Publications by authors named "Jinlong Jiang"

26 Publications

  • Page 1 of 1

miR-143-3p represses leukemia cell proliferation by inhibiting KAT6A expression.

Anticancer Drugs 2021 Aug 27. Epub 2021 Aug 27.

Department of blood internal medicine, Funing People's Hospital, Funing Department of blood internal medicine, Jiangsu Provincial People's Hospital, Nanjing Department of blood internal medicine, The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, China.

Objective: The present study is designed to investigate the expressions of microRNA-143-3p (miR-143-3p) and Lysine acetyltransferase 6A (KAT6A) in acute myeloid leukemia (AML) samples and AML cell lines and to explore the possible effects and underlying mechanisms of miR-143-3p on the proliferation of AML cells.

Methods: The expressions of miR-143-3p and KAT6A in AML samples and cell lines were detected by RT-qPCR assay. CCK-8 and flow cytometry were performed to evaluate the role of KAT6A in viability of AML cells. EdU assay was performed to determine the effects of KAT6A on proliferation of AML cells. Western blot analysis was utilized to assess the impacts of KAT6A on proliferation-related protein expressions of AML cells. ELISA assay was adopted to illustrate the influence of KAT6A on inflammatory responses of AML cells. In addition, the relationship between KAT6A and miR-143-3p was predicted by ENCORI and miRWalk, and confirmed by dual-luciferase reporter assay. Moreover, the effects of KAT6A on the proliferation of AML cells mediated with miR-143-3p were carried out by rescue experiment.

Results: The expression of KAT6A was significantly upregulated, while miR-134-4p was downregulated both in the AML tissues and in AML cell lines. In addition, the silence of KAT6A significantly inhibited the viability of AML cells. Besides, KAT6A silencing notably suppressed the proliferation of AML cells and reduced the protein expressions of Ki-67 and PCNA. Knockdown of KAT6A notably decreased the expression levels of IL-1β, TNF-α and IL-6, and increased the expression levels of TGF-β and IL-10. Moreover, overexpression of miR-143-3p repressed viability and proliferation of AML cells and overexpression of KAT6A partially reversed the inhibitory effects of miR-143-3p mimic on viability and proliferation of AML cells.

Conclusion: miR-143-3p/KAT6A played an essential role in the viability and proliferation of AML cells.
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http://dx.doi.org/10.1097/CAD.0000000000001231DOI Listing
August 2021

Adsorption of Hg(II) in solution by mercaptofunctionalized palygorskite.

Environ Sci Pollut Res Int 2021 Jul 31. Epub 2021 Jul 31.

Key Laboratory for Organic Electronics and Information Displays & Jiangsu Key Laboratory for Biosensors, Institute of Advanced Materials, Nanjing University of Posts and Telecommunications, No. 9 Wenyuan Road, Yadong New District, Nanjing, 210023, China.

In the past 10 years, the treatment and restoration of soil and water bodies contaminated by mercury and other heavy metals have received unprecedented attention and support from China's environmental protection authorities. The search for low-cost and high-efficiency adsorbents has become one of the research hotspots in this field. In this paper, a simple and environment-friendly method was used to graft 3-mercaptopropyl trimethoxysilane on the surface of palygorskite. The synthesized mercaptofunctionalized palygorskite (M-PAL) was characterized by XRD, FT-IR, BET and SEM-EDS, respectively, and its adsorption conditions, adsorption models and thermodynamic parameters for Hg were systematically investigated. The experimental results indicated that the saturated adsorption capacity of Hg on the M-PAL could reach 203.4 mg·g, within 120 min at pH 4 and 298 K. By analyzing the experimental data of adsorption kinetics and thermodynamics, it was found that the adsorption process of Hg conformed to the pseudo-second-order kinetic model, which belonged to chemical adsorption of the rate-controlled step; the Langmuir model better described the adsorption isotherm. The thermodynamic parameters obtained (ΔH=29.95 kJ·mol, ΔS=103.09 J·mol·K and ΔG<0) show that the whole process is a spontaneous endothermic process. When the concentration of Na, K, Ca, Mg, Cl, NO, HCO and CHO was 200 times that of Hg, although these organic acids had a slightly greater effect on the adsorption of Hg on mercaptofunctionalized palygorskite than inorganic ions, the adsorption capacity remained above 185 mg·g. The adsorption products could be still stable in simulated acid rain with pH 3, 4, 5, 6, 7 and oxalic acid solution with concentration of 1, 2, 3, 4 and 5 mmol·L, and the desorption rates were about 3%. Through XPS analysis, the specific coordination of Hg with the S atom on the surface of M-PAL was confirmed.
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http://dx.doi.org/10.1007/s11356-021-15637-0DOI Listing
July 2021

An Efficient Catalyst Derived from Carboxylated Lignin-Anchored Iron Nanoparticle Compounds for Carbon Monoxide Hydrogenation Application.

ACS Omega 2021 Jun 18;6(25):16592-16599. Epub 2021 Jun 18.

Research Center of secondary Resources and Environment, Changzhou Institute of Technology, No.666, Liaohe Road, Changzhou City 213022, China.

Catalytic activity and target product selectivity are strongly correlated to the size, crystallographic phase, and morphology of nanoparticles. In this study, waste lignin from paper pulp industry is employed as the carbon source, which is modified with carboxyl groups at the molecular level to facilitate anchoring of metals, and a new type of carbon-based catalyst was obtained after carbonization. As a result, the size of the metal particles is effectively controlled by the chelation between -COO and Fe. Furthermore, Fe/CM-CL with a particle size of 1.5-2.5 nm shows excellent catalytic performance, the conversion of carbon monoxide reaches 82.3%, and the selectivity of methane reaches 73.2%.
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http://dx.doi.org/10.1021/acsomega.1c01935DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8246691PMC
June 2021

Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.

J Med Chem 2021 06 26;64(11):7691-7701. Epub 2021 May 26.

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

A renal outer medullary potassium channel (ROMK, Kir1.1) is a putative drug target for a novel class of diuretics with potential for treating hypertension and heart failure. Our first disclosed clinical ROMK compound, (MK-7145), demonstrated robust diuresis, natriuresis, and blood pressure lowering in preclinical models, with reduced urinary potassium excretion compared to the standard of care diuretics. However, projected to a short human half-life (∼5 h) that could necessitate more frequent than once a day dosing. In addition, a short half-life would confer a high peak-to-trough ratio which could evoke an excessive peak diuretic effect, a common liability associated with loop diuretics such as furosemide. This report describes the discovery of a new ROMK inhibitor (MK-8153), with a longer projected human half-life (∼14 h), which should lead to a reduced peak-to-trough ratio, potentially extrapolating to more extended and better tolerated diuretic effects.
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http://dx.doi.org/10.1021/acs.jmedchem.1c00406DOI Listing
June 2021

Taming Polysulfides in an Li-S Battery With Low-Temperature One-step Chemical Synthesis of Titanium Carbide Nanoparticles From Waste PTFE.

Front Chem 2021 11;9:638557. Epub 2021 Mar 11.

Hubei Collaborative Innovation Center for Advanced Organic Chemical Materials, Ministry-of-Education Key Laboratory for the Green Preparation and Application of Functional Materials, Hubei Key Laboratory of Polymer Materials, School of Materials Science and Engineering, Hubei University, Wuhan, China.

In this work, titanium carbide (TiC) nanoparticles have been successfully synthesized at much lower temperatures of 500°C using cheaper starting materials, such as waste polytetrafluoroethylene (PTFE) (carbon source) and titanium and metallic sodium, than the traditional carbothermal reduction of TiO at 1,800°C. An XRD pattern proved the formation of face-centered cubic TiC, and TEM images showed the obtained TiC nanoparticles with an average size of approximately 50 nm. In addition, the separator coated with TiC nanoparticles as an active material of interlayer effectively mitigates the shuttling problem by taming the polysulfides in Li-S batteries compared with a traditional celgard separator. The assembled cell realizes good cycling stability with 501 mAh g and a low capacity fading of 0.1% per cycle after 300 cycles at 1 C due to high utilization of the sulfur-based active species.
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http://dx.doi.org/10.3389/fchem.2021.638557DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7991077PMC
March 2021

High-efficient removal of U(VI) from aqueous solution by self-assembly pomelo peel/palygorskite composite.

Environ Sci Pollut Res Int 2021 Apr 4;28(14):17290-17305. Epub 2021 Jan 4.

National & Local Joint Engineering Research Center for Mineral Salt Deep Utilization, Huaiyin Institute of Technology, Huaian, 223003, People's Republic of China.

The efficient separation of low-concentration radionuclides by the eco-friendly adsorbent is a compelling requirement in the development of nuclear industry. Hence, a novel composite consisted of one-dimensional palygorskite (Pal) and three-dimensional pomelo peel (PP) is prepared by self-assembly approach (PP/Pal) and coupling agent approach (PP/KPal) for removing uranium (U(VI)) from aqueous solution. Moreover, the mass ratio (PP/Pal), adsorbent dosage, pH, contact time, temperature, and ionic strength are investigated. Two adsorption kinetic models and isotherm models are used to investigate the kinetic behaviors and adsorption capacity, respectively. The maximum adsorption capacities were 370.5 mg·g on PP/Pal and 357.3 mg·g on PP/KPal at pH 6.0, contact time 150 min and 25 °C. Meanwhile, the composite can be easily separated from water via a simple filtering. Furthermore, thermodynamic parameters indicate that adsorption is an endothermic and spontaneous process. And the surface complexation, ion exchange, and electrostatic attraction play a vital role. This work shows that the PP/Pal composite with high efficiency, low cost, and green has a further application in the treatment of wastewater containing U(VI).
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http://dx.doi.org/10.1007/s11356-020-12162-4DOI Listing
April 2021

Synthesis of Hierarchical Porous NiCoS/g-CN Composite for Supercapacitor with Excellent Cycle Stability.

Nanomaterials (Basel) 2020 Aug 20;10(9). Epub 2020 Aug 20.

Department of Physics, School of Science, Lanzhou University of Technology, Lanzhou 730050, China.

In this work, the hierarchical porous NiCoS/g-CN composite was prepared by growing NiCoS nanoparticles on graphitic carbon nitride (g-CN) nanosheets via a hydrothermal route. Due to the self-assembly of larger size g-CN nanosheets as a skeleton, the prepared nanocomposite possesses a unique hierarchical porous structure that can provide short ions diffusion and fast electron transport. As a result, the NiCoS/g-CN composite exhibits a high specific capacitance of 1827 F g at a current density of 1 A g, which is 1.53 times that of pure NiCoS (1191 F g). In particular, the NiCoS/g-CN//activated carbon (AC) asymmetric supercapacitor delivers a high energy density of 49.0 Wh kg at a power density of 799.0 W kg. Moreover, the assembled device shows outstanding cycle stability with 95.5% capacitance retention after 8000 cycles at a high current density of 10 A g. The attractive performance indicates that the easily synthesized and low-cost NiCoS/g-CN composite would be a promising electrode material for supercapacitor application.
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http://dx.doi.org/10.3390/nano10091631DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7558685PMC
August 2020

Flower-like NiO/ZnO hybrid coated with N-doped carbon layer derived from metal-organic hybrid frameworks as novel anode material for high performance sodium-ion batteries.

J Colloid Interface Sci 2020 Mar 21;563:354-362. Epub 2019 Dec 21.

National & Local Joint Engineering Research Center for Mineral Salt Deep Utilization, Huaiyin Institute of Technology, Huaian 223003, China.

Metal-organic hybrid frameworks are considered as the promising precursor to prepare high performance anode materials for sodium-ion batteries (SIBs). In the present work, flower-like NiO/[email protected] with hollow and porous structure was prepared via a facile solvothermal and calcination process. The hollow and porous structure not only improve the electron transport capability, and but also inhibits the aggregation and accommodates the volume change of NiO/[email protected] Meanwhile, the coated amorphous carbon layer could also increase the electron conductivity and buffer the huge volume expansion of active material NiO/ZnO. When used as anode for SIBs, NiO/[email protected] demonstrates a high specific capacity of 300 mAh g with good cycling stability for 150 cycles, fast charge and discharge capability (154 mAh g at 2500 mA g) and superior long cycling life at high current density for 2500 cycles. The strategy in this work should provide a new insight into fabrication novel structural anode materials for high performance SIBs.
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http://dx.doi.org/10.1016/j.jcis.2019.12.090DOI Listing
March 2020

A Miniature Particle Mass Spectrometer.

Anal Chem 2019 08 26;91(15):9393-9397. Epub 2019 Jul 26.

Beijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems , Institute of Chemistry, Chinese Academy of Sciences , Beijing 100190 , China.

Microparticles play important roles in our life. Besides chemical compositions and morphology, the size of microparticles will also decide their behavior in the environment or in organisms. Weighing the mass of microparticles by mass spectrometry is a useful method to characterize their size. In this technical note, a miniature particle mass spectrometer with an aerodynamic desorption/ionization ion source has been developed. We used a compact main control board to produce an ac voltage for trapping and ejecting the particles. The sampling process and data acquisition were also controlled by this board. We utilized this instrument to measure polystyrene spheres, silica particles, and mice red blood cells. Mass distributions of these particles were obtained rapidly with good accuracy.
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http://dx.doi.org/10.1021/acs.analchem.9b01069DOI Listing
August 2019

Sandwiched spherical tin dioxide/graphene with a three-dimensional interconnected closed pore structure for lithium storage.

Nanoscale 2018 Aug;10(34):16116-16126

School of Environmental and Chemical Engineering, Shanghai University, Shanghai, 200444, China.

Low reversion of lithium oxide (Li2O) and the tin (Sn) coarsening causing irreversible capacity loss is the main reason for the poor cycle performance in tin dioxide (SnO2) based composites. In this research, a novel sandwiched spherical tin dioxide/graphene with a three-dimensional interconnected closed pore structure is synthesized. The microstructural characterization shows that the spherical graphene with submicron sized diameters interconnects with each other forming an interconnected flexible conductive network, whereas a large number of SnO2 nanoparticles (approximately 5 nm) are limited homogeneously in between the interlayers of the sphere-like graphene shell. The sandwich structure of the SnO2/graphene and the closed graphene sphere can provide double protection for the SnO2. When it is used as an anode material for energy storage, the generated Li2O can remain in close contact with Sn to make the conversion reaction (SnO2 + 4Li+ + 2e- ↔ Sn + Li2O) highly reversible in situ and the reversibility even does not diminish markedly after 100 cycles. A high reversible specific capacity of 914.8 mA h g-1 is expressed in the sandwiched spherical SnO2/graphene composite at 100 mA g-1 after 100 cycles, which is significantly higher than that of a SnO2/graphene aerogel with an open pore structure.
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http://dx.doi.org/10.1039/c8nr03776kDOI Listing
August 2018

Enhanced Uptake of Iodide from Solutions by Hollow Cu-Based Adsorbents.

Materials (Basel) 2018 May 10;11(5). Epub 2018 May 10.

Key Laboratory for Palygorskite Science and Applied Technology of Jiangsu Province, Faculty of Chemical Engineering, Huaiyin Institute of Technology, Huaian 223003, China.

Cu₂O exhibits excellent adsorption performance for the removal of I anions from solutions by doping of metallic Ag or Cu. However, the adsorption process only appears on the surface of adsorbents. To further improve the utilization efficiencies of Cu content of adsorbents in the uptake process of I anions, hollow spheres of metallic Cu, Cu/Cu₂O composite and pure Cu₂O were prepared by a facile solvothermal method. Samples were characterized and employed for the uptake of I anions under various experimental conditions. The results show that Cu content can be tuned by adjusting reaction time. After the core was hollowed out, the uptake capacity of the samples increased sharply, and was proportional to the Cu content. Moreover, the optimal uptake was reached within only few hours. Furthermore, the uptake mechanism is proposed by characterization and analysis of the composites after uptake. Cu-based adsorbents have higher uptake performance when solutions are exposed to air, which further verified the proposed uptake mechanism. Finally, hollow Cu-based adsorbents exhibit excellent selectivity for I anions in the presence of large concentrations of competitive anions, such as Cl, SO₄ and NO₃, and function well in an acidic or neutral environment. Therefore, this study is expected to promote the development of Cu-based adsorbents into a highly efficient adsorbent for the removal of iodide from solutions.
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http://dx.doi.org/10.3390/ma11050769DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5978146PMC
May 2018

Microstructure and optical properties of ZnO nanorods prepared by anodic arc plasma method.

J Appl Biomater Funct Mater 2018 Jan;16(1_suppl):105-111

2 School of Science, Lanzhou University of Technology, Lanzhou, China.

Introduction: A one-dimensional ZnO nanostructure is a versatile and multifunctional n-type semiconductor. In this paper, ZnO nanorods were successfully prepared by the anodic arc plasma method in an oxidizing atmosphere.

Methods: The composition, morphology, crystal microstructure, and optical properties of ZnO nanorods were characterized by using X-ray diffraction (XRD), high-resolution transmission electron microscopy (HRTEM) and the corresponding selected-area electron diffraction (SAED), X-ray energy dispersive spectrometry (XEDS), ultraviolet-visible (UV-VIS) spectroscopy, Raman scattering spectrum (Raman), and photoluminescence spectrum (PL).

Results: The experiment results show that ZnO nanorods synthesized by this method possess hexagonal wurtzite crystal structure with good crystallization, no other impurity phases are observed, the crystalline size is about 18 nm, and the lattice constant distortion occurs compared to that of bulk ZnO. The morphology of the sample is a rod-like shape, the length ranges from 100 nm to 300 nm, the average diameter is approximately 20 nm, and the aspect ratio is relatively high. The UV-VIS absorption spectrum occurs red shift, The Raman spectrum further demonstrates that the major peaks are assigned to ZnO optical vibrational modes, and the PL spectrum exhibits coexistence properties of ultraviolet (UV) and green emission.

Conclusions: The results prove that ZnO nanorods with hexagonal wurtzite crystal structure were successfully prepared by the anodic arc plasma method in an oxidizing atmosphere.
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http://dx.doi.org/10.1177/2280800017751492DOI Listing
January 2018

Preparation of 1D Hierarchical Material Mesosilica/Pal Composite and Its Performance in the Adsorption of Methyl Orange.

Materials (Basel) 2018 Jan 20;11(1). Epub 2018 Jan 20.

Faculty of Chemical Engineering, Huaiyin Institute of Technology, Key Laboratory for Palygorskite Science and Applied Technology of Jiangsu Province, Huai'an 223003, China.

This paper highlights the synthesis of a one-dimensional (1D) hierarchical material mesosilica/palygorskite (Pal) composite and evaluates its adsorption performance for anionic dye methyl orange (MO) in comparison with Pal and Mobile crystalline material-41 (MCM-41). The Mesosilica/Pal composite is consisted of mesosilica coated Pal nanorods and prepared through a dual template approach using cetyltrimethyl ammonium bromide (CTAB) and Pal as soft and hard templates, respectively. The composition and structure of the resultant material was characterized by a scanning electron microscope (SEM), transmissionelectron microscopy (TEM), N₂ adsorption-desorption analysis, small-angle X-Ray powder diffraction (XRD), and zeta potential measurement. Adsorption experiments were carried out with different absorbents at different contact times and pH levels. Compared with Pal and MCM-41, the mesosilica/Pal composite exhibited the best efficiency for MO adsorption. Its adsorption ratio is as high as 70.4%. Its adsorption equilibrium time is as short as 30 min. Results testify that the MO retention is promoted for the micro-mesoporous hierarchical structure and positive surface charge electrostatic interactions of the mesosilica/Pal composite. The regenerability of the mesosilica/Pal composite absorbent was also assessed. 1D morphology makes it facile to separate from aqueous solutions. It can be effortlessly recovered and reused for up to nine cycles.
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http://dx.doi.org/10.3390/ma11010164DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5793662PMC
January 2018

Alginate-based attapulgite foams as efficient and recyclable adsorbents for the removal of heavy metals.

J Colloid Interface Sci 2018 Mar 13;514:190-198. Epub 2017 Dec 13.

College of Chemical Engineering, Jiangsu Key Lab for the Chemistry & Utilization of Agricultural and Forest Biomass, Nanjing Forestry University, Nanjing, Jiangsu 210037, China. Electronic address:

Floatable and porous foam adsorbents constructed by encapsulating attapulgite (ATP) in sodium alginate (SA) were fabricated via a freeze-drying and post cross-linking method, and both attapulgite and sodium alginate possessed adsorptive sites. These adsorbents were characterized by XRD, FTIR, and SEM to investigate their crystal structures, surface properties, size and morphology. In the adsorption tests, the adsorption capacity was derived from the Langmuir isotherm model, and the maximal adsorption capacity of as-prepared adsorbents was 119.0 mg g for Cu(II) and 160.0 mg g for Cd(II). In addition to the remarkable adsorptive performances, these adsorbents presented strong chemical stability and were readily recyclable because of their floatability in water solution. These aforementioned advantages highlight that the alginate-encapsulated attapulgite foams are potential scalable adsorbents for heavy metal ions removal from polluted water, and such a structure design could intrigue the development of novel adsorptive materials.
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http://dx.doi.org/10.1016/j.jcis.2017.12.035DOI Listing
March 2018

Simple fabrication of easy handling millimeter-sized porous attapulgite/polymer beads for heavy metal removal.

J Colloid Interface Sci 2017 Sep 27;502:52-58. Epub 2017 Apr 27.

College of Chemical Engineering, Nanjing Forestry University, Nanjing, Jiangsu 210037, China; Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals, Nanjing 210037, China. Electronic address:

A simple method was offered to synthesize porous attapulgite (ATP)/polymer beads. The polymeric network acts as both holder to support ATP inside the inner pore structure and as the obstacle to avoid the agglomeration of ATP during the adsorption process. Moreover, such beads are millimeter-size and can float on water surface, making such beads easy-to-handle and facile-to-recover without weight loss. The maximum adsorption capacity of such beads for Cu(II) and Cd(II) were 25.3 and 32.7mg/g, respectively, and pH value plays a key role in determining the adsorption capacities. The ATP/polymer beads also show good recycling ability and chemical stability. All these properties make such beads promising candidates as adsorbents for heavy metal removal.
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http://dx.doi.org/10.1016/j.jcis.2017.04.086DOI Listing
September 2017

Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.

Bioorg Med Chem Lett 2016 12 24;26(23):5695-5702. Epub 2016 Oct 24.

Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.

Following the discovery of small molecule acyl piperazine ROMK inhibitors, the acyl octahydropyrazino[2,1-c][1,4]oxazine series was identified. This series displays improved ROMK/hERG selectivity, and as a consequence, the resulting ROMK inhibitors do not evoke QTc prolongation in an in vivo cardiovascular dog model. Further efforts in this series led to the discovery of analogs with improved pharmacokinetic profiles. This new series also retained comparable ROMK potency compared to earlier leads.
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http://dx.doi.org/10.1016/j.bmcl.2016.10.064DOI Listing
December 2016

Growing Carbon Nanotubes from Both Sides of Graphene.

ACS Appl Mater Interfaces 2016 Mar 8;8(11):7356-62. Epub 2016 Mar 8.

School of Physical Science and Technology, Lanzhou University , Lanzhou 730000, Gansu China.

The design and synthesis of hybrid structures between graphene and carbon nanotubes is an intriguing topic in the field of carbon nanomaterials. Here the synthesis of vertically aligned CNT carpets underneath graphene and from both sides of graphene is described with continuous ordering over a large area. Scanning electron microscopy and Raman spectroscopic characterizations show that CNT carpets grow underneath graphene through a base-growth mechanism, and grow on top of graphene through a tip-growth mechanism. Good electrical contact is observed from the top CNT carpets, through the graphene layer, to the bottom CNT carpets. This sandwich-like CNT/graphene/CNT hybrid structure could provide an approach to design and fabricate multilayered graphene/CNTs materials, as well as potential applications in the fields of nanomanufacturing and energy storage.
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http://dx.doi.org/10.1021/acsami.5b12254DOI Listing
March 2016

Growth and Transfer of Seamless 3D Graphene-Nanotube Hybrids.

Nano Lett 2016 Feb 26;16(2):1287-92. Epub 2016 Jan 26.

Department of Chemistry, ‡NanoCarbon Center, and §Department of Materials Science and NanoEngineering, Rice University , 6100 Main Street, Houston, Texas 77005, United States.

Seamlessly connected graphene and carbon nanotube hybrids (GCNTs) have great potential as carbon platform structures in electronics due to their high conductivity and high surface area. Here, we introduce a facile method for making patterned GCNTs and their intact transfer onto other substrates. The mechanism for selective growth of vertically aligned CNTs (VA-CNTs) on the patterned graphene is discussed. The complete transfer of the GCNT pattern onto other substrates is possible because of the mechanical strength of the GCNT hybrids. Electrical conductivity measurements of the transferred GCNT structures show Ohmic contact through the VA-CNTs to graphene--evidence of its integrity after the transfer process.
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http://dx.doi.org/10.1021/acs.nanolett.5b04627DOI Listing
February 2016

2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.

J Med Chem 2013 Jul 9;56(14):5940-8. Epub 2013 Jul 9.

Discovery Chemistry, ‡In Vitro Pharmacology, §Drug Metabolism, and ∥Laboratory Animal Resources, Merck Research Laboratories, Merck & Co. , Rahway, New Jersey 07065, United States.

Hydroisoindoline 2 has been previously identified as a potent, brain-penetrant NK1 receptor antagonist with a long duration of action and improved profile of CYP3A4 inhibition and induction compared to aprepitant. However, compound 2 is predicted, based on data in preclinical species, to have a human half-life longer than 40 h and likely to have drug-drug-interactions (DDI), as 2 is a victim of CYP3A4 inhibition caused by its exclusive clearance pathway via CYP3A4 oxidation in humans. We now report 2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one (3) as a next generation NK1 antagonist that possesses an additional clearance pathway through glucuronidation in addition to that via CYP3A4 oxidation. Compound 3 has a much lower propensity for drug-drug interactions and a reduced estimated human half-life consistent with once daily dosing. In preclinical species, compound 3 has demonstrated potency, brain penetration, and a safety profile similar to 2, as well as excellent pharmacokinetics.
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http://dx.doi.org/10.1021/jm400751pDOI Listing
July 2013

Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.

Bioorg Med Chem Lett 2012 Feb 10;22(4):1550-6. Epub 2012 Jan 10.

Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA.

A series of benzodihydroisofurans were discovered as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase (PrCP) inhibitors. The structure-activity relationship (SAR) is focused on improving PrCP activity and metabolic stability, and reducing plasma protein binding. In the established diet-induced obese (eDIO) mouse model, compound ent-3a displayed target engagement both in plasma and in brain. However, this compound failed to induce significant body weight loss in eDIO mice in a five-day study.
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http://dx.doi.org/10.1016/j.bmcl.2012.01.002DOI Listing
February 2012

Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.

J Med Chem 2009 May;52(9):3039-46

Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.

3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one (17) is a high affinity, brain-penetrant, hydroisoindoline-based neurokinin-1 (NK(1)) receptor antagonist with a long central duration of action in preclinical species and a minimal drug-drug interaction profile. Positron emission tomography (PET) studies in rhesus showed that this compound provides 90% NK(1) receptor blockade in rhesus brain at a plasma level of 67 nM, which is about 10-fold more potent than aprepitant, an NK(1) antagonist marketed for the prevention of chemotherapy-induced and postoperative nausea and vomiting (CINV and PONV). The synthesis of this enantiomerically pure compound containing five stereocenters includes a Diels-Alder condensation, one chiral separation of the cyclohexanol intermediate, an ether formation using a trichloroacetimidate intermediate, and bis-alkylation to form the cyclic amine.
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http://dx.doi.org/10.1021/jm8016514DOI Listing
May 2009

2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.

Bioorg Med Chem Lett 2006 Oct 17;16(20):5270-4. Epub 2006 Aug 17.

Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065-0900, USA.

A series of 2-aminoquinoline compounds was prepared and evaluated in MCH1R binding and functional antagonist assays. Small dialkyl, methylalkyl, methylcycloalkyl, and cyclic amines were tolerated at the quinoline 2-position. The in vivo efficacy of compound 12 was explored and compared to that of a related inactive analog to determine their effects on food intake and body weight in rodents.
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http://dx.doi.org/10.1016/j.bmcl.2006.08.006DOI Listing
October 2006

4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.

Bioorg Med Chem Lett 2006 Oct 17;16(20):5275-9. Epub 2006 Aug 17.

Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.

Structure-activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated.
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http://dx.doi.org/10.1016/j.bmcl.2006.08.008DOI Listing
October 2006

Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.

Bioorg Med Chem Lett 2004 Nov;14(22):5599-603

Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.

A series of neutral, nonbasic quinolone GnRH antagonists were prepared via Mitsunobu alkylation of protected and unprotected 4-hydroxy quinolone intermediates. The synthetic route was improved by utilization of unique reactivity and convergency afforded by the use of mono and bis-trimethylsilylethyl protected quinolones. Potent neutral GnRH antagonists were identified, including ether and lactam derivatives, that show similar in vitro binding affinity and functional activity as compared to the earlier basic 4-aminoalkyl quinolone series of nonpeptide GnRH antagonists.
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http://dx.doi.org/10.1016/j.bmcl.2004.08.056DOI Listing
November 2004

Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.

Bioorg Med Chem Lett 2004 Apr;14(7):1795-8

Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065, USA.

Syntheses and structure-activity relationships of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists are described. Some of substituents on the piperidine ring that were investigated included a fused phenyl group, a (6R)-trifluoromethyl group, (6S) and (6R)-methyl group. This study showed that GnRH binding potency was tolerated by a small group at the 6-position of the piperidine, and blocking the 6-position by a trifluoromethyl group reduced clearance rate and increased oral bioavailability.
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http://dx.doi.org/10.1016/j.bmcl.2003.12.101DOI Listing
April 2004

Synthesis of 4-trifluoromethylated 2-alkyl- and 2,3-dialkyl-substituted azetidines.

Org Lett 2003 Oct;5(22):4101-3

Department of Medicinal Chemistry, Merck Research Laboratory, P.O. Box 2000, Rahway, New Jersey 07065, USA.

[reaction: see text]. A diastereoselective approach to the synthesis of 4-trifluoromethylated 2-alkyl- and 2,3-dialkylazetidines, including BOC-protected 4-trifluoromethylazetidin-2-ylcarboxylic acid, was developed via Wittig reaction of 4-trifluomethylated beta-lactam followed by alkylation and hydrogenation.
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http://dx.doi.org/10.1021/ol030099pDOI Listing
October 2003
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