancement in graphene could be attractive candidates for applications in graphene-based photodetectors and image sensors.

8.
Opt Express ; 25(2): 1495-1504, 2017 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-28158030

RESUMO

We theoretically investigate the coupling between molecular excitons and dipolar Fano-like cavity plasmon resonance in two-layered core-shell resonators consisting of a dielectric core with high refractive index and a thin metal outer shell gapped by a low refractive index thin dielectric layer containing molecules. We demonstrate that associated with the excitation of the dipolar Fano-like cavity plasmon, the electric fields can be highly localized within the dielectric gap shell, leading to very small mode volumes. By using the three-oscillator temporal coupled model to describe the proposed plasmon-exciton system, we are able to demonstrate that the coupling between molecular excitons and cavity plasmon resonance can reach the strong coupling regime. Furthermore, we also demonstrate that reducing the thickness or the refractive index of the dielectric gap shell layer can result in further compression of the mode volumes, and consequently decrease the minimum number of the coupled excitons that are required to fulfill the criteria for strong coupling.

9.
Sci Rep ; 6: 33628, 2016 09 19.
Artigo em Inglês | MEDLINE | ID: mdl-27641709

RESUMO

The effects of cabbage waste (CW) addition on methane production in cow dung and corn straw co-fermentation systems were investigated. Four experimental groups, each containing 55 g of substrate, were set up as follows: 100% cow dung (C); 36% cabbage and 64% cow dung (CC); 36% straw and 64% cow dung (SC); and 18% cabbage, 18% straw, and 64% cow dung (CSC). After seven days of fermentation, the maximum methane yield was 134 mL in the CSC group, which was 2.81-fold, 1.78-fold, and 1340-fold higher than that obtained in the CC, SC, and C groups, respectively. CW treatment of the CSC group enhanced cellulase activity and enriched culturable cellulose-degrading bacterial strains. Miseq sequencing data revealed that the predominant phylum in the CSC group was Bacteroidetes, which contains most of the cellulose-degrading bacteria. Our results suggested that CW treatment elevated cellulose degradation and promoted methane production.


Assuntos
Brassica , Celulose , Fermentação , Metano/biossíntese , Resíduos , Zea mays , Anaerobiose , Animais , Bactérias/classificação , Bactérias/genética , Bactérias/metabolismo , Biodegradação Ambiental , Biodiversidade , Bovinos , Celulase/metabolismo , Fatores de Tempo
10.
Nanoscale ; 8(19): 10358-63, 2016 May 21.
Artigo em Inglês | MEDLINE | ID: mdl-27139034

RESUMO

Fano resonances have been realized in plasmonic systems and have found intriguing applications, in which, however, precisely controlled symmetry breaking or particular arrangement of multiple constituents is usually involved. Although simple core-shell type architectures composed of a spherical dielectric core and a concentric metallic shell layer have been proposed as good candidates that support inherent Fano resonances, these theoretical predictions have rarely seen any detailed experimental investigation. Here, we report on the experimental investigation of the magnetic and electric-based multipolar plasmonic Fano resonances in the dielectric-metal core-shell resonators that are formed by wrapping a nearly perfect metal shell layer around a dielectric sphere. We demonstrate that these Fano resonances originate from the interference between the Mie cavity and sphere plasmon resonances. Moreover, we present that the variation on either the dielectric core size or core refractive index allows for easily tuning the observed Fano resonances over a wide spectral range. Our findings are supported by excellent agreement with analytical calculations, and offer unprecedented opportunities for realizing ultrasensitive bio-sensors, lasing and nonlinear optical devices.

11.
Ecotoxicology ; 25(1): 234-47, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26589947

RESUMO

Strain LZ-C, isolated from a petrochemical wastewater discharge site, was found to be resistant to heavy metals and to degrade various aromatic compounds, including naphenol, naphthalene, 2-methylnaphthalene and toluene. Data obtained from 16S rRNA gene sequencing showed that this strain was closely related to Delftia lacustris. The 5,889,360 bp genome of strain LZ-C was assembled into 239 contigs and 197 scaffolds containing 5855 predicted open reading frames (ORFs). Among these predicted ORFs, 464 were different from the type strain of Delftia. The minimal inhibitory concentrations were 4 mM, 30 µM, 2 mM and 1 mM for Cr(VI), Hg(II), Cd(II) and Pb(II), respectively. Both genome sequencing and quantitative real-time PCR data revealed that genes related to Chr, Czc and Mer family genes play important roles in heavy metal resistance in strain LZ-C. In addition, the Na(+)/H(+) antiporter NhaA is important for adaptation to high salinity resistance (2.5 M NaCl). The complete pathways of benzene and benzoate degradation were identified through KEGG analysis. Interestingly, strain LZ-C also degrades naphthalene but lacks the key naphthalene degradation gene NahA. Thus, we propose that strain LZ-C exhibits a novel protein with a function similar to NahA. This study is the first to reveal the mechanisms of heavy metal resistance and salinity tolerance in D. lacustris and to identify a potential 2-methylnaphthalene degradation protein in this strain. Through whole-genome sequencing analysis, strain LZ-C might be a good candidate for the bioremediation of heavy metals and polycyclic aromatic hydrocarbons.


Assuntos
Delftia/genética , Delftia/metabolismo , Genoma Bacteriano , Metais Pesados/metabolismo , Hidrocarbonetos Policíclicos Aromáticos/metabolismo , Poluentes do Solo/metabolismo , China , Reação em Cadeia da Polimerase em Tempo Real , Análise de Sequência de DNA
12.
Sci Rep ; 5: 12491, 2015 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-26282896

RESUMO

Efficient control of optical radiation at subwavelength scales plays important roles for various applications. Dielectric nanoparticles or dielectric shells with a large refractive index of n ~ 3-4, which are only achievable for limited semiconductors, are involved in most designs so far to control the scattering by overlapping the electric and magnetic dipolar modes of the same magnitude. Here we propose a new mechanism based on the interplay between dipolar and quadrupolar resonances of different amplitudes, both magnetic and electric, to suppress the backward scattering or the forward scattering by using metallo-dielectric core-shell nanoparticles with a dielectric shell layer having a refractive index of n = 2.0. We demonstrate that broadband zero-backward or near-zero-forward scattering can be achieved by optimizing the structural parameters. We also demonstrate that the core-shell nanoparticles with identical dielectric shells but metal cores with various sizes are able to suppress the backward or forward scattering at the same wavelength, thus revealing a large tolerance to fabrication errors induced by the size distributions in the metal cores. These features make the proposed core-shell nanoparticles beyond the dipole limit more easily realized in practical experiments.

13.
Ecotoxicology ; 23(8): 1534-45, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25086489

RESUMO

Staphylococcus aureus strain LZ-01, isolated from the Lanzhou reaches of the Yellow River, is capable of reducing Cr(VI) to Cr(III) aerobically. We employed transcriptome sequencing analysis to identify genes involved in Cr(VI) stress responses in S. aureus LZ-01. Our results showed that 512 of the 2,370 predicted genes displayed up-regulation (>2-fold), and 49 genes were down-regulated (<50 %) after Cr(VI) exposure. Among up-regulated genes, 128 genes were annotated to encode proteins involved in cellular processes; 68 were categorized to transport and binding proteins; 26 were involved in DNA repair and 32 were associated with regulatory functions. To further elucidate the Cr(VI) resistance and reduction mechanism, we carried out physiological tests and quantitative PCR analysis. Both RNA-seq and qRT-PCR data showed genes encoding a thioredoxin reductase and main subunits of cytochrome c oxidase complex were up-regulated upon Cr(VI) treatment. Either cadmium or NaN3 treatment could inhibit Cr(VI) reduction which indicates that thioredoxin and cytochrome are involved in Cr(VI) reduction strain LZ-01. 29 ABC-type metal/multidrug transporters and efflux pumps were up-regulated, suggesting that they are involved in Cr(VI) resistance by pumping chromium ions out of cells. The up-regulation of 26 DNA repair genes demonstrate that Cr(VI) is toxic to DNA and those DNA protection proteins need to be responded for Cr(VI) stress. Based on these results, the mechanism of strain LZ-01 resists and reduces Cr(VI) is revealed.


Assuntos
Cromo/toxicidade , Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Transcriptoma , China , DNA Bacteriano/genética , Perfilação da Expressão Gênica , Genes Bacterianos , Rios/química , Staphylococcus aureus/genética , Estresse Fisiológico , Poluentes Químicos da Água/toxicidade
14.
J Med Chem ; 48(8): 2964-71, 2005 Apr 21.
Artigo em Inglês | MEDLINE | ID: mdl-15828835

RESUMO

The synthesis, antiviral and pharmacokinetic properties of zanamivir (ZMV) dimers 8 and 13 are described. The compounds are highly potent neuraminidase (NA) inhibitors which, along with dimer 3, are being investigated as potential second generation inhaled therapies both for the treatment of influenza and for prophylactic use. They show outstanding activity in a 1 week mouse influenza prophylaxis assay, and compared with ZMV, high concentrations of 8 and 13 are found in rat lung tissue after 1 week. Retention of compounds in rat lung tissue correlated both with molecular weight (excluding 3 and 15) and with a capacity factor K' derived from immobilized artificial membrane (IAM) chromatography (including 3 and 15). Pharmacokinetic parameters for 3, 8 and 13 in rats show the compounds have short to moderate plasma half-lives, low clearances and low volumes of distribution. Dimer 3 shows NA inhibitory activity against N1 viruses including the recent highly pathogenic H5N1 A/Chicken/Vietnam/8/2004. In plaque reduction assays, 3, 8 and 13 show good to outstanding potency against a panel of nine flu A and B virus strains. Consistent with its shorter and more rigid linking group, dimer 8 has been successfully crystallized.


Assuntos
Antivirais/síntese química , Virus da Influenza A Subtipo H5N1 , Vírus da Influenza A/efeitos dos fármacos , Vírus da Influenza B/efeitos dos fármacos , Neuraminidase/antagonistas & inibidores , Infecções por Orthomyxoviridae/prevenção & controle , Ácidos Siálicos/química , Ácidos Siálicos/síntese química , Animais , Antivirais/química , Antivirais/farmacocinética , Antivirais/farmacologia , Linhagem Celular , Cristalização , Dimerização , Guanidinas , Vírus da Influenza A/enzimologia , Vírus da Influenza B/enzimologia , Pulmão/efeitos dos fármacos , Pulmão/enzimologia , Pulmão/virologia , Masculino , Membranas Artificiais , Camundongos , Modelos Moleculares , Peso Molecular , Infecções por Orthomyxoviridae/virologia , Piranos , Ratos , Ratos Sprague-Dawley , Ácidos Siálicos/farmacocinética , Ácidos Siálicos/farmacologia , Estereoisomerismo , Ensaio de Placa Viral , Zanamivir
15.
Antimicrob Agents Chemother ; 48(12): 4542-9, 2004 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-15561823

RESUMO

Dimeric derivatives (compounds 7 to 9) of the influenza virus neuraminidase inhibitor zanamivir (compound 2), which have linking groups of 14 to 18 atoms in length, are approximately 100-fold more potent inhibitors of influenza virus replication in vitro and in vivo than zanamivir. The observed optimum linker length of 18 to 22 A, together with observations that the dimers cause aggregation of isolated neuraminidase tetramers and whole virus, indicate that the dimers benefit from multivalent binding via intertetramer and intervirion linkages. The outstanding long-lasting protective activities shown by compounds 8 and 9 in mouse influenza infectivity experiments and the extremely long residence times observed in the lungs of rats suggest that a single low dose of a dimer would provide effective treatment and prophylaxis for influenza virus infections.


Assuntos
Antivirais/administração & dosagem , Antivirais/farmacologia , Inibidores Enzimáticos/administração & dosagem , Inibidores Enzimáticos/farmacologia , Neuraminidase/antagonistas & inibidores , Orthomyxoviridae/enzimologia , Animais , Antivirais/uso terapêutico , Linhagem Celular , Cromatografia em Gel , Efeito Citopatogênico Viral/efeitos dos fármacos , Cães , Inibidores Enzimáticos/uso terapêutico , Guanidinas , Indicadores e Reagentes , Cinética , Pulmão/metabolismo , Masculino , Camundongos , Microscopia Eletrônica , Orthomyxoviridae/efeitos dos fármacos , Orthomyxoviridae/crescimento & desenvolvimento , Infecções por Orthomyxoviridae/prevenção & controle , Piranos , Ratos , Ratos Sprague-Dawley , Ácidos Siálicos/química , Ácidos Siálicos/farmacologia , Relação Estrutura-Atividade , Ensaio de Placa Viral , Replicação Viral/efeitos dos fármacos , Zanamivir
16.
Bioorg Med Chem Lett ; 14(6): 1589-92, 2004 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-15006410

RESUMO

A set of trimeric and tetrameric derivatives 6-11 of the influenza virus neuraminidase inhibitor zanamivir 1 have been synthesized by coupling a common monomeric zanamivir derivative 3 onto various multimeric carboxylic acid core groups. These discrete multimeric compounds are all significantly more antiviral than zanamivir and also show outstanding long-lasting protective activity when tested in mouse influenza infectivity experiments.


Assuntos
Antivirais/química , Inibidores Enzimáticos/química , Vírus da Influenza A/enzimologia , Neuraminidase/antagonistas & inibidores , Animais , Antivirais/farmacologia , Antivirais/uso terapêutico , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/uso terapêutico , Guanidinas , Vírus da Influenza A/efeitos dos fármacos , Camundongos , Neuraminidase/metabolismo , Infecções por Orthomyxoviridae/tratamento farmacológico , Infecções por Orthomyxoviridae/enzimologia , Piranos , Ácidos Siálicos/química , Ácidos Siálicos/farmacologia , Ácidos Siálicos/uso terapêutico , Zanamivir
17.
J Med Chem ; 46(15): 3181-4, 2003 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-12852746

RESUMO

A series of capsid-binding compounds was screened against human rhinovirus (HRV) using a CPE based assay. The ethyl oxime ether 14 was found to have outstanding anti-HRV activity (median IC(50) 4.75 ng/mL), and unlike the equivalent ethyl ester compound 3 (Pirodavir), it has good oral bioavailability, making it a promising development candidate. Compound 14 illustrates that an oxime ether group can act as a metabolically stable bioisostere for an ester functionality.


Assuntos
Antivirais/síntese química , Capsídeo/metabolismo , Oximas/síntese química , Rhinovirus/efeitos dos fármacos , Administração Oral , Animais , Antivirais/farmacocinética , Antivirais/farmacologia , Disponibilidade Biológica , Linhagem Celular , Éteres , Feminino , Humanos , Masculino , Camundongos , Oximas/farmacocinética , Oximas/farmacologia , Piperidinas/farmacocinética , Piperidinas/farmacologia , Ligação Proteica , Piridazinas/farmacocinética , Piridazinas/farmacologia , Ratos , Relação Estrutura-Atividade
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