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1.
ACS Appl Mater Interfaces ; 16(20): 26870-26885, 2024 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-38739846

RESUMO

Pathogen detection has become a major research area all over the world for water quality surveillance and microbial risk assessment. Therefore, designing simple and sensitive detection kits plays a key role in envisaging and evaluating the risk of disease outbreaks and providing quality healthcare settings. Herein, we have designed a facile and low-cost colorimetric sensing strategy for the selective and sensitive determination of ß-galactosidase producing pathogens. The hexagonal boron nitride quantum dots (h-BN QDs) were established as a nanozyme that showed prominent peroxidase-like activity, which catalyzes 3,3',5,5'-tetramethylbenzidine (TMB) oxidation by H2O2. The h-BN QDs were embedded on a layer-by-layer assembled agarose biopolymer. The ß-galactosidase enzyme partially degrades ß-1,4 glycosidic bonds of agarose polymer, resulting in accessibility of h-BN QDs on the solid surface. This assay can be conveniently conducted and analyzed by monitoring the blue color formation due to TMB oxidation within 30 min. The nanocomposite was stable for more than 90 days and was showing TMB oxidation after incubating it with Escherichia coli (E. coli). The limit of detection was calculated to be 1.8 × 106 and 1.5 × 106 CFU/mL for E. coli and Klebsiella pneumonia (K. pneumonia), respectively. Furthermore, this novel sensing approach is an attractive platform that was successfully applied to detect E. coli in spiked water samples and other food products with good accuracy, indicating its practical applicability for the detection of pathogens in real samples.


Assuntos
Benzidinas , Compostos de Boro , Colorimetria , Escherichia coli , Pontos Quânticos , beta-Galactosidase , Pontos Quânticos/química , Colorimetria/métodos , beta-Galactosidase/metabolismo , beta-Galactosidase/química , Escherichia coli/isolamento & purificação , Escherichia coli/enzimologia , Compostos de Boro/química , Benzidinas/química , Peróxido de Hidrogênio/química , Peróxido de Hidrogênio/análise , Peroxidase/química , Peroxidase/metabolismo , Limite de Detecção , Oxirredução , Klebsiella pneumoniae/enzimologia , Klebsiella pneumoniae/isolamento & purificação
2.
ACS Appl Mater Interfaces ; 15(41): 47902-47920, 2023 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-37812745

RESUMO

Recently, single atom catalysts (SACs) featuring M-Nx (M = metal) active sites on carbon support have drawn considerable attention due to their promising enzyme-like catalytic properties. However, typical synthesis methods of SACs often involve energy-intensive carbonization processes. Herein, we report a facile one-pot, low-temperature, wet impregnation method to fully utilize M-N4 sites of manganese phthalocyanine (MnPc) by decorating molecular MnPc over the sheets of graphene nanoplatelets (GNP). The synthesized MnPc@GNP exhibits remarkable peroxidase-mimic catalytic activity toward the oxidation of chromogenic 3,3',5,5'-tetramethylbenzidine (TMB) substrate owing to the efficient utilization of atomically dispersed Mn and the high surface-to-volume ratio of the porous catalyst. A nanozyme-based colorimetric sensing probe is developed to detect important biomarker glutathione (GSH) within only 5 min in solution phase based on the ability of GSH to effectively inhibit the TMB oxidation. The high sensitivity and selectivity of the developed colorimetric assay enable us to quantitatively determine GSH concentration in different biological fluids. This work, for the first time, reports a rapid MnPc@GNP nanozyme-based colorimetric assay in the solid substrate by fabricating microfluidic paper-based analytical devices (µPADs). GSH is successfully detected on the fabricated µPADs coated with only 6.0 µg of nanozyme containing 1.6 nmol of Mn in the linear range of 0.5-10 µM with a limit of detection of 1.23 µM. This work also demonstrates the quantitative detection of GSH in mice liver tissue lysate using µPADs, which paves the way to develop µPADs for point-of-care testing.


Assuntos
Grafite , Animais , Camundongos , Grafite/química , Manganês , Microfluídica , Oxirredutases/química , Peroxidase/química , Colorimetria/métodos , Glutationa , Peróxido de Hidrogênio/química
3.
Int J Biol Macromol ; 235: 123900, 2023 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-36870643

RESUMO

Safe delivery of hydrophobic drugs to the tumor site is a major problem for the scientific community. To improve the in vivo efficacy of hydrophobic drugs by avoiding solubility concerns and providing targeted delivery by nanoparticle, we have developed robust iron oxide nanoparticles coated chitosan with ([2- (methacryloyloxy) ethyl] trimethyl ammonium chloride) (METAC) [CS-IONPs-METAC-PTX] as a drug carrier for the delivery of hydrophobic drug, paclitaxel (PTX). Drug carrier was characterized using various techniques like FT-IR, XRD, FE-SEM, DLS and VSM. Maximum drug release of 93.50 ± 2.80 % from CS-IONPs-METAC-PTX occurs at pH 5.5 in 24 h. Significantly, the nanoparticles exhibited excellent therapeutic efficacy when appraised in L929 (Fibroblast) cell lines with a good cell viability profile. CS-IONPs-METAC-PTX shows excellent cytotoxic effect in MCF-7 cell lines. In 100 µg/mL concentration, CS-IONPs-METAC-PTX formulation shows 13.46 ± 0.40 % of cell viability. Selectivity index of 2.12 indicates the highly selective and safe performance of CS-IONPs-METAC-PTX. Admirable hemocompatibility of the developed polymer material demonstrating its applicability towards drug delivery. Results of the investigation substantiate that the prepared drug carrier is a potent material for the delivery of PTX.


Assuntos
Quitosana , Nanopartículas de Magnetita , Nanopartículas , Paclitaxel/farmacologia , Paclitaxel/química , Quitosana/química , Espectroscopia de Infravermelho com Transformada de Fourier , Nanopartículas/química , Portadores de Fármacos/química , Polímeros , Liberação Controlada de Fármacos
4.
Chem Asian J ; 18(8): e202300121, 2023 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-36814113

RESUMO

Three different compositions of NiCo2 S4 (NCS) materials were prepared using three solvents, named NCS HTDI (hydrothermal in DI water), NCS STEG (solvothermal in ethylene glycol), and a novel carbon-encapsulated NCS STFA (solvothermal in formamide). The structural and morphological properties of the prepared NCS HTDI, NCS STEG, and NCS HTDI materials were analyzed using various physical characterization techniques. As prepared, NCS materials were tested as an electrode for supercapacitor (SC) application using a 3-electrode system in a basic electrolyte (3 M KOH). NCS HTDI exhibits a specific capacitance of 2536 F g-1 , NCS STEG shows 1355 F g-1 , and NCS STFA shows 1178 F g-1 at an input current density of 1 A g-1 . The SBN-PSC material is utilized as a counter electrode in the NCS STFA || SBN-PSC-based asymmetric SC device. The device exhibits exceptionally superior electrochemical performance with a specific capacitance of 172 F g-1 at 10 A g-1 input current density and 97% capacity retention after 5000 cycles in a voltage window of 1.6 V. The results confirm the superiority of NCS STFA||SBN-PSC deviceas an excellent high-energy and high-power SC.

5.
Chem Asian J ; 18(7): e202300068, 2023 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-36808866

RESUMO

In order to subdue the obvious problem of uneven electric field distribution on regularly used copper/aluminum current collectors for alkali metal batteries, graphene on porous stainless steel (pSS_Gr) was fabricated using the ion etching technique that is employed as an effective host for lithium and sodium metal anodes. The binder-free pSS_Gr demonstrated stable Li plating and stripping at areal current and capacity of 6 mA cm-2 and 2.54 mAh cm-2 , respectively, for over 1000 cycles with 98% coulombic efficiency (C.E.). Also, in the case of Na metal anode, the host has shown stable performance at 4 mA cm-2 and 1 mAh cm-2 over 1000 cycles with ∼100% C.E.. Further, a full cell composed of Li-plated pSS_Gr as an anode and LiFePO4 as a cathode is electrochemically tested at 50 mA g-1 current density with stable 100 cycles.

6.
ACS Appl Mater Interfaces ; 13(45): 54133-54142, 2021 Nov 17.
Artigo em Inglês | MEDLINE | ID: mdl-34726370

RESUMO

High-performance nonvolatile resistive random access memories (ReRAMs) and their small stimuli control are of immense interest for high-speed computation and big-data processing in the emerging Internet of Things (IoT) arena. Here, we examine the resistive switching (RS) behavior in growth-controlled HfO2/La0.67Sr0.33MnO3 (LSMO) heterostructures and their tunability in a low magnetic field. It is demonstrated that oxygen-deficient HfO2 films show bipolar switching with a high on/off ratio, stable retention, as well as good endurance owing to the orthorhombic-rich phase constitution and charge (de)trapping-enabled Schottky-type conduction. Most importantly, we have demonstrated that RS can be tuned by a very low externally applied magnetic field (∼0-30 mT). Remarkably, application of a magnetic field of 30 mT causes RS to be fully quenched and frozen in the high resistive state (HRS) even after the removal of the magnetic field. However, the quenched state could be resurrected by applying a higher bias voltage than the one for initial switching. This is argued to be a consequence of the electronically and ionically "active" nature of the HfO2-x/LSMO interface on both sides and its susceptibility to the electric and low magnetic field effects. This result could pave the way for new designs of interface-engineered high-performance oxitronic ReRAM devices.

7.
Int J Biol Macromol ; 192: 950-957, 2021 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-34662655

RESUMO

The hydrophobicity of most of the anticancer drugs offers a great challenge in selecting a system for their effective transport. Here comes the importance of micelles that offers a hydrophobic core for incorporating these drugs. In this study, Hyaluronic Acid coated Pluronic mixed micelle loaded with Paclitaxel and Curcumin was designed and evaluated its anticancer activity in MCF-7 cells. Pluronic F127 (PF127) and Pluronic P123 (PP123) were taken for preparing the mixed micelles. The targeting ligand folic acid (FA) was conjugated to one end of PP123 forming FA-PP. The end hydroxyl groups of PF127 were oxidized to aldehyde groups resulted in PF-CHO. Mixed micelles were prepared from PF-CHO and FA-PP and the end aldehyde groups were used for coating the micelles with hyaluronic acid. The material was characterized using FTIR, H1NMR, DLS, FE-SEM and TEM. The coated micelles showed spherical shape with drug loading efficiency of 50.15 and 65.05% for Paclitaxel and Curcumin, respectively. In vitro drug release was studied at pH 5.5 and 7.4. Dual drug-loaded material showed higher in-vitro anticancer activity than free Paclitaxel and Curcumin. The results suggested that synthesized mixed micelle with dual drugs showed great potential for targeted delivery to MCF-7 cells.


Assuntos
Materiais Revestidos Biocompatíveis , Curcumina/administração & dosagem , Portadores de Fármacos/química , Ácido Hialurônico/química , Micelas , Paclitaxel/administração & dosagem , Poloxaleno/química , Antineoplásicos/administração & dosagem , Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Curcumina/química , Curcumina/farmacologia , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Humanos , Interações Hidrofóbicas e Hidrofílicas , Estrutura Molecular , Paclitaxel/química , Paclitaxel/farmacologia , Tamanho da Partícula , Análise Espectral
8.
Int J Biol Macromol ; 183: 2044-2054, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34097960

RESUMO

Targeted delivery and controlled release of drugs are attractive methods for avoiding the drug's leakage during blood circulation and burst release of the drug. We prepared a nano cellulose-based drug delivery system (DDS) for the effective delivery of curcumin (CUR). In the present scenario, the role of nanoparticles in fabricating the DDS is an important one and was characterized using various techniques. The drug loading capacity was high as 89.2% at pH = 8.0, and also the maximum drug release takes place at pH = 5.5. In vitro cell viability studies of DDS on MDA MB-231; breast cancer cells demonstrated its cytotoxicity towards cancer cells. The prepared DDS was also examined for apoptosis, hemocompatibility, and Chorioallantoic membrane (CAM) studies to assess its pharmaceutical field application and the investigation results recommended that it may serve as a potential device for targeted delivery and controlled release of CUR for cancer treatment.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Celulose/síntese química , Curcumina/farmacologia , Portadores de Fármacos , Nanopartículas , Animais , Antineoplásicos Fitogênicos/toxicidade , Apoptose/efeitos dos fármacos , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Celulose/análogos & derivados , Celulose/toxicidade , Cério/química , Embrião de Galinha , Reagentes de Ligações Cruzadas/química , Curcumina/química , Curcumina/toxicidade , Preparações de Ação Retardada , Composição de Medicamentos , Liberação Controlada de Fármacos , Compostos de Epóxi/química , Feminino , Ácido Fólico/química , Humanos , Concentração de Íons de Hidrogênio , Metacrilatos/química , Sulfatos/química
10.
RSC Adv ; 10(43): 25988-25998, 2020 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-35518634

RESUMO

The unique structural merits of heterostructured nanomaterials including the electronic interaction, interfacial bonding and synergistic effects make them attractive for fabricating highly efficient optoelectronic devices. Herein, we report the synthesis of MnO2 nanorods and a rGO/MnO2 nano-heterostructure using low-cost hydrothermal and modified Hummers' methods, respectively. Detailed characterization and confirmation of the structural and morphological properties are done via X-ray Diffraction (XRD), Field Emission Scanning Electron Microscopy (FESEM) and Transmission Electron Microscopy (TEM). Compared to the isolated MnO2 nanorods, the rGO/MnO2 nano-heterostructure exhibits impressive field emission (FE) performance in terms of the low turn-on field of 1.4 V µm-1 for an emission current density of 10 µA cm-2 and a high current density of 600 µA cm-2 at a relatively very low applied electric field of 3.1 V µm-1. The isolated MnO2 nanorods display a high turn-on field of 7.1 for an emission current density of 10 µA cm-2 and a low current density of 221 µA cm-2 at an applied field of 8.1 V µm-1. Besides the superior FE characteristics of the rGO/MnO2 nano-heterostructure, the emission current remains quite stable over the continuous 2 h period of measurement. The improvement of the FE characteristics of the rGO/MnO2 nano-heterostructure can be ascribed to the nanometric features and the lower work function (6.01 and 6.12 eV for the rGO with 8% and 16% oxygen content) compared to the isolated α-MnO2(100) surface (Φ = 7.22 eV) as predicted from complementary first-principles electronic structure calculations based on density functional theory (DFT) methods. These results suggest that an appropriate coupling of rGO with MnO2 nanorods would have a synergistic effect of lowering the electronic work function, resulting in a beneficial tuning of the FE characteristics.

11.
Nanoscale Adv ; 2(7): 2914-2924, 2020 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-36132406

RESUMO

Conversion-type anode materials have been intensely studied for application in Li-ion batteries (LIBs) due to their potentially higher capacities than current graphite-based anodes. This work reports the development of a high-capacity and stable anode from a nanocomposite of N and S co-doped carbon spheres (NSCSs) with Co3O4 (NSCS-Co3O4). A hydrothermal reaction of saccharose with l-cysteine was carried out, followed by its carbonization. CSs when used as supports for conversion-type materials provide efficient electron/ion transfer channels, enhancing the overall electrochemical performance of the electrodes. Additionally, the heteroatoms doped in a carbon matrix alter the electronic properties, often increasing the reactivity of the carbon surface, and they are reported to be effective for anchoring metal oxide nanoparticles. Consequently, the NSCS-Co3O4 nanocomposites developed in this work exhibit enhanced and stable reversible specific capacity over several cycles. Stable cycling behavior was observed at 1 A g-1 with 1285 mA h g-1 of specific capacity retained after 350 cycles along with more than 99% of coulombic efficiency. This material shows excellent rate capability with a specific capacity of 745 mA h g-1 retained even at a high current density of 5 A g-1. Detailed DFT-based calculations revealed the role of doped supports in controlling the volume expansion upon lithiation.

12.
RSC Adv ; 9(62): 36343-36350, 2019 11 04.
Artigo em Inglês | MEDLINE | ID: mdl-35540581

RESUMO

The remnants of the anaerobic digestion process, 'the digestate,' mainly consist of fibrous lignin and cellulose like molecules, as a significant carbon repository along with some other inorganic impurities. The present work demonstrates the potential use of anaerobically treated fruit and vegetable waste (FVW) as a source of porous carbon for supercapacitor electrode materials. This work suggests that the FVW digestate can inherit silicon (Si) and calcium (Ca) based inorganic impurities, which play an essential role as structure directing agents for digestate derived carbon. These contaminants act as hard templates during carbonization to create hierarchical pores and contribute to an enhancement in surface area. Different batches from an anaerobic biogas digester plant are converted to porous carbon and examined as a potential supercapacitor electrode material. A maximum capacitance of 235 F g-1 is achieved from DDHPC-4kh carbon with a specific surface area of 2502 m2 g-1 at a current density of 1 A g-1 in an acidic aqueous electrolyte. The results are significant in comparison to other bio-sourced precursors studied previously.

13.
ACS Omega ; 3(10): 13676-13684, 2018 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-30411047

RESUMO

Pure TiO2 and Cu-doped TiO2 nanoparticles are synthesized by the biomediated green approach using the Bengal gram bean extract. The extract containing biomolecules acts as capping agent, which helps to control the size of nanoparticles and inhibit the agglomeration of particles. Copper is doped in TiO2 to enhance the electronic conductivity of TiO2 and its electrochemical performance. The Cu-doped TiO2 nanoparticle-based anode shows high specific capacitance, good cycling stability, and rate capability performance for its envisaged application in lithium-ion battery. Among pure TiO2, 3% Cu-doped TiO2, and 7% Cu-doped TiO2 anode, the latter shows the highest capacity of 250 mAh g-1 (97.6% capacity retention) after 100 cycles and more than 99% of coulombic efficiency at 0.5 A g-1 current density. The improved electrochemical performance in the 7% Cu-doped TiO2 is attributed to the synergetic effect between copper and titania. The results reveal that Cu-doped TiO2 nanoparticles might be contributing to the enhanced electronic conductivity, providing an efficient pathway for fast electron transfer.

14.
ACS Appl Mater Interfaces ; 9(40): 34773-34782, 2017 Oct 11.
Artigo em Inglês | MEDLINE | ID: mdl-28926228

RESUMO

Lithium ion batteries (LIBs) with polymer based electrolytes have attracted enormous attention due to the possibility of fabricating intrinsically safer and flexible devices. However, economical and eco-friendly sustainable technology is an oncoming challenge to fulfill the ever increasing demand. To circumvent this issue, we have developed a gel polymer electrolyte (GPE) based on renewable polymers like cellulose triacetate and poly(polyethylene glycol methacrylate) p(PEGMA) using a photo polymerization technique. Cellulose triacetate offers good mechanical strength with improved ionic conductivity, owing to its ether and carbonyl functional groups. It is observed that the presence of an open network has a critical impact on lithium ion transport. At room temperature, GPE PC exhibits an optimal ionic conductivity of 1.8 × 10-3 S cm-1 and transference number of 0.7. Interestingly, it affords an excellent electrochemical stability window up to 5.0 V vs Li/Li+. GPE PC shows a discharge capacity of 164 mAhg-1 after the first cycle when evaluated in a Li/GPE/LiFePO4 cell at 0.5 C-rate. Interfacial compatibility of GPE PC with lithium metal improves the overall cycling performance. This system provides a guiding principle toward a future renewable and flexible electrolyte design for flexible LIBs (FLIBs).

15.
ACS Omega ; 2(7): 3601-3609, 2017 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-30023698

RESUMO

Efficient Na ion intercalation/deintercalation in the semigraphitic lattice of a hard carbon derived from the walnut shell is demonstrated. High-temperature (1000 °C) pyrolysis of walnut shells under an inert atmosphere yields a hard carbon with a low surface area (59 m2 g-1) and a large interplanar c axis separation of 0.39-0.36 nm as compared to 0.32 nm for graphite, suitable for Na ion intercalation/deintercalation. A stable reversible capacity of 257 mAh g-1 is observed at a current density of 50 mA g-1 for such nutshell-derived carbon (NDC) with an impressive rate performance. No loss of electrochemical performance is observed for high current cycling (100 mA g-1 → 2 A g-1 → 100 mA g-1). Additionally, the NDC shows remarkably stable electrochemical performance up to 300 charge-discharge cycles at 100 mA g-1 with a minimal drop in capacity.

16.
J Hazard Mater ; 325: 90-100, 2017 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-27915103

RESUMO

Synthesis of easily separable and eco-friendly efficient catalyst with both photocatalytic and photo-Fenton degradation properties is of great importance for environment remediation application. Herein, ammonia-modified graphene (AG) sheets decorated with Fe3O4 nanoparticles (AG/Fe3O4) as a magnetically recoverable photocatalyst by a simple in situ solution chemistry approach. First, we have functionalized graphene oxide (GO) sheets by amide functional group and then Fe3O4 nanoparticles (NPs) are doped onto the functionalized GO surface. The AG/Fe3O4 nanocomposite showed efficient photocatalytic activity towards degradation of phenol (92.43%), 2-nitrophenol (2-NP) (98%) and 2-chlorophenol (2-CP) (97.15%) within 70-120min. Consequently, in case of photo-Fenton degradation phenomenon, 93.56% phenol, 98.76% 2-NP and 98.06% of 2-CP degradation were achieved within 50-80min using AG/Fe3O4 nanocomposite under sunlight irradiation. The synergistic effect between amide functionalized graphene and Fe3O4 nanoparticles (NPs) enhances the photocatalytic activity by preventing the recombination rate of electron-hole-pair in Fe3O4 NPs. Furthermore, the remarkable reusability of the AG/Fe3O4 nanocomposite was observed up to ten cycles during the photocatalytic degradation of these phenolic compounds.

17.
Chemistry ; 22(21): 7134-40, 2016 05 17.
Artigo em Inglês | MEDLINE | ID: mdl-27072914

RESUMO

Two-dimensional hexagonal boron carbon nitride (BCN) nanosheets (NSs) were synthesized by new approach in which a mixture of glucose and an adduct of boric acid (H3 BO3 ) and urea (NH2 CONH2 ) is heated at 900 °C. The method is green, scalable and gives a high yield of BCN NSs with average size of about 1 µm and thickness of about 13 nm. Structural characterization of the as-synthesized material was carried out by several techniques, and its energy-storage properties were evaluated electrochemically. The material showed excellent capacitive behaviour with a specific capacitance as high as 244 F g(-1) at a current density of 1 A g(-1) . The material retains up to 96 % of its initial capacity after 3000 cycles at a current density of 5 A g(-1) .


Assuntos
Compostos de Boro/química , Capacitância Elétrica , Química Verde/métodos , Nanoestruturas/química , Técnicas Eletroquímicas/instrumentação , Eletrodos , Química Verde/economia , Nanoestruturas/ultraestrutura , Propriedades de Superfície
18.
ACS Appl Mater Interfaces ; 8(7): 4298-302, 2016 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-26866275

RESUMO

In this study, we report on carbon coating of vertically aligned silicon nanowire (SiNWs) arrays via a simple hydrothermal process using glucose as carbon precursor. Using this process, a thin carbon layer is uniformly deposited on the SiNWs. Under optimized conditions, the coated SiNWs electrode showed better electrochemical energy storage capacity as well as exceptional stability in aqueous system as compared to uncoated SiNWs. The as-measured capacitance reached 25.64 mF/cm(2) with a good stability up to 25000 charging/discharging cycles in 1 M Na2SO4 aqueous solution.

19.
Org Biomol Chem ; 14(1): 288-95, 2016 Jan 07.
Artigo em Inglês | MEDLINE | ID: mdl-26592920

RESUMO

An efficient and simple approach has been developed for the regio-selective synthesis of iodo-substituted dihydrofurans from amine substituted alkynols. The resulting iodo-substituted dihydrofurans have been further diversified by C-C couplings and C-N coupling reactions to afford a diverse range of substituted dihydrofuran derivatives.

20.
J Pharm Sci ; 104(12): 4207-4216, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26413799

RESUMO

A 1:1 monohydrate salt containing gefitinib, an orally administrated chemotherapy treatment for lung and breast cancers and furosemide, a loop diuretic drug, commonly used in the treatment of hypertension and edema, has been prepared. The molecular salt crystallized in triclinic P-1 space group. The C-O bond lengths (~1.26 Å) in the COOH group show that proton transfer has occurred from furosemide to morpholine moiety of the gefitinib suggesting cocrystal to be ionic. The morpholine moiety of the gefitinib showed significant conformational change because of its involvement in conformation dictating the strong N-H···O hydrogen bonding interaction. The strong hydrogen bonding interaction between gefitinib and furosemide places their benzene rings in stacking mode to facilitate the generation of π-stack dimers. The neighboring dimers are bridged to each other via water molecule through N-H···O, C-H···O, O-H···N, and O-H···O interactions. The remarkable stability of the salt hydrate could be attributed to the strong hydrogen bonding interactions in the crystal structure. Interestingly, release of water from the lattice at 140°C produced new anhydrous salt that has better solubility and dissolution rate than salt hydrate. The drug-drug molecular salt may have some bearing on the treatment of patient suffering from anticancer and hypertension.


Assuntos
Antineoplásicos/química , Furosemida/química , Quinazolinas/química , Cloreto de Sódio/química , Inibidores de Simportadores de Cloreto de Sódio e Potássio/química , Água/química , Gefitinibe , Ligação de Hidrogênio , Estrutura Molecular , Solubilidade
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