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Molecules, Volume 17, Issue 12 (December 2012), Pages 13704-15021

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Open AccessArticle Compounds from the Roots and Rhizomes of Valeriana amurensis Protect against Neurotoxicity in PC12 Cells
Molecules 2012, 17(12), 15013-15021; https://doi.org/10.3390/molecules171215013
Received: 12 November 2012 / Revised: 6 December 2012 / Accepted: 11 December 2012 / Published: 18 December 2012
Cited by 20 | PDF Full-text (287 KB)
Abstract
Three new germacrane-type sesquiterpenoids, heishuixiecaoline A–C (compounds 13), were isolated along with ten known compounds 413 from fraction of Valeriana amurensis roots and rhizomes effective against Alzheimer’s disease (AD). The structures of 13 were elucidated on
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Three new germacrane-type sesquiterpenoids, heishuixiecaoline A–C (compounds 13), were isolated along with ten known compounds 413 from fraction of Valeriana amurensis roots and rhizomes effective against Alzheimer’s disease (AD). The structures of 13 were elucidated on the basis of their spectroscopic data. We also investigated the protective effect of compounds 113 on the neurotoxicity of PC12 cells induced by amyloid-beta (Aβ25–25), respectively. As a result, germacrane-type sesquiterpenoids 14 and lignans 57 were seen to afford protection against Aβ-induced toxicity in PC 12 cells. This study will contribute to revealing the chemical basis for the therapeutic effect of V. amurensis against AD. Full article
Open AccessArticle Structural Changes of Oil Palm Empty Fruit Bunch (OPEFB) after Fungal and Phosphoric Acid Pretreatment
Molecules 2012, 17(12), 14995-15012; https://doi.org/10.3390/molecules171214995
Received: 16 November 2012 / Revised: 11 December 2012 / Accepted: 13 December 2012 / Published: 17 December 2012
Cited by 28 | PDF Full-text (1424 KB)
Abstract
Oil palm empty fruit bunch (OPEFB) was pretreated using white-rot fungus Pleurotus floridanus, phosphoric acid or their combination, and the results were evaluated based on the biomass components, and its structural and morphological changes. The carbohydrate losses after fungal, phosphoric acid, and
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Oil palm empty fruit bunch (OPEFB) was pretreated using white-rot fungus Pleurotus floridanus, phosphoric acid or their combination, and the results were evaluated based on the biomass components, and its structural and morphological changes. The carbohydrate losses after fungal, phosphoric acid, and fungal followed by phosphoric acid pretreatments were 7.89%, 35.65%, and 33.77%, respectively. The pretreatments changed the hydrogen bonds of cellulose and linkages between lignin and carbohydrate, which is associated with crystallinity of cellulose of OPEFB. Lateral Order Index (LOI) of OPEFB with no pretreatment, with fungal, phosphoric acid, and fungal followed by phosphoric acid pretreatments were 2.77, 1.42, 0.67, and 0.60, respectively. Phosphoric acid pretreatment showed morphological changes of OPEFB, indicated by the damage of fibre structure into smaller particle size. The fungal-, phosphoric acid-, and fungal followed by phosphoric acid pretreatments have improved the digestibility of OPEFB’s cellulose by 4, 6.3, and 7.4 folds, respectively. Full article
Open AccessArticle The Role of Slingshot-1L (SSH1L) in the Differentiation of Human Bone Marrow Mesenchymal Stem Cells into Cardiomyocyte-Like Cells
Molecules 2012, 17(12), 14975-14994; https://doi.org/10.3390/molecules171214975
Received: 7 November 2012 / Revised: 11 December 2012 / Accepted: 12 December 2012 / Published: 17 December 2012
Cited by 13 | PDF Full-text (1111 KB)
Abstract
Adult cardiomyocytes (CMs) have very limited capacity to regenerate. Therefore, there is a great interest in developing strategies to treat infarcted CMs that are able to regenerate cardiac tissue and promote revascularization of infarcted zones in the heart. Recently, stem cell transplantation has
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Adult cardiomyocytes (CMs) have very limited capacity to regenerate. Therefore, there is a great interest in developing strategies to treat infarcted CMs that are able to regenerate cardiac tissue and promote revascularization of infarcted zones in the heart. Recently, stem cell transplantation has been proposed to replace infarcted CMs and to restore the function of the affected tissue. This area of research has become very active in recent years due to the huge clinical need to improve the efficacy of currently available therapies. Slingshot (SSH) is a family of protein phosphatases, which can specifically dephosphorylate and reactivate cofilin and inhibit the polymerization of actin filaments and actively involved in cytoskeleton rearrangement. In this study, we found that SSH1L promoted morphology changes of microfilaments during differentiation but was inhibited by the inhibitors of actin polymerization such as cytochalasin D. Overexpression of SSH1L could promote cardiac-specific protein and genes expression. 5-Aza can induce the differentiation of hMSCs into cardiomyocyte-like cells in vitro. We also observed that SSH1L efficiently promotes hMSCs differentiation into cardiomyocyte-like cells through regulation and rearrangement of cytoskeleton. Our work provides evidence that supports the positive role of SSH1L in the mechanism of stem cell differentiation into cardiomyocyte-like cells. Full article
Open AccessCommunication Large-Scale Separation of Alkaloids from Corydalis bungeana Turcz. by pH-Zone-Refining Counter-Current Chromatography
Molecules 2012, 17(12), 14968-14974; https://doi.org/10.3390/molecules171214968
Received: 31 October 2012 / Revised: 27 November 2012 / Accepted: 11 December 2012 / Published: 17 December 2012
Cited by 13 | PDF Full-text (350 KB)
Abstract
pH-Zone-refining counter-current chromatography (pH-zone-refining CCC) was successfully applied for the large-scale separation of alkaloids from Corydalis bungeana. The crude extract was separated by a two-phase solvent system composed of petroleum ether–ethyl acetate–methanol–water (5:5:2:8, v/v) where triethylamine (10 mM) was added
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pH-Zone-refining counter-current chromatography (pH-zone-refining CCC) was successfully applied for the large-scale separation of alkaloids from Corydalis bungeana. The crude extract was separated by a two-phase solvent system composed of petroleum ether–ethyl acetate–methanol–water (5:5:2:8, v/v) where triethylamine (10 mM) was added to the upper organic stationary phase as a retainer and hydrochloric acid (5 mM) to the aqueous mobile phase as a displacer. As a result, 285 mg of protopine, 86 mg of corynoloxine, 430 mg of coryno1ine, and 115 mg of acetylcorynoline were obtained from 3.0 g of crude extract in a one-step separation. The purities of these compounds were 99.1%, 98.3%, 99.0% and 98.5%, respectively, as determined by HPLC. The chemical structures of these isolated compounds were confirmed by ESI-MS, 1H-NMR and 13C-NMR. Full article
Open AccessArticle Phenolic Profiles and Antioxidant Activity of Litchi (Litchi Chinensis Sonn.) Fruit Pericarp from Different Commercially Available Cultivars
Molecules 2012, 17(12), 14954-14967; https://doi.org/10.3390/molecules171214954
Received: 13 October 2012 / Revised: 5 December 2012 / Accepted: 11 December 2012 / Published: 17 December 2012
Cited by 26 | PDF Full-text (253 KB)
Abstract
Litchi fruit pericarp (LFP) contains significant amounts of phenolics which have been found to exhibit diverse biological activities. The purpose of this work was to determine the varietal differences in phenolic profiles and antioxidant activity of LFP from nine commercially available cultivars. The
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Litchi fruit pericarp (LFP) contains significant amounts of phenolics which have been found to exhibit diverse biological activities. The purpose of this work was to determine the varietal differences in phenolic profiles and antioxidant activity of LFP from nine commercially available cultivars. The total phenolic and flavonoid contents ranged from 9.39 to 30.16 mg gallic acid equivalents/g fresh weight (FW) and from 7.12 to 23.46 mg catechin equivalents/g FW, respectively. The total anthocyanin contents ranged from 1.77 to 20.94 mg cyanidin-3-glucoside equivalents/100 g FW. Three anthocyanins, including cyanidin-3-rutinoside, cyanidin-3-glucoside, malvidin-3-glucoside, were detected, and cyanidin-3-rutinoside was the predominant constituent which contributes from 68.8% to 100% to total anthocyanins, The total procyanidin contents ranged from 4.35 to 11.82 mg epicatechin equivalents/g FW. Procyanidin B2, epicatechin, A-type procyanidin trimer, and procyanidin A2 were detected in all nine litchi varieties. The oxygen radical absorbance capacity activities and DPPH radical-scavenging activities ranged from 430.49 to 1752.30 μmol TE/100 g FW and from 4.70 to 11.82 mg/g (IC50), respectively. These results indicate that there are significant differences in phytochemical profiles and antioxidant activity among the tested varieties. Knowing the phenolic profiles and antioxidant activity of LFP of different varieties gives the insights into its potential application to promote health. Full article
Open AccessArticle QSPR Models for Predicting Log Pliver Values for Volatile Organic Compounds Combining Statistical Methods and Domain Knowledge
Molecules 2012, 17(12), 14937-14953; https://doi.org/10.3390/molecules171214937
Received: 10 September 2012 / Revised: 12 December 2012 / Accepted: 13 December 2012 / Published: 17 December 2012
Cited by 7 | PDF Full-text (530 KB) | Supplementary Files
Abstract
Volatile organic compounds (VOCs) are contained in a variety of chemicals that can be found in household products and may have undesirable effects on health. Thereby, it is important to model blood-to-liver partition coefficients (log Pliver) for VOCs in a fast
[...] Read more.
Volatile organic compounds (VOCs) are contained in a variety of chemicals that can be found in household products and may have undesirable effects on health. Thereby, it is important to model blood-to-liver partition coefficients (log Pliver) for VOCs in a fast and inexpensive way. In this paper, we present two new quantitative structure-property relationship (QSPR) models for the prediction of log Pliver, where we also propose a hybrid approach for the selection of the descriptors. This hybrid methodology combines a machine learning method with a manual selection based on expert knowledge. This allows obtaining a set of descriptors that is interpretable in physicochemical terms. Our regression models were trained using decision trees and neural networks and validated using an external test set. Results show high prediction accuracy compared to previous log Pliver models, and the descriptor selection approach provides a means to get a small set of descriptors that is in agreement with theoretical understanding of the target property. Full article
(This article belongs to the Special Issue QSAR and Its Applications)
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Open AccessArticle Copper Nanoparticles Mediated by Chitosan: Synthesis and Characterization via Chemical Methods
Molecules 2012, 17(12), 14928-14936; https://doi.org/10.3390/molecules171214928
Received: 26 October 2012 / Revised: 12 November 2012 / Accepted: 21 November 2012 / Published: 14 December 2012
Cited by 77 | PDF Full-text (663 KB)
Abstract
Herein we report a synthesis of copper nanoparticles (Cu-NPs) in chitosan (Cts) media via a chemical reaction method. The nanoparticles were synthesized in an aqueous solution in the presence of Cts as stabilizer and CuSO4·5H2O precursor. The synthesis proceeded
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Herein we report a synthesis of copper nanoparticles (Cu-NPs) in chitosan (Cts) media via a chemical reaction method. The nanoparticles were synthesized in an aqueous solution in the presence of Cts as stabilizer and CuSO4·5H2O precursor. The synthesis proceeded with addition of NaOH as pH moderator, ascorbic acid as antioxidant and hydrazine as the reducing agent. The characterization of the prepared NPs was done using ultraviolet-visible spectroscopy, which showed a 593 nm copper band. The Field Emission Scanning Electron Microscope (FESEM) images were also observed, and found to be in agreement with the UV-Vis result, confirming the formation of metallic Cu-NPs. The mean size of the Cu-NPs was estimated to be in the range of 35–75 nm using X-ray diffraction. XRD was also used in analysis of the crystal structure of the NPs. The interaction between the chitosan and the synthesized NPs was studied using Fourier transform infrared (FT-IR) spectroscopy, which showed the capping of the NPs by Cts. Full article
Open AccessArticle Hydroxysafflor Yellow A (HSYA) from Flowers of Carthamus tinctorius L. and Its Vasodilatation Effects on Pulmonary Artery
Molecules 2012, 17(12), 14918-14927; https://doi.org/10.3390/molecules171214918
Received: 22 October 2012 / Revised: 19 November 2012 / Accepted: 7 December 2012 / Published: 13 December 2012
Cited by 14 | PDF Full-text (368 KB)
Abstract
Flowers of Carthamus tinctorius L. are traditionally used in China to treat cerebrovascular and cardiovascular diseases. Hydroxysafflor yellow A (HSYA), the main constituent of Carthamus tinctorius L. flowers, is known for its multiple biological activities. In the present study, HSYA was isolated from
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Flowers of Carthamus tinctorius L. are traditionally used in China to treat cerebrovascular and cardiovascular diseases. Hydroxysafflor yellow A (HSYA), the main constituent of Carthamus tinctorius L. flowers, is known for its multiple biological activities. In the present study, HSYA was isolated from Carthamus tinctorius L. flowers by a macroporous resin adsorption chromatography method coupled with a Waters high-throughput auto-purification system and it's vasodilatation effects on pulmonary artery (PA) were explored by an assay of tension study on rat pulmonary artery (PA) rings. Results suggest that HSYA possesses vascular relaxation effects on rat PA by activating the KV channel in pulmonary vascular smooth muscle cells (PVSMCs). Full article
(This article belongs to the Section Natural Products Chemistry)
Open AccessArticle Absorption and Interaction of the Main Constituents from the Traditional Chinese Drug Pair Shaoyao-Gancao via a Caco-2 Cell Monolayer Model
Molecules 2012, 17(12), 14908-14917; https://doi.org/10.3390/molecules171214908
Received: 6 November 2012 / Revised: 15 November 2012 / Accepted: 30 November 2012 / Published: 13 December 2012
Cited by 12 | PDF Full-text (263 KB)
Abstract
Shaoyao-Gancao (Paeoniae Radix Alba and Glycyrrhizae Radix et Rhizoma) is a traditional Chinese drug pair widely used in decoctions for relieving pains, especially abdominal pain. We aimed to determine the intestinal absorption and interaction of three active compounds (glycyrrhizic acid, liquiritin,
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Shaoyao-Gancao (Paeoniae Radix Alba and Glycyrrhizae Radix et Rhizoma) is a traditional Chinese drug pair widely used in decoctions for relieving pains, especially abdominal pain. We aimed to determine the intestinal absorption and interaction of three active compounds (glycyrrhizic acid, liquiritin, and paeoniflorin) in this drug pair. We investigated the transport of these compounds across intestinal epithelial cells by using the Caco-2 cell monolayer in both the apical-to-basolateral (A-B) and B-A directions. All compounds could only travel through the Caco-2 cell monolayer at a low level when the cells were treated with single component solutions. In the presence of verapamil, an inhibitor of P-glycoprotein (P-gp), the absorptive permeability (PAB) of paeoniflorin and liquiritin increased significantly (p < 0.05) and efflux ratios decreased, while the absorption of glycyrrhizic acid did not change significantly, which indicated that paeoniflorin and liquiritin might be P-gp substrates. In addition, when liquiritin and glycyrrhizic acid in Gancao extract and paeoniflorin in Shaoyao extract were examined, PAB of paeoniflorin and liquiritin were significantly higher, while glycyrrhizic acid retained the same absorption level compared to the corresponding single component solutions, which suggested that some certain ingredients in the extracts can promote the absorption of paeoniflorin and liquiritin, but not that of glycyrrhizic acid. Furthermore, compared to the results of treatment with individual extracts, treatment of cells with a mixture of the two extracts considerably increased (p < 0.05) the absorption of glycyrrhizic acid and paeoniflorin and showed no change in the absorption of liquiritin, which implied that the transport of glycyrrhizic acid and paeoniflorin is increased by some ingredients from the complementary drug in the drug pair, while that of liquiritin remains unaffected. Full article
(This article belongs to the Section Molecular Diversity)
Open AccessArticle Two New Oleanane-Type Triterpenoids from Platycodi Radix and Anti-proliferative Activity in HSC-T6 Cells
Molecules 2012, 17(12), 14899-14907; https://doi.org/10.3390/molecules171214899
Received: 9 November 2012 / Revised: 29 November 2012 / Accepted: 30 November 2012 / Published: 13 December 2012
Cited by 6 | PDF Full-text (230 KB)
Abstract
Two new oleanane-type triterpenoids, named platycodonoids A and B (1, 2), together with five known saponins, including platycodin D (3), deapioplatycodin D (4), 3-O-β-D-glucopyranosyl polygalacic acid (5), 3-O-β-D-glucopyranosyl platycodigenin (
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Two new oleanane-type triterpenoids, named platycodonoids A and B (1, 2), together with five known saponins, including platycodin D (3), deapioplatycodin D (4), 3-O-β-D-glucopyranosyl polygalacic acid (5), 3-O-β-D-glucopyranosyl platycodigenin (6) and polygalacin D (7), were isolated from the roots of Platycodon grandiflorum. On the basis of spectral data and chemical evidence, the structures of the new compounds were elucidated as 2β,3β,23,24-tetrahydroxy-28-nor-olean-12-en-16-one (1) and 2β,3β,23,24- tetrahydroxy-28-nor-olean-12-en-16-one-3-O-β-D-glucopyranoside (2). Compounds 17 were evaluated for their in vitro anti-proliferative activity against the HSC-T6 cell line. Full article
Open AccessArticle Synthesis and in Vitro Antioxidant Activity Evaluation of 3-Carboxycoumarin Derivatives and QSAR Study of Their DPPH• Radical Scavenging Activity
Molecules 2012, 17(12), 14882-14898; https://doi.org/10.3390/molecules171214882
Received: 21 September 2012 / Revised: 3 December 2012 / Accepted: 5 December 2012 / Published: 13 December 2012
Cited by 16 | PDF Full-text (379 KB)
Abstract
The in vitro antioxidant activities of eight 3-carboxycoumarin derivatives were assayed by the quantitative 1,1-diphenyl-2-picrylhydrazil (DPPH•) radical scavenging activity method. 3-Acetyl-6-hydroxy-2H-1-benzopyran-2-one (C1) and ethyl 6-hydroxy-2-oxo-2H-1-benzopyran-3-carboxylate (C2) presented the best radical-scavenging activity. A quantitative structure-activity relationship
[...] Read more.
The in vitro antioxidant activities of eight 3-carboxycoumarin derivatives were assayed by the quantitative 1,1-diphenyl-2-picrylhydrazil (DPPH•) radical scavenging activity method. 3-Acetyl-6-hydroxy-2H-1-benzopyran-2-one (C1) and ethyl 6-hydroxy-2-oxo-2H-1-benzopyran-3-carboxylate (C2) presented the best radical-scavenging activity. A quantitative structure-activity relationship (QSAR) study was performed and correlated with the experimental DPPH• scavenging data. We used structural, geometrical, topological and quantum-chemical descriptors selected with Genetic Algorithms in order to determine which of these parameters are responsible of the observed DPPH• radical scavenging activity. We constructed a back propagation neural network with the hydrophilic factor (Hy) descriptor to generate an adequate architecture of neurons for the system description. The mathematical model showed a multiple determination coefficient of 0.9196 and a root mean squared error of 0.0851. Our results shows that the presence of hydroxyl groups on the ring structure of 3-carboxy-coumarins are correlated with the observed DPPH• radical scavenging activity effects. Full article
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Open AccessArticle Chemical Composition and Insecticidal Activity of the Essential Oil of Illicium pachyphyllum Fruits against Two Grain Storage Insects
Molecules 2012, 17(12), 14870-14881; https://doi.org/10.3390/molecules171214870
Received: 23 November 2012 / Revised: 10 December 2012 / Accepted: 11 December 2012 / Published: 13 December 2012
Cited by 25 | PDF Full-text (278 KB)
Abstract
The aim of this research was to determine chemical composition and insecticidal activity of the essential oil of Illicium pachyphyllum fruits against two grain storage insects, Sitophilus zeamais and Tribolium castaneum, and to isolate any insecticidal constituents from the essential oil. The
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The aim of this research was to determine chemical composition and insecticidal activity of the essential oil of Illicium pachyphyllum fruits against two grain storage insects, Sitophilus zeamais and Tribolium castaneum, and to isolate any insecticidal constituents from the essential oil. The essential oil of I. pachyphyllum fruits was obtained by hydrodistillation and analyzed by GC-MS. A total of 36 components of the essential oil were identified, with the principal compounds in the essential oil being trans-ρ-mentha-1(7),8-dien-2-ol (24.56%), D-limonene (9.79%), caryophyllene oxide (9.32%), and cis-carveol (5.26%) followed by β-caryophyllene (4.63%) and bornyl acetate. Based on bioactivity-guided fractionation, the three active constituents were isolated and identified as trans-ρ-mentha-1(7),8-dien-2-ol, D-limonene and caryophyllene oxide. The essential oil of I. pachyphyllum fruits exhibited contact toxicity against S. zeamais and T. castaneum adults, with LD50 values of 17.33 μg/adult and 28.94 μg/adult, respectively. trans-p-Mentha-1(7),8-dien-2-ol (LD50 = 8.66 μg/adult and 13.66 μg/adult, respectively) exhibited stronger acute toxicity against S. zeamais and T. castaneum adults than either caryophyllene oxide (LD50 = 34.09 μg/adult and 45.56 μg/adult) and D-limonene (LD50 = 29.86 μg/adult and 20.14 μg/adult). The essential oil of I. pachyphyllum possessed fumigant toxicity against S. zeamais and T. castaneum adults with LC50 values of 11.49 mg/L and 15.08 mg/L, respectively. trans-p-Mentha-1(7),8-dien-2-ol exhibited stronger fumigant toxicity against S. zeamais and T. castaneum adults, respectively, with LC50 values of 6.01 mg/L and 8.14 mg/L, than caryophyllene oxide (LC50 = 17.02 mg/L and 15.98 mg/L) and D-limonene (LC50 = 33.71 mg/L and 21.24 mg/L). The results indicate that the essential oil of I. pachyphyllum fruits and its constituent compounds have potential for development into natural insecticides or fumigants for the control of insects in stored grains. Full article
(This article belongs to the Section Natural Products Chemistry)
Open AccessArticle Study of Rigid Cross-Linked PVC Foams with Heat Resistance
Molecules 2012, 17(12), 14858-14869; https://doi.org/10.3390/molecules171214858
Received: 11 October 2012 / Revised: 2 December 2012 / Accepted: 10 December 2012 / Published: 13 December 2012
PDF Full-text (295 KB)
Abstract
Three heat resistant cross-linked PVC foam plastics were prepared and their performances were compared with universal cross-linked PVC structural foam. The results show that these three heat resistant foams have higher glass transition temperatures (close to 100 °C) than universal structural foam (83.2
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Three heat resistant cross-linked PVC foam plastics were prepared and their performances were compared with universal cross-linked PVC structural foam. The results show that these three heat resistant foams have higher glass transition temperatures (close to 100 °C) than universal structural foam (83.2 °C). Compared with the universal structural foam, the three heat resistant foams show much higher decomposition temperature and better chemical stability due to the crosslinking of PVC macromolecular chains. The heat distortion temperature (HDT) values of the three heat resistant foam plastics are just a little higher than that of universal structural foam. The three heat resistant foam plastics have good dimensional stability at 140 °C, and when used as core material can closely adhere to the face plates in medium temperature curing processes. Compared with universal structural foam, the three heat resistant foam plastics have slightly better mechanical properties. Full article
Open AccessArticle 1,3-Bisdiphenylethenyl-substituted Carbazolyl Derivatives as Charge Transporting Materials
Molecules 2012, 17(12), 14846-14857; https://doi.org/10.3390/molecules171214846
Received: 19 November 2012 / Revised: 9 December 2012 / Accepted: 11 December 2012 / Published: 13 December 2012
Cited by 4 | PDF Full-text (337 KB)
Abstract
Synthesis of 1,3-diphenylethenylcarbazolyl-based charge transporting materials involving electron donating hydrazone moieties and an electron withdrawing 1,3-indandione moiety is reported. The obtained materials were examined by various techniques, including differential scanning calorimetry, UV-Vis spectroscopy, xerographic time of flight technique and the electron photoemission in
[...] Read more.
Synthesis of 1,3-diphenylethenylcarbazolyl-based charge transporting materials involving electron donating hydrazone moieties and an electron withdrawing 1,3-indandione moiety is reported. The obtained materials were examined by various techniques, including differential scanning calorimetry, UV-Vis spectroscopy, xerographic time of flight technique and the electron photoemission in air method. Photoemission spectra of the amorphous films of the investigated compounds showed ionization potentials of 5.54–5.90 eV. The hole drift mobility was measured by the xerographic time of flight technique. The highest hole drift mobility, exceeding 10−5 cm2/V·s at 6.4 × 105 V/cm electric field, was observed for the 1,3-diphenylethenylcarbazolyl derivative molecularly doped with a N,N-diphenylhydrazone moiety in the polymeric host bisphenol-Z polycarbonate (PC-Z). Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle A General Synthesis of Bis-indolylpiperazine-2,5-diones
Molecules 2012, 17(12), 14841-14845; https://doi.org/10.3390/molecules171214841
Received: 15 November 2012 / Revised: 5 December 2012 / Accepted: 5 December 2012 / Published: 13 December 2012
Cited by 3 | PDF Full-text (177 KB)
Abstract
The one-pot synthesis of three dragmacidin derivatives is reported. Sarcosine anhydride (4) is brominated and immediately reacted with the corresponding indole to produce the products, namely 3,6-bis(5′-methoxy-3′-indolyl)-1,4-dimethylpiperazine-2,5-dione (1), 3,6-bis(7′-methyl-3′-indolyl)-1,4-dimethylpiperazine-2,5-dione (2) and 3,6-bis-(6′-chloro-3′-indolyl)-1,4-dimethylpiperazine-2,5-dione (3), which are characterized by 1H-NMR. Full article
(This article belongs to the Section Organic Chemistry)
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