30062-34-1Relevant academic research and scientific papers
Synthesis, opto-physics, and electroluminescence of cyclometalated iridium (III) complex with alkyltrifluorene picolinic acid
Wang, Yafei,Tan, Hua,Liu, Yu,Jiang, Chenxian,Hu, Zhengyong,Zhu, Meixiang,Wang, Lei,Zhu, Weiguo,Cao, Yong
, p. 1483 - 1488 (2010)
To improve the opto-physics, electroluminescence, and dispersibility of iridium (III) complexes in polymer light-emitting devices, we synthesized and characterized two red-emitting heteroleptic cyclometalated iridium (III) complexes of (Piq)2Ir(Tfl-pic) and (Piq)2Ir(Brfl-pic), in which Piq is 1-phenylisoquinoline, Tfl-pic and Brfl-pic are alkyltrifluorene- and dibromoalkylfluorene-containing picolinic acid derivatives bridged with alkoxy chain, respectively. Compared to (Piq)2Ir(pic) and (Piq)2Ir(Brfl-pic), (Piq)2Ir(Tfl-pic) exhibited higher thermal stability, better dispersibility and excellent quantum efficiency. High-efficiency red emission with a maximum current efficiency of 6.28 cdA-1 and a maximum EL peak at 608 nm was obtained in the (Piq)2Ir(Tfl-pic)-doped devices using a blend of poly(9,9-dioctylfluorene) and 2-(4-biphenyl)-5-(4-tert -butylphenyl)-1,3,4-oxadiazole as a host matrix.
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs
Xu, Mingshuo,Wang, Yu,Yang, Feipu,Wu, Chunhui,Wang, Zhen,Ye, Bin,Jiang, Xiangrui,Zhao, Qingjie,Li, Jianfeng,Liu, Yongjian,Zhang, Junchi,Tian, Guanghui,He, Yang,Shen, Jingshan,Jiang, Hualiang
, p. 606 - 611 (2018)
In previous study, a series of benzamides was identified as potent antipsychotic agents. As a continuation of the program to discover novel antipsychotics, herein we reported the evaluation of a series of pyridinecarboxamide derivatives. The most promising compound 7h not only held good activities on dopamine D2, serotonin 5-HT1A and 5-HT2A receptors, but also exhibited low potency for α1A, H1 and 5-HT2C receptors, indicating a low propensity of side effects like orthostatic hypotension and weight gain. Furthermore, 7h exhibited more potent antipsychotic-like effect than aripiprazole in behavioral studies. The preliminary results were promising enough for further research around this scaffold.
A multi-functional picolinohydrazide-based chemosensor for colorimetric detection of iron and dual responsive detection of hypochlorite
Kim, Cheal,Kim, Mingeun,Lee, Su Chan,Lim, Mi Hee,Yang, Minuk
, (2021)
A novel effective chemosensor HPHN, (E)-6-hydroxy-N′-((2-hydroxynaphthalen-1-yl)methylene) picolinohydrazide, was synthesized. HPHN sensed Fe3+/2+ with the changes of color from yellow to orange without obvious inhibition from other cations. In addition, HPHN could detect ClO? by both the color change from yellow to colorless and the fluorescence quenching. The binding modes of HPHN with Fe3+/2+ and ClO? were determined to be 1:1 with Job plot and ESI-mass analysis. HPHN displayed low detection limits of 0.29 μM for Fe3+ and 0.77 μM for Fe2+. For ClO?, the detection limit was 6.20 μM by colorimetric method and 3.99 μM by fluorescent one, respectively. Moreover, HPHN can be employed to quantify Fe3+ and ClO? in environmental samples and apply to cell imaging for ClO?.
Azacycle diketone compound and preparation method thereof (by machine translation)
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Paragraph 0275-0281, (2020/09/12)
The invention provides a azacyclodiketone compound which is characterized by being a compound represented by the following structure. The compound has inhibitory activity on cap-dependent endonuclease. (by machine translation)
KIF18A INHIBITORS
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Paragraph 0276, (2020/07/14)
Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
6-hydroxymethyl-1-phenylpyridine-2-ketone as well as preparation method and application thereof
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Paragraph 0027; 0030; 0031, (2017/08/29)
The invention relates to 6-hydroxymethyl-1-phenylpyridine-2-ketone as well as a preparation method and application thereof. With 2-carboxyl-6-pyridone as a starting material, a target compound is obtained through three-step reaction. The compound is a ver
Structure-activity relationships of small molecule autotaxin inhibitors with a discrete binding mode
Miller, Lisa M.,Keune, Willem-Jan,Castagna, Diana,Young, Louise C.,Duffy, Emma L.,Potjewyd, Frances,Salgado-Polo, Fernando,García, Paloma Engel,Semaan, Dima,Pritchard, John M.,Perrakis, Anastassis,MacDonald, Simon J. F.,Jamieson, Craig,Watson, Allan J. B.
supporting information, p. 722 - 748 (2017/02/05)
Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others. Many of the developed synthetic inhibitors for ATX have resembled the lipid chemotype of the native ligand; however, a small number of inhibitors have been described that deviate from this common scaffold. Herein, we report the structure-activity relationships (SAR) of a previously reported small molecule ATX inhibitor. We show through enzyme kinetics studies that analogues of this chemotype are noncompetitive inhibitors, and by using a crystal structure with ATX we confirm the discrete binding mode.
TRIAZOLE AGONISTS OF THE APJ RECEPTOR
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Paragraph 0328; 0329, (2016/12/07)
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures where the definitions of the variables are provided herein.
PYRAZOLYL-SUBSTITUTED PYRIDONE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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Paragraph 00413-00414, (2016/04/09)
There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.
ARYLHYDRAZIDES CONTAINING A 2-PYRIDONE MOIETY AS SELECTIVE ANTIBACTERIAL AGENTS
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Page/Page column 46-47, (2016/03/12)
The present invention belongs to the field of antibacterial agents, more specifically to antibacterials for treating Acinetobacter baumannii infections. The invention provides arylhydrazides containing a 2-pyridone moiety, according to formula (I), which
