Design and synthesis of ligustrazine derivatives as potential anti-Alzheimer's agents.

A novel series of ligustrazine derivatives was designed, synthesized, and evaluated as acetylcholinesterase (AChE) and butylcholinesterase (BuChE) inhibitors for the treatment of Alzheimer's disease (AD). studies displayed that some of the synthesized compounds revealed promising AChE and BuChE inhibitory effects. Particularly, compounds and , indicated highly AChE inhibitory activity with IC values of 1.

Brain metastases from small cell lung cancer and non-small cell lung cancer: comparison of spatial distribution and identification of metastatic risk regions.

Purpose: This study aims to investigate the spatial distribution difference of brain metastases (BM) between small-cell lung cancer (SCLC) and non-small-cell lung cancer (NSCLC) and to identify the metastatic risk in brain regions.

Methods: T1-enhanced MR images of 2997 BM from 728 eligible patients with SCLC and NSCLC were retrospectively reviewed by three independent medical institutions in China. All images were spatially normalised according to the Montreal Neurological Institute space, following BM delineation confirmed by three senior radiologists.

Case report: Cerebrospinal fluid-derived circulating tumor DNA diagnoses and guides the treatment of a lung adenocarcinoma case with leptomeningeal metastasis.

Leptomeningeal metastasis (LM) occurs in 3~5% of non-small cell lung cancer (NSCLC) patients. Diagnosis of patients with LM and disease monitoring remains challenging due to the low sensitivity and specificity of the commonly used approaches, such as cerebrospinal fluid (CSF) cytology and magnetic resonance imaging (MRI). Therefore, new approaches are necessary to improve the detection of LM.

Simultaneous and rapid analysis of chiral Danshensu and its ester derivatives by supercritical fluid chromatography.

The analysis and separation of chiral compounds with wide polar range by supercritical fluid chromatography is of major importance in the process of drug development and quality control. In this work, a fast and reliable enantioselective method for the simultaneous quantitative determination of 8 DBZ-related enantiomers has been successfully developed by supercritical fluid chromatography using an amylose-based reversed-chiral stationary phase. Within less than seven minutes all target compounds could be baseline resolved, using a mobile phase comprising supercritical carbon dioxide and methanol with 0.

Chiral Cyclopropenimine-catalyzed Asymmetric Michael Addition of Bulky Glycine Imine to α,β-Unsaturated Isoxazoles.

A highly efficient asymmetric Michael addition of bulky glycine imine to α,β-unsaturated isoxazoles has been achieved by using 5 mol% of chiral cyclopropenimine as a chiral organo-superbase catalyst under mild conditions. Michael adducts were obtained in excellent yields (up to 97%) and stereoselectivities (up to >99 : 1 dr and 98% ee). A significant solvent effect was found in these chiral organosuperbase catalyzed asymmetric Michael reactions.

Exploration of spatial distribution of brain metastasis from small cell lung cancer and identification of metastatic risk level of brain regions: a multicenter, retrospective study.

Objectives: This study aimed to explore the spatial distribution of brain metastases (BMs) from small cell lung cancer (SCLC) a homogenous sample, and to identify the metastatic risk levels in brain regions.

Methods: T1-enhanced magnetic resonance imaging (MRI) from SCLC patients were retrospectively reviewed from three medical institutions in China. All images were registered to the standard brain template provided by the Montreal Neurological Institute (MNI) 152 database, followed by transformation of the location of all BMs to the space of standard brain.

Capacity degradation of LiTiO during long-term cycling in terms of composition and structure.

Capacity fading of LiTiO (LTO) is inevitable during cycling; hence it is of great significance to clarify the factors causing the capacity degradation so as to take some measures to prolong the lifespan of LTO. Despite the investigation on the capacity fading mechanism within finite charge/discharge cycles, the fading mechanism during long-term cycling is still absent. Here, LTO half-cells underwent more than 700 lithiation/delithiation cycles at a current rate of 0.

Co-Modification of commercial TiO anode by combining a solid electrolyte with pitch-derived carbon to boost cyclability and rate capabilities.

The bad electrochemical performance circumscribes the application of commercial TiO (c-TiO) anodes in Li-ion batteries. Carbon coating could ameliorate the electronic conductivity of TiO, but the ionic conductivity is still inferior. Herein, a co-modification method was proposed by combining the solid electrolyte of lithium magnesium silicate (LMS) with pitch-derived carbon to concurrently meliorate the electronic and ionic conductivities of c-TiO.

The asarone-derived phenylpropanoids from the rhizome of Acorus calamus var. angustatus Besser.

Phenylpropanoids comprise a broad spectrum of biologically active natural products. As part of our ongoing research on antiepileptic active compounds from traditional Chinese herb, Acorus calamus var. angustatus Besser, three undescribed phenylpropanoids and twenty-two known ones were isolated.

A uniform few-layered carbon coating derived from self-assembled carboxylate monolayers capable of promoting the rate properties and durability of commercial TiO.

The poor cyclability and rate property of commercial TiO (c-TiO) hinder its utilization in lithium-ion batteries (LIBs). Coating carbon is one of the ways to ameliorate the electrochemical performance. However, how to effectively form a uniform thin carbon coating is still a challenge.

Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

Inspired by the traditional Chinese herbal pair of Polygala tenuifolia-Acori Tatarinowii for treating epilepsy, 33 novel substituted cinnamic α-asaronol esters and analogues were designed by Combination of Traditional Chinese Medicine Molecular Chemistry (CTCMMC) strategy, synthesized and tested systematically not only for anticonvulsant activity in three mouse models but also for LDH inhibitory activity. Thereinto, 68-70 and 75 displayed excellent and broad spectra of anticonvulsant activities with modest ability in preventing neuropathic pain, as well as low neurotoxicity. The protective indices of these four compounds compared favorably with stiripentol, lacosamide, carbamazepine and valproic acid.

Facile Synthesis of Highly Graphitized Carbon via Reaction of CaC with Sulfur and Its Application for Lithium/Sodium-Ion Batteries.

In the present work, we report, for the first time, a novel one-step approach to prepare highly graphitized carbon (HGC) material by selectively etching calcium from calcium carbide (CaC) using a sulfur-based thermo-chemical etching technique. Comprehensive analysis using X-ray diffraction, Raman spectroscopy, X-ray photoelectron spectroscopy, and N adsorption-desorption isotherms reveals a highly graphitized mesoporous structure for the CaC-derived carbon with a specific surface area of 159.5 m g.

Excavating precursors from the traditional Chinese herb Polygala tenuifolia and Gastrodia elata: Synthesis, anticonvulsant activity evaluation of 3,4,5-trimethoxycinnamic acid (TMCA) ester derivatives.

Epilepsy is a group of neurological disorders characterized by recurrent seizures that disturbs about 60 million people worldwide. In this article, a novel series of 3,4,5-trimethoxycinnamic acid (TMCA) ester derivatives 1-35 were designed inspired from the traditional Chinese herb pair drugs Polygala tenuifolia and Gastrodia elata and synthesized followed by in vivo and in silico evaluation of their anticonvulsant potential. All the synthesized derivatives were biologically evaluated for their anticonvulsant potential using two acute model of seizures induced in mice, the maximal electroshock (MES) and sc-pentylenetetrazole (PTZ) models.

Pharmacokinetics and tissue distribution evaluation of α-asaronol and its main metabolite in rats by HPLC method.

α-Asaronol is one of trace metabolites of α-asarone formed in vivo and in vitro and exhibits good anticonvulsant activities with low neurotoxicity. The present study was mainly to describe the pharmacokinetics and tissue distribution of α-asaronol and its metabolite E-2,4,5-trimethoxy cinnamic acid (E-2,4,5-TMCA), in rat after oral and intravenous administration of α-asaronol. The results indicate that α-asaronol can be absorbed (t = 5-10 min) and transformed to E-2,4,5-TMCA (t = 10-15 min) rapidly after oral administration.

Combined Modification of Dual-Phase LiTiO-TiO by Lithium Zirconates to Optimize Rate Capabilities and Cyclability.

The low electrical conductivity and ordinary lithium-ion transfer capability of LiTiO restrict its application to some degree. In this work, dual-phase LiTiO-TiO (LTOT) was modified by composite zirconates of LiZrO, LiZrO (LZO) to boost the rate capabilities and cyclability. When the homogeneous mixture of LiNO, Zr(NO)·5HO and LTOT was roasted at 700 °C for 5 h, the obtained composite achieved a superior reversible capacity of 183.

Correction: Sun, Y.; et al. Design, Synthesis, and Evaluation of Novel 2-Hydroxypyrrolobenzodiazepine-5,11-dione Analogues as Potent Angiotensin Converting Enzyme (ACE) Inhibitors. 2017, 22, 1739.

The author wishes to make the following corrections to this paper [...

Uniform Surface Modification of LiZnTiO by Liquated NaMoO To Boost Electrochemical Performance.

Poor ionic and electronic conductivities are the key issues to affect the electrochemical performance of LiZnTiO (LZTO). In view of the water solubility, low melting point, good electrical conductivity, and wettability to LZTO, NaMoO (NMO) was first selected to modify LZTO via simply mixing LZTO in NMO water solution followed by calcining the dried mixture at 750 °C for 5 h. The electrochemical performance of LZTO could be enhanced by adjusting the content of NMO, and the modified LZTO with 2 wt % NMO exhibited the most excellent rate capabilities (achieving lithiation capacities of 225.

Design, Synthesis and Evaluation of Novel 2-Hydroxypyrrolobenzodiazepine-5,11-dione Analogues as Potent Angiotensin Converting Enzyme (ACE) Inhibitors.

Under the guidance of combination of traditional Chinese medicine chemistry (CTCMC), this study describes the preparation of a phenolic acid/dipeptide/borneol hybrid consisting of phenolic acid and a bornyl moiety connected to the dipeptide -terminal and -terminal respectively. It also evaluates their angiotensin converting enzyme (ACE) inhibitory and synergistic antihypertensive activities. Briefly, a series of novel 2-hydroxypyrrolobenzodiazepine-5,11-dione analogues were prepared and investigated for their ability to inhibit ACE.

Ionic Conductor of LiSiO as an Effective Dual-Functional Modifier To Optimize the Electrochemical Performance of LiTiO for High-Performance Li-Ion Batteries.

Ionic conductor of LiSiO (LSO) was used as an effective modifier to fabricate surface-modified LiTiO (LTO) via simply mixing followed by sintering at 750 °C in air. The electrochemical performance of LTO was enhanced by merely adjusting the mass ratio of LTO/LSO, and the LTO/LSO composite with 0.51 wt % LSO exhibited outstanding rate capabilities (achieving reversible capacities of 163.

Simple preparation of carbon nanofibers with graphene layers perpendicular to the length direction and the excellent li-ion storage performance.

Sulfur-containing carbon nanofibers with the graphene layers approximately vertical to the fiber axis were prepared by a simple reaction between thiophene and sulfur at 550 °C in stainless steel autoclaves without using any templates. The formation mechanism was discussed briefly, and the potential application as anode material for lithium-ion batteries was tentatively investigated. The carbon nanofibers exhibit a stable reversible capacity of 676.

Carbon-coated Fe-Mn-O composites as promising anode materials for lithium-ion batteries.

Fe-Mn-O composite oxides with various Fe/Mn molar ratios were prepared by a simple coprecipitation method followed by calcining at 600 °C, and carbon-coated oxides were obtained by pyrolyzing pyrrole at 550 °C. The cycling and rate performance of the oxides as anode materials are greatly associated with the Fe/Mn molar ratio. The carbon-coated oxides with a molar ratio of 2:1 exhibit a stable reversible capacity of 651.

Enhanced electrochemical performance of FeWO4 by coating nitrogen-doped carbon.

FeWO4 (FWO) nanocrystals were prepared at 180 °C by a simple hydrothermal method, and carbon-coated FWO (FWO/C) was obtained at 550 °C using pyrrole as a carbon source. The FWO/C obtained from the product hydrothermally treated for 5 h exhibits reversible capacities of 771.6, 743.

Property changes of powdery polyacrylonitrile synthesized by aqueous suspension polymerization during heat-treatment process under air atmosphere.

High molecular weight powdery polyacrylonitrile (PAN) polymers were prepared by aqueous suspension polymerization employing itaconic acid (IA) as comonomer and alpha,alpha(')-azobisisobutyronitrile (AIBN) as initiator at 60 degrees C. PAN polymers obtained with different monomer ratios were characterized by EA, DSC, FTIR and XRD. It is investigated that the oxygen element content in PAN polymers increased with the increase of required IA amounts in the feed and heat-treatment temperatures.