[Determination of new carmine in beverages by one step rapid solid phase extraction based on metal organic framework extractant].

New coccine is an azo pigment that is widely used in food. To mitigate potential health issues arising from excessive consumption, China has issued provisions on the allowed addition limit of new coccine in food. Currently, there are certain difficulties with establishing detection methods for such trace pigments in foods; for example, preprocessing is complex and time-intensive.

Hafnium oxide layer-enhanced single-walled carbon nanotube field-effect transistor-based sensing platform.

Single-walled carbon nanotube-based field effect transistors (SWCNT-FETs) are ideal candidates for fabricating sensors and have been widely used for chemical sensing applications. SWCNT-FETs have low selectivity because of the environmentally sensitive electronic properties of SWCNTs, and SWCNT-FETs also show a high noise signal and poor sensitivity because of charge trapping from Si-OH hydration of the SiO/Si substrate on the SWCNTs. Herein, poly (4-vinylpyridine) (P4VP) was used for noncovalent attachment to SWCNTs and selective binding to copper ions (Cu).

Rapid degradation of refractory organic pollutants by continuous ozonation in a micro-packed bed reactor.

Recently microreactor technology attracts attention due to the excellent multiphase mixing and enhanced mass transfer. Herein, a continuous ozonation system based on a micro-packed bed reactor (μPBR) was used to improve the dissolution rate of ozone and achieved a rapid and efficient degradation of refractory organic pollutants. The effects of liquid flow rate, gas flow rate, initial pH, initial O concentration and initial phenol concentration on the phenol and chemical oxygen demand (COD) removal efficiencies were also investigated.

Thiolated poly(aspartic acid)-functionalized two-dimensional MoS, chitosan and bismuth film as a sensor platform for cadmium ion detection.

In this work, a sensitive electrochemical platform for determination of cadmium ions (Cd) is obtained using thiolated poly(aspartic acid) (TPA)-functionalized MoS as a sensor platform by differential pulse anodic stripping voltammetry (DPASV). The performance of the TPA-MoS-modified sensor is systemically studied. It demonstrates that the TPA-MoS nanocomposite modified sensor exhibits superior analytical performance for Cd over a linear range from 0.

[Determination of carbendazim residues in by high performance liquid chromatography-triple quadrupole mass spectrometry].

A novel method based on high performance liquid chromatography-triple quadrupole mass spectrometry (HPLC-MS/MS) was established for the determination of carbendazim in . The sample was extracted by ethyl acetate under alkaline conditions and centrifuged. The supernatant was concentrated by rotary evaporation, redissolved, and then enriched and purified on a mixed-mode cation exchange solid phase extraction column (MCX).

A new aptamer/black phosphorous interdigital electrode for malachite green detection.

Malachite Green (MG), a cationic triphenylmethane dye, has adverse effects on the immune and reproductive system. Thus, it is essential to develop a rapid, sensitive and high-selective method for determination of MG. Black phosphorus (BP) has high charge-carrier mobility (∼1000 cm V s) and high adsorption capacity for cationic dyes (i.

Passivation of black phosphorus as organic-phase enzyme platform for bisphenol A determination.

Black phosphorus (BP) has a high charge-carrier mobility (∼1000 cm V s), but the bare BP degrades rapidly in the presence of oxygen and water which limits the application of the BP. In this study, a simple, non-covalent passivation strategy is developed by modifying of the BP with hexamethylendiamine (HA). The functionalized BP exhibits good stability over 4 weeks.

Selective Sensing of Copper Ions by Mesoporous Porphyrinic Metal-Organic Framework Nanoovals.

Copper is a common element in the environment and human body. Exposure to high concentrations of Cu potentially causes health issues, such as Wilson and Alzheimer's diseases. It is of great importance for the highly selective and sensitive detection of Cu.

Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.

Imidazo-[1, 2-a]pyrazine 1 is a potent inhibitor of Aurora A and B kinase in vitro and is effective in in vivo tumor models, but has poor oral bioavailbility and is unsuitable for oral dosing. We describe herein our effort to improve oral exposure in this class, resulting ultimately in the identification of a potent Aurora inhibitor 16, which exhibited good drug exposure levels across species upon oral dosing, and showed excellent in vivo efficacy in a mouse xenograft tumor model when dosed orally.

SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors.

Purpose: Aurora kinases are required for orderly progression of cells through mitosis, and inhibition of these kinases by siRNA or small molecule inhibitors results in cell death. We previously reported the synthesis of SCH 1473759, a novel sub-nanomolar Aurora A/B inhibitor.

Methods: We utilized SCH 1473759 and a panel of tumor cell lines and xenograft models to gain knowledge about optimal dosing schedule and chemotherapeutic combinations for Aurora A/B inhibitors.

Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.

Aurora kinases are cell cycle regulated serine/threonine kinases that have been linked to cancer. Compound 1 was identified as a potent Aurora inhibitor but lacked oral bioavailability. Optimization of 1 led to the discovery of a series of fluoroamine and deuterated analogues, exemplified by compound 25, with an improved pharmacokinetic profile.

Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core.

The imidazo-[1,2-a]-pyrazine (1) is a dual inhibitor of Aurora kinases A and B with modest cell potency (IC50 = 250 nM) and low solubility (5 μM). Lead optimization guided by the binding mode led to the acyclic amino alcohol 12k (SCH 1473759), which is a picomolar inhibitor of Aurora kinases (TdF K d Aur A = 0.02 nM and Aur B = 0.

Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.

Inhibiting human immunodeficiency virus type 1 (HIV-1) infection by blocking the host cell coreceptors CCR5 and CXCR4 is an emerging strategy for antiretroviral therapy. Currently, several novel coreceptor inhibitors are being developed in the clinic, and early results have proven promising. In this report, we describe a novel CCR5 antagonist, vicriviroc (formerly SCH-D or SCH 417690), with improved antiviral activity and pharmacokinetic properties compared to those of SCH-C, a previously described CCR5 antagonist.

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist.

The nature and the size of the benzylic substituent are shown to be the key to controlling receptor selectivity (CCR5 vs M1, M2) and potency in the title compounds. Optimization of the lead benzylic methyl compound 3 led to the methoxymethyl analogue 30, which had excellent receptor selectivity and oral bioavailability in rats and monkeys. Compound 30 (Sch-417690/Sch-D), a potent inhibitor of HIV-1 entry into target cells, is currently in clinical trials.