DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
·
2019
·
IF 2.367
Dan Lou,Xiao Cui,Su-Su Bao,Wei Sun,Wen-He Pan,Meng-Chun Chen,Yao-Yao Dong,Guo-Xin Hu,Rui-Jie Chen,Zhe Wang
We investigated the effect of azole antifungal drugs (ketoconazole, voriconazole, and itraconazole) on the pharmacokinetics of apatinib in rats. The rats in ketoconazole, voriconazole, and itraconazole groups received single-dose apatinib 30 mg/kg after the oral administration of ketoconazole, voriconazole, and itraconazole, respectively. Co-administration of ketoconazole or voriconazole significantly increased the apatinib Cmax and AUC(0–t) and decreased the clearance. Co-administration of itraconazole did not significantly affect the pharmacokinetics parameters of apatinib. It could be concluded that both ketoconazole and voriconazole significantly increase the exposure of apatinib, and affect the pharmacokinetics of apatinib in rat. Apatinib can be co-administered with itraconazole, but ketoconazole and voriconazole should be avoided if possible or be underwent therapeutic drug monitoring of apatinib. A further clinical study should be conducted to investigate the inhibitory effect of azole antifungal drugs on the apatinib plasma concentration.
研究领域:
药理学
·
临床医学
✓ 已验证
DOI
高影响因子
MICROCHEMICAL JOURNAL
·
2023
·
IF 4.8
Zhiqin Huang,Qingli Zeng,Dan Li,Laisheng Li
The new type of bis- triazolyl bridged cyclodextrin-based stationary phase (BCDP) was prepared through “Click reaction”. BCDP had high selectivity for triazoles and was used for the simultaneous fast separation and determination of enantiomeric residues (flutriafol, hexaconazole and diniconazole) in fruits and vegetables by high-performance liquid chromatography (HPLC). The QuEChERS method assisted by magnetic nanoparticles was used for sample pretreatment, and then a gradient elution was carried out by using MeOH-H 2 O as the mobile phase on BCDP to achieve rapid resolution of the triazole enantiomers within 25 min. After condition optimization, simultaneous baseline separations of the six enantiomers were achieved with resolutions of 1.54 (flutriafol), 2.27 (hexaconazole) and 1.97 (diniconazole). A new HPLC quantification method of the six enantiomeric residues in apples, tomatoes and cucumbers was established by an internal standard with a photo-diode array (PDA) detector at 210 nm. The results showed that the excellent linear relationships of all triazole enantiomers were observed in the concentration range of 0.5–50 mg L -1 ( R 2 = 0.9986–0.9999). The average recoveries of enantiomers in fruits and vegetables were from 91.95 % to 109.92 % with RSDs of 0.97 %–1.32 % for intraday and 1.30 %–3.03 % for interday. The limits of detection (LODs, S/N = 3) and limits of quantitation (LOQs, S/N = 10) of all enantiomers were less than 0.03 mg kg −1 and 0.10 mg kg −1 , respectively. BCDP had high selectivity for triazole due to its synergistic inclusion with triazoles and advantage in fast and simultaneous separation of multiple triazole enantiomers, which could save analysis time and reduce solvent consumption. BCDP was a new separation material for the scientific evaluation of chiral pesticides in the food safety analysis.
研究领域:
食品安全分析
·
农药残留检测
·
分析化学
✓ 已验证
产品关联
DOI
高影响因子
ChemistrySelect
·
2024
·Vol. 9
·期 36
·e202401875
·
IF 1.9
Haonan Li,Chenping Gao,Qingjie Liu,Yanchun Guo,Yufen Zhao
Graphical We report here a new I 2 /H 2 O 2 co-catalyzed oxidative [4+1] cyclization of benzaldehyde with 2-(aminomethyl)pyridine or o -phenylenediamine/2-aminothiophenol to provide various substituted imidazo[1,5- a ]pyridines and benzimidazoles/thiazole via C(acyl)−N bond construction. Some of heterocyclic products exhibit blue luminescence properties, as well as large Stokes shifts, eminent fluorescence quantum yields (64 %) and long fluorescence lifetimes. An efficient I 2 (10 mmol %)/H 2 O 2 mediated oxidative formal [4+1] cyclization of 2-pyridinemethylamine or o -phenylenediamine (2-aminobenzenethiol) with benzaldehyde via C−N bond formation has been developed. This strategy provides a straightforward approach to imidazo[1,5- a ]pyridines, iodo-substituted imidazo[1,5- a ]pyridines and benzimidazole (benzothiazole) derivatives in yields ranging from 60 % to 98 %, respectively. Several heterocyclic products exhibit promising blue luminous performance with satisfactory fluorescence quantum yields of up to 64 %, large Stokes shifts, and a longer lifetime (7.35 ns). The band gap energies obtained from DFT are also consistent with the absorption spectra.
研究领域:
有机化学
·
光物理化学
✓ 已验证
DOI
高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2020
·Vol. 43
·期 16
·3183-3196
·
IF 2.878
Lu-Ning Sun,Ye Zhang,Yu-Qing Yang,Ye Shen,Yu-Wen Ying,Yu-Wen Su,Xue-Hui Zhang,Yun Liu,Xu Huang,Yong-Qing Wang
Proton pump inhibitors, including omeprazole, rabeprazole, lansoprazole, and pantoprazole, achieved simultaneous enantioselective determination in the human plasma by chiral liquid chromatography–tandem mass spectrometry. The four corresponding stable isotope-labeled proton pump inhibitors were adopted as the internal standards. Each enantiomer and the internal standards were extracted with acetonitrile containing 0.1% ammonia, then separated with a Chiralpak IC column (5 µm, 4.6 mm × 150 mm) within 10 min. The mobile phase was composed of acetonitrile–ammonium acetate (10 mM) containing 0.2% acetic acid (50:50, v/v). To quantify all enantiomers, an API 4000 tandem mass spectrometer was used, and multiple reaction monitoring transitions were performed on m/z 360.1→242.1, 384.1→200.1, 370.1→252.1, and 346.1→198.1, respectively. No significant matrix effect was observed for all analytes. The calibration curve for all enantiomers were linear from 1.25 to 2500 ng/mL. The precisions for intra- and inter-run were < 14.2%, and the accuracy fell in the interval of –5.3 to 8.1%. Stability of samples was confirmed under the storage and processing conditions. The developed method was also suitable for separation and determination of ilaprazole enantiomers. The validated method combining the equilibrium dialysis method was applied to the protein binding ratio studies of four pairs proton pump inhibitor enantiomers in human plasma.
研究领域:
药物分析
·
临床药理学
✓ 已验证
DOI
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 6
·2442
·
IF 4.6
Hongwu Liu,Shan Yang,Ting Li,Siyue Ma,Peiyi Wang,Guoqing Wang,Shanshan Su,Yue Ding,Linli Yang,Xiang Zhou,Song Yang
Imidazole alkaloids, a common class of five-membered aromatic heterocyclic compounds, exist widely in plants, animals and marine organisms. Because of imidazole’s extensive and excellent biological and pharmacological activities, it has always been a topic of major interest for researchers and has been widely used as an active moiety in search of bioactive molecules. To find more efficient antibacterial compounds, a series of novel imidazole-fragment-decorated 2-(pyrazol-4-yl)-1,3,4-oxadiazoles were designed and synthesized based on our previous works via the active substructure splicing principle, and their bioactivities were systematically evaluated both in vitro and in vivo. The bioassays showed that some of the target compounds displayed excellent in vitro antibacterial activity toward three virulent phytopathogenic bacteria, includingXanthomonas oryzaepv.oryzae(Xoo),Xanthomonas axonopodispv.citri(Xac) andPseudomonas syringaepv.actinidiae(Psa), affording the lowest EC50values of 7.40 (7c), 5.44 (9a) and 12.85 (9a) μg/mL, respectively. Meanwhile, compound7cpossessed good in vivo protective and curative activities to manage rice bacterial leaf blight at 200 μg/mL, with control efficacies of 47.34% and 41.18%, respectively. Furthermore, compound9ashowed commendable in vivo protective and curative activities to manage kiwifruit bacterial canker at 200 μg/mL, with control efficacies of 46.05% and 32.89%, respectively, which were much better than those of the commercial bactericideTC(31.58% and 17.11%, respectively). In addition, the antibacterial mechanism suggested that these new types of title compounds could negatively impact the cell membranes of phytopathogenic bacteria cells and cause the leakage of the intracellular component, thereby leading to the killing of bacteria. All these findings confirm that novel 2-(pyrazol-4-yl)-1,3,4-oxadiazoles containing an imidazole fragment are promising lead compounds for discovering new bactericidal agents.
研究领域:
药理学
·
植物病理学
·
有机化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2019
·Vol. 24
·期 7
·1311
·
IF 3.06
Ming-Jie Chu,Wei Wang,Zi-Li Ren,Hao Liu,Xiang Cheng,Kai Mo,Li Wang,Feng Tang,Xian-Hai Lv
To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors. Compound4dexhibited the most potent antibacterial activity with Minimum inhibitory concentration (MIC) alues of 4 µg/mL, 2 µg/mL, 4 µg/mL, and 0.5 µg/mL againstStaphylococcus aureus,Listeria monocytogenes,Escherichia coli, andSalmonella gallinarum, respectively. The in vivo enzyme inhibition assay4ddisplayed the most potent topoisomerase II (IC50= 13.5 µg/mL) and topoisomerase IV (IC50= 24.2 µg/mL) inhibitory activity. Molecular docking was performed to position compound4dinto the topoisomerase II active site to determine the probable binding conformation. In summary, compound4dmay serve as potential topoisomerase II inhibitor.Keywords:pyrazole;triazole;ester;antibacterial;topoisomerase II inhibitor
研究领域:
药理学
·
微生物学
·
药物化学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2024
·
IF 5.3
Bin Chen,Hegang Shu,Yujun Guo,Yingjie Xu
In this work, the effect of the structure and substitution of azole-based anion on the CO 2 capture and viscosity ( η ) of metal chelate-based dual functional ionic liquids (DFILs) with [K(DGA) 2 ] + cation was investigated. The CO 2 absorption capacity of DFILs at 0.1 MPa and 333.2 K shows that methyl and nitro groups on the azole-based anion, such as pyrazolide ([Pyr] − ) and imidazolide ([Im] − ), attenuate their reactivity with CO 2 through the steric hindrance and electron-withdrawing effects, respectively. Furthermore, the CO 2 absorption capacity of [K(DGA) 2 ][Pyr] is larger than that of [K(DGA) 2 ][Im], which is due to the interaction of the two adjacent N atoms in the [Pyr] − anion with CO 2 , as confirmed by DFT calculations. The CO 2 absorption mechanism shows that both [Pyr] − anion and [K(DGA) 2 ] + cation of [K(DGA) 2 ][Pyr] can chemically interact with CO 2 , making its saturated uptake at 333.2 K as high as 1.47 mol CO 2 per mole IL. Moreover, CO 2 interacts preferentially with [Pyr] − , and the [K(DGA) 2 ] + –CO 2 interaction is enhanced when the CO 2 uptake is greater than 0.5 mol CO 2 per mole IL. η of pure [K(DGA) 2 ][Pyr] is lower than that of pure [K(DGA) 2 ][Im]. η of [K(DGA) 2 ][Pyr] increases with the increase of CO 2 absorption, and the rapid increase in η after CO 2 uptake greater than 0.5 is attributed to the formation of [K(DGA) 2 ] + –CO 2 interactions.
研究领域:
化学
·
环境科学
✓ 已验证
产品关联
DOI
高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
·
2016
·Vol. 408
·期 19
·5247-5259
·
IF 3.125
Pan Ziyu,Peng Jingdong,Zang Xu,Lei Gang,He Yan,Liu Di
A novel, highly selective, and sensitive resonance light scattering (RLS) detection approach coupled with high performance liquid chromatography (HPLC) was researched and developed for the synchronous analysis of three kinds of benzimidazole anthelmintics, including mebendazole (MBZ), albendazole (ABZ), and fenbendazole (FBZ) for the first time. In the pH range of 3.5–3.7 Britton-Robinson buffer medium, three kinds of anthelmintics, which were separated by HPLC, reacted with eosin Y (EY) to form 1:1 ion-association complexes, resulting in significantly enhanced RLS signals and the maximum peak located at 335 nm. The enhanced RLS intensity was in proportion to the MBZ, ABZ, and FBZ concentration in the range 0.2–25, 0.2–23, and 0.15–20 μg/mL, respectively. The limit of detection was in the range of 0.064–0.16 μg/mL. In addition, human urine was determined to validate the proposed method by spiked samples and real urine samples. Satisfactory results were obtained by HPLC-RLS method.
The diagram mechanism of generating resonance between emitted light and scattered light
研究领域:
分析化学
·
药物分析
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MYCOLOGIA
·
2021
·
IF 2.696
Lili Wang,Min Zhang,Jian Guo,Wenzheng Guo,Ni Zhong,Hui Shen,Jinfeng Cai,Zhaoqin Zhu,Wenjuan Wu
Recently, Cryptococcus and non-albicans Candida (NAC) have emerged as health-threatening pathogens for clinical fungal infections. Due to their increased resistance to existing antifungal drugs, novel antifungals are urgently needed. In this study, we evaluated the antifungal effect of VT-1161 and its comparators itraconazole and fluconazole against common fluconazole-sensitive or -resistant Cryptococcus and NAC strains. The tested strains were obtained from Chinese patients by the Invasive Fungal Infection Group within the past 2 years. The minimum inhibitory concentrations (MICs) of VT-1161 and other triazoles were measured according to the Clinical and Laboratory Standards Institute (CLSI) M27-Ed4 guidelines. We found that VT-1161 exhibited strong in vitro activity against Cryptococcus spp.. VT-1161 (geometric mean MIC = 0.024 μg/mL) was 21.7-fold and 104.5-fold more potent than itraconazole and fluconazole, respectively. Against the seven Cryptococcus neoformans isolates with higher fluconazole MICs (≥8 μg/mL based on the MIC90 value of this azole), VT-1161 maintained potent activities, with MICs ranging between 0.031 and 0.5 μg/mL. For NAC spp., VT-1161 (geometric mean MIC = 0.099 μg/mL) was 6.0-fold and 11.4-fold more effective than itraconazole and fluconazole, respectively. There is a positive correlation of the MICs between VT-1161 and itraconazole/fluconazole. The MIC values of VT-1161 against Candida glabrata and Candida tropicalis were significantly lower than those of fluconazole, whereas for Candida parapsilosis the differences in the MIC values between VT-1161 and fluconazole were not statistically significant. The results showed that tetrazole VT-1161 might be a promising candidate for treating Cryptococcus and NAC infections.
研究领域:
医学
·
微生物学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
LANGMUIR
·
2024
·
IF 3.7
Satish Gudala,Miao Dong,Xinrui Lin,Ruotong Liu,Annadurai Vinothkanna,Anubhuti Jha,Archi Sharma,Dazhuang Wang,Xinghua Liu,Jianxin Yang
A series of 1,2,4-triazolo-quinazolinones and 1,2-benzisothiazolone derivatives (S1–S12) were successfully synthesized as environmentally friendly alternatives to copper-based antifouling paints using N-alkylation, cyclocondensation, and one-pot three-component and amide coupling reactions. The monoclinic structure of single-crystal 1,2,4-triazolo-quinazolin-acetic acid (S8) was confirmed by single-crystal X-ray diffraction analysis. All the synthesized molecules were studied for their in silico molecular docking interactions with three target proteins, namely, RbmA, ToxR, and Bap. Following that, the antialgal activity was assessed against two types of marine algae: Chlorella sp. and Chaetoceros curvisetus. The minimal inhibitory concentration and zone of inhibition have been used to evaluate the antibacterial activities of S1–S12 against both marine Gram-positive (Staphylococcus aureus) and Gram-negative (Vibrio parahemolyticus and Vibrio vulnificus) bacteria. Additionally, antifouling studies have been done on all the compounds, and among them, 1,2,4-triazolo-quinazolinyl-acetate (S7), 1,2,4-triazolo-quinazolinyl-acetic acid (S8), 1,2,4-triazolo-quinazolinyl-oxobutanoate (S9), benzo[d]isothiazolyl butanoate (S10), benzo[d]isothiazolyl-acetic acid (S11), and 1,2,4-triazolo-quinazolinyl-acetyl-benzo[d]isothiazolone (S12) exhibited good antialgal, antibacterial, and antifouling activities.
研究领域:
海洋生物学
·
药物化学
·
环境科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF POLYMERS AND THE ENVIRONMENT
·
2017
·Vol. 26
·期 2
·765-777
·
IF 1.877
Sun Lei,Chen Dongmei,Wan Shungang,Yu Zebin
Biochar derived from sugarcane bagasse was prepared at different pyrolysis temperatures and holding times for adsorption of dimetridazole and metronidazole from aqueous solution. The optimal pyrolysis temperature and holding time were 500 °C and 120 min, respectively. The removal efficiencies of dimetridazole and metronidazole were 98.0% and 88.8%, respectively, at biochar dosage of 4.0 g L −1 and solution temperature of 30 °C. Kinetics data were fitted by four kinetics models, and results indicated that adsorption was governed by pseudo-second-order kinetics. Adsorption is a multi-step process that involves film diffusion and pore filling. In addition, five isotherm models were employed to describe the adsorption equilibrium. Brunauer–Emmett–Teller model presented better fitting for the adsorption equilibrium, and the maximum adsorption capacities were 72.17 and 23.61 mg g − 1 for dimetridazole and metronidazole, respectively. The calculated values of ΔG 0 and ΔH 0 indicated the non-spontaneous and exothermic nature of the adsorption process at the range of temperature studied. Thermodynamic studies also revealed that physical and chemical adsorptions were co-action. The adsorption mechanisms of dimetridazole and metronidazole onto biochar were mainly hydrogen bonding and π–π interaction. All the results revealed that sugarcane bagasse biochar can be used as alternative to costly adsorbents for the removal of dimetridazole and metronidazole from aqueous solution.
研究领域:
环境科学
·
化学工程
✓ 已验证
产品关联
DOI
高影响因子
DYES AND PIGMENTS
·
2017
·
IF 3.473
Bin Jia,Hong Lian,Zheng Chen,Yi Chen,Jinhai Huang,Qingchen Dong
Two host materials TIC1 (N-linked carbazole) and TIC2 ( C-3 -linked carbazole) via changing the substitution position of carbazole , indole and thiazole moieties are reported. Their structural and physical properties were fully characterized. The thermal analysis demonstrated that both TIC1 and TIC2 are thermally stable. The triplet energy levels of TIC1 and TIC2 were determined to be 2.54 and 2.58 eV, respectively. Green and blue OLEDs with TIC1 and TIC2 acting as host materials were fabricated to investigate their performances in PHOLED . Both green and blue PHOLEDs based on TIC2 show the best performance with the maximum current efficiency and maximum power efficiency of 60.0 cd/A and 48.0 lm/W (for green), 18.4 cd/A and 15.2 lm/W (for blue), respectively. The characteristic measurements of OLED devices reveal that both TIC1 and TIC2 are promising host materials for practical application. By comparing with the commercial host material of 4,4′-bis(carbazol-9-yl)biphenyl (CBP) and N , N -dicarbazoyl-3,5-benzene (mCP), the power efficiency of green and blue PHOLED was enhanced by 55.3% and 245%, respectively.
研究领域:
材料科学
·
光学工程
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）