MOLECULES
·
2016
·Vol. 21
·期 3
·299
·
IF 2.465
Bo Jin,Rongzong Zheng,Rufang Peng,Shijin Chu
Five new bis(3-hydroxy-4-pyridinone) tetradentate chelators were synthesized in this study. The structures of these tetradentate chelators were characterized by1H-NMR,13C-NMR, FT-IR, UV-vis, and mass spectral analyses. The binding abilities of these tetradentate chelators for uranyl ion at pH 7.4 were also determined by UV spectrophotometry in aqueous media. Results showed that the efficiencies of these chelating agents are dependent on the linker length. Ligand4bis the best chelator and suitable for further studies.Keywords:chelating agent;3-hydroxy-4-pyridinone;uranium;tetradentate chelator
研究领域:
化学
·
环境科学
✓ 已验证
DOI
PubMed
高影响因子
TETRAHEDRON
·
2024
·
IF 2.1
Nan Wang,Yuanyuan Huang,Mengke Wang,Weichun Huang,You Zi
Herein, a new approach for the synthesis of ( Z )- N -alkenyl-2-pyridones from 2-pyridones and propiolates using phosphine catalysis under mild conditions is reported. This dual Z -diastereoselective and N -selective reaction demonstrates excellent selectivity, yielding sole ( Z )- N -alkenyl-2-pyridones. Furthermore, scale-up studies confirm its practical applicability, with consistent efficiencies observed.
研究领域:
有机化学
·
合成化学
✓ 已验证
DOI
高影响因子
MOLECULES
·
2021
·Vol. 26
·期 7
·1925
·
IF 4.412
Xiao-Qiang Jiang,Shi-Quan Chen,Yan-Fei Liu,Xin-Guang Pan,Dan Chen,Shi-Fan Wang
Solvothermal synthesis of multiple dihydropyrimidinones at a time has been developed in inexpensive and green bio-based solvent lactic acid without any additional catalysts or additives. By this method, thirty new dihydropyrimidinone derivatives were synthesized in two batches and characterized. All of the compounds were screened by Eg5 motor protein ATPase assay, and the positive compounds were tested against the Caco-2 cell line, HeLa cell line, L929 cell line and T24 cell line in vitro. Among them, compound C9 exhibited the best inhibitory activity against motor protein ATPase with an IC50value of 30.25 μM and significant cytotoxic activity in the micromolar range against the cells above. The Lineweaver–Burk plot revealed that compound C9 was a mixed-type Eg5 inhibitor. A molecular modeling study using the Discovery Studio program was performed, where compound C9 exhibited good binding interaction with Eg5 motor protein ATPase, and this was consistent with the attained experimental results.
研究领域:
药物化学
·
肿瘤学
·
合成化学
✓ 已验证
DOI
高影响因子
DYES AND PIGMENTS
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2017
·
IF 3.473
Xiao-Lei Zhao,Hui-Fen Qian,Wei Huang
A family of bi-heterocyclic dyes have been first synthesized by using heterocyclic pyridone and benzothiazole components. UV−Vis spectral analyses reveal distinct spectral behaviors depending on the introduced electron-withdrawing and electron-donating groups in the benzothiazol ring as well as the polarity of solvents. Namely, nitrobenzothiazol based bi-heterocyclic dyes display more obvious solvatochromism compared with both methylbenzothiazol based ones and previously reported azobenzene based half-heterocyclic pyridone dyes. More interestingly, 1 H NMR and UV−Vis spectral results as well as single-crystal structures manifest that these dyes are in the hydrazone form in the solid state and in the non-polar solvents. However, they adopt dominating azo form in polar solvents and it can be transformed to the hydrazone form in the acidic condition, which are both different from all known half-heterocyclic pyridone dyes. In addition, transformation from hydrazone to deprotonated azo form can be achieved via metal-ion complexation, and four Ni II and Cu II complexes with different pyridone N -tails have been structurally characterized. It is noted that the ligands adopt different tridentate coordination fashions with Ni II and Cu II ions and a rare tetranuclear Cu II complex with equal Cu⋯Cu separation is obtained.
研究领域:
有机化学
·
配位化学
✓ 已验证
DOI
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2019
·Vol. 34
·期 3
·e5454
·
IF 3.259
Ningbo Li,Yijun Wang,Feijun Liu,Xin Zhao,Xinhua Xu,Quan An,Keming Yun
An air-stable complex of zirconium (IV)-salophen perfluorooctanesulfonate ( 1 ) was successfully synthesized by reacting Zr (salphen)Cl 2 and C 8 F 17 SO 3 Ag. Complex 1 was characterized and studied by different techniques (NMR, IR, HRMS, TG-DSC, conductivity and acidity measurements), and was found to be air-stable, water tolerant, thermally stable and strongly Lewis-acidic. Complex 1 exhibited high catalytic efficiency for the synthesis of 3,4-dihydropyrimidin-2-(1H)-ones/thiones via the Biginelli reaction of aldehydes, 1,3-dicarbonyl compounds and urea/thiourea under solvent-free conditions. Furthermore, complex 1 could be reused 5 times with minimal changes in catalytic efficiency. Compared with previously reported methods, the important features of this protocol are the solvent-free conditions, the short reaction times, the wide substrate compatibility, the high efficiency and the good reusability.
研究领域:
化学
·
催化科学
✓ 已验证
DOI
高影响因子
RESEARCH ON CHEMICAL INTERMEDIATES
·
2012
·Vol. 38
·期 7
·1699-1705
·
IF 0.697
Xie Wen Lin,Xiao Chuang Ping,Xie Ling,Zhou Ying,Li Xue Feng,Tang Xu Fu,Yuan Chun Tao,Qiu Ming Hua
4 - Substituted 3-hydroxy-2(1 H )-pyridinones 2 were prepared by Mannich reaction of 3-hydroxy-2(1 H )-pyridinones with secondary amines and formaldehyde. The isolated products were then reacted with aromatic amines in the presence of NaIO 3 as oxidant via oxidation–Michael addition to yield 4,5,6-trisubstituted-2,3-pyridinediones 3 in good yields (80.2–88.9%). The structures of the products were characterized by 1 H NMR, ESI-MS, and IR, and elemental analysis.
研究领域:
有机化学
·
药物化学
✓ 已验证
DOI
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2017
·
IF 5.401
Tingting Luo,Yiqi Li,Yanxue Xu,Shiting Zhang,Yujue Wang,Xingming Kou,Dan Xiao
In this article, a hyperfluorescence 2-pyridone derivative (D-TPCA) has been synthesized within 5 min by the microwave-assistant heat treatment of the aqueous mixture of citric acid and 2-aminoethanethiol hydrochloride. The as-prepared D-TPCA exhibited good aqueous solubility and excellent fluorescent property with a quantum yield of 89.9%. Because the fluorescence of D-TPCA could be effectively quenched by picric acid (PA), D-TPCA could be served as a “turn-off” fluorescence sensor for PA in aqueous solution. The proposed sensing method permitted a selective and sensitive detection of PA in a linear range of 0–45 μM with a detection limit of 56.0 nM. The determination results of PA in real water samples with a recovery range of 95.4–107.3% confirmed a good analytical performance of this sensor. In addition, the possible sensing mechanism has been discussed in detail.
研究领域:
分析化学
·
材料科学
✓ 已验证
DOI
高影响因子
LETTERS IN ORGANIC CHEMISTRY
·
2023
·Vol. 20
·期 12
·1159-1169
·
IF 0.8
Yaghoubi Fatemeh,imanzadeh Gholamhassan,Asgharzadeh Roghayyeh,Soltanzadeh Zahra,Öztürk Turan
Dihydropyrimidines are one of the most important heterocyclic ring systems having a serious place in medicinal and organic synthesis. In this paper, a new series of dihydropyrimidines consisting of sulfur atoms were synthesized using inorganic base K2CO3 and TBAB as an organic salt
to make high polarity in reaction media. Interestingly, different 3,4-dihydropyrimidin-2(1H)-thiones reacted smoothly with various acrylic esters to afford adducts viahighly regioselective N3-Michael addition reaction was carried out at 100°C in 12 h. result: Unfortunately, the
reaction failed with fumaric esters owing steric effects. Avoiding organic solvents during this reaction effectively led to the development of an economic approach. Structures of the new compounds were established on the basis of 1H NMR, 13C NMR, and IR spectral data.
研究领域:
有机化学
·
药物化学
✓ 已验证
DOI
高影响因子
Materials Express
·
2024
·Vol. 14
·期 5
·734-739
·
IF 0.7
Chen Zhi,Wen Di
Osteoarthritis considerably affects the daily activities of humans and pets. Medication is an effective treatment option for osteoarthritis. However, commonly used medications require frequent injections or oral administration, which may cause side effects such as gastrointestinal reactions,
drug overdose, and missed doses. In this study, we developed lubricative drug-releasing microspheres based on poly(lactic-co-glycolic acid) (PLGA), for the treatment of osteoarthritis. PLGA microspheres formed using microfluidic electronic technology have uniform spherical morphology, sufficient
biocompatibility, and excellent drug-release performance. Animal experiments in rabbits have shown that flavopiridol-loaded PLGA is an effective drug carrier for osteoarthritis treatment, since it promotes glycosaminoglycan deposition. Therefore, our flavopiridol-loaded lubricating microspheres
is anticipated to exhibit considerable potential for osteoarthritis treatment in humans and pets.
研究领域:
药学
·
生物医学工程
·
动物医学
✓ 已验证
DOI
高影响因子
JOURNAL OF MEMBRANE SCIENCE
·
2022
·
IF 10.53
Sher Ayaz,Zi-Ying Yao,Ya-Jun Chen,Hai-Yin Yu
As a key constituent of anion exchange membrane fuel cells, anion exchange membrane (AEM) faces a tough challenge to withstand the nucleophilic (OH − ) attack on central cation in alkaline atmosphere which causes a constant degradation and thus affects the long term performance of the AEM. Aromatic cations unlike aliphatic amine cations are resistant to Hofmann β-elimination, however due to planar geometry they are more vulnerable to nucleophilic substitution reaction . To understand the problem and to formulate a mechanism to protect the AEM, a series of cationic membranes was fabricated based on poly(arylene ether ketone) having pendant quaternized derivatives of pyrimidinium and pyridazinium cations employing DCC-coupling reaction. The chemical structure characterization of the target products was conducted by 1 H NMR and FT-IR spectroscopy. Various physicochemical properties of the membranes were investigated including thermomechanical behavior, ion exchange capacity, water uptake, swelling ratio, ionic conductivity , fuel cell performance and oxidative and chemical stabilities. No serious swelling was observed with adequate water uptake at temperature between 20 °C and 80 °C. The membranes with both pyrimidinium and pyridazinium cations exhibited sufficient ionic conductivity . The highest recorded conductivity was 45.7 mS cm −1 and peak power density was 194 mW cm −2 . The oxidative stability of all membranes was high (more than 90%) however, alkaline stability results suggest a different behavior. Pyridazinium cations with substituents simultaneously at C-3 and C-6 positions is thoroughly protected from OH − attack while pyrimidinium (simultaneously protected at C-4 and C-6 positions) degraded at accelerated rate with raising temperature. This work not only explores the possibility of utilizing aromatic cations that weren't used before but also provides a wider understanding of the relationship of aromatic cation structure and membrane stability and performance thus helping in designing stable anion exchange membranes for long-lasting fuel cells.
研究领域:
材料科学
·
化学工程
·
能源科学
✓ 已验证
DOI
高影响因子
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
·
2020
·
IF 4.673
L. Ravithej Singh,Yu-Lin Chen,Yuan-Yuan Xie,Wei Xia,Xing-Wen Gong,Robert C. Hider,Tao Zhou
In an attempt to synthesise new tyrosinase inhibitors, we designed and synthesised a series of chalcone-hydroxypyridinone hybrids as potential tyrosinase inhibitors adopting strategic modifications of kojic acid. All the newly synthesised compounds were characterised by NMR and mass spectrometry. Initial screening of the target compounds demonstrated that compounds 1a, 1d, and 1n had relatively strong inhibitory activities against tyrosinase monophenolase, with IC50 values of 3.07 ± 0.85, 2.25 ± 0.8 and 2.75 ± 1.19 μM, respectively. The inhibitory activity against monophenolase was 6- to 8-fold higher than that of kojic acid. Compounds 1a, 1d, and 1n also showed inhibition of diphenolase, with IC50 values of 17.05 ± 0.07, 11.70 ± 0.03 and 19.3 ± 0.28 μM, respectively. The inhibition kinetics of diphenolase indicates that compounds 1a and 1d induce reversible inhibition on tyrosinase. Finally, we found that copper coordination should be one of the important inhibitory mechanism of these compounds in tyrosinase.
研究领域:
药物化学
·
生物化学
✓ 已验证
DOI
高影响因子
Food and Bioprocess Technology
·
2017
·Vol. 10
·期 12
·2146-2155
·
IF 2.576
Chen Kai,Zhao De-Yin,Chen Yu-Lin,Wei Xiao-Yi,Li Yin-Ting,Kong Li-Min,Hider Robert C.,Zhou Tao
In order to search for a new method for the anti-browning of food products, a novel hydroxypyridinone (HPO) derivative with a formyl group was evaluated for its anti-tyrosinase property. This compound was found to exhibit potent tyrosinase inhibition on the monophenolase activity of mushroom tyrosinase with an IC 50 value of 1.33 μM, indicating that this HPO derivative was 12-fold stronger than kojic acid (IC 50 15.89 μM). This molecule can inhibit tyrosinase via two action modes, namely copper reduction and chelation, and the formation of a Schiff’s base with the amino group at the active site of the enzyme. A synergistic effect of these two action modes to enhance the inhibitory activity was observed. This compound was also investigated for the inhibitory effect on diphenolase activity of mushroom; the inhibitory mechanism was found to be reversible and of competitive-uncompetitive mixed-type inhibition. This hydroxypyridinone was demonstrated to effectively control the browning of vegetable products.
研究领域:
生物化学
·
食品科学
·
分子生物学
·
药物设计
·
酶学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）