26214-65-3Relevant articles and documents
Rational Development of Novel Activity Probes for the Analysis of Human Cytochromes P450
Sellars, Jonathan D.,Skipsey, Mark,Sadr-ul-Shaheed,Gravell, Sebastian,Abumansour, Hamza,Kashtl, Ghasaq,Irfan, Jawaria,Khot, Mohamed,Pors, Klaus,Patterson, Laurence H.,Sutton, Chris W.
, p. 1122 - 1128 (2016)
The identification and quantification of functional cytochromes P450 (CYPs) in biological samples is proving important for robust analyses of drug efficacy and metabolic disposition. In this study, a novel CYP activity-based probe was rationally designed and synthesised, demonstrating selective binding of CYP isoforms. The dependence of probe binding upon the presence of NADPH permits the selective detection of functionally active CYP. This allows the detection and analysis of these enzymes using biochemical and proteomic methodologies and approaches.
A new two-dimensional donor/acceptor copolymer based on 4,8-bis(2′-ethylhexylthiophene)thieno[2,3-f]benzofuran for high-performance polymer solar cells
Fan, Ling,Cui, Ruili,Guo, Xiuping,Qian, Dong,Qiu, Beibei,Yuan, Jun,Li, Yongfang,Huang, Wenlong,Yang, Junliang,Liu, Weifang,Xu, Xinjun,Li, Lidong,Zou, Yingping
, p. 5651 - 5659 (2014)
A new alkylthienyl substituted thieno[2,3-f]benzofuran (TBF)-based polymer (PTBFTDTBT) was synthesized and characterized. PTBFTDTBT had a high molecular weight, good solubility in common organic solvents, broad visible absorption from 300 to 750 nm, and a relatively deep highest occupied molecular orbital level (-5.2 eV). PTBFTDTBT also showed a field hole mobility up to the order of 10-2 using an organic field effect transistor (OFET) method and an order of 10-2 using a space-charge-limited current (SCLC) method. With the structure of indium tin oxide (ITO)/poly(3,4-ethylenedioxythiophene): polystyrene sulfonate/PTBFTDTBT:PC71BM (1:2, w/w)/Ca/Al, a power conversion efficiency of 6.42% was obtained with a high short circuit current (Jsc) of 13.51 mA cm-2 and fill factor (FF) of 61%, under the illumination of AM1.5G, at 100 mW cm-2, without any post-treatment. The study demonstrates that TBF is a promising building block for organic electronics. This journal is the Partner Organisations 2014.
Directed metalation cascade to access highly functionalized thieno[2,3-f ]benzofuran and exploration as building blocks for organic electronics
Aeschi, Yves,Li, Hui,Cao, Zhencai,Chen, Songjie,Amacher, Anneliese,Bieri, Nathalie,Oezen, Bilal,Hauser, Juerg,Decurtins, Silvio,Tan, Songting,Liu, Shi-Xia
, p. 5586 - 5589 (2013)
A tandem directed metalation has been successfully applied to the preparation of thieno[2,3-f]benzofuran-4,8-dione, providing an efficient and facile approach to symmetrically and unsymmetrically functionalize the thieno[2,3-f]benzofuran core at the 2,6 positions as well as to introduce the electron-withdrawing or -donating groups (EWG or EDG) at its 4,8 positions. The presence of various functional groups makes late-stage derivatization attainable.
Synthesis of a 4,8-dialkoxy-benzo[1,2-b:4,5-b′]difuran unit and its application in photovoltaic polymer
Huo, Lijun,Huang, Ye,Fan, Benhu,Guo, Xia,Jing, Yan,Zhang, Maojie,Li, Yongfang,Hou, Jianhui
, p. 3318 - 3320 (2012)
A new building block of benzo[1,2-b:4,5-b′]difuran (BDF) was firstly designed and synthesized. The newly designed unit was applied for constructing a new photovoltaic low band gap polymer, PBDFDTBT, which exhibited promising power conversion efficiency of 5.0%. The Royal Society of Chemistry 2012.
Benzamide compound and application thereof as herbicide
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Paragraph 0059; 0063-0065, (2021/06/12)
The invention discloses a benzamide compound and an application thereof as a herbicide. The compound is shown in a general formula (I) as shown in the specification, and each substituent group in the general formula I is defined in the specification. The
Design and synthesis of heteroaromatic-based benzenesulfonamide derivatives as potent inhibitors of H5N1 influenza A virus
Yu, Yongshi,Tazeem,Xu, Zhichao,Du, Liaoqi,Jin, Mengyu,Dong, Chune,Zhou, Hai-Bing,Wu, Shuwen
, p. 89 - 100 (2019/01/30)
Influenza A virus is an enveloped negative single-stranded RNA virus that causes febrile respiratory infection and represents a clinically challenging threat to human health and even lives worldwide. Even more alarming is the emergence of highly pathogenic avian influenza (HPAI) strains such as H5N1, which possess much higher mortality rate (60%) than seasonal influenza strains in human infection. In this study, a novel series of heteroaromatic-based benzenesulfonamide derivatives were identified as M2 proton channel inhibitors. A systematic investigation of the structure-activity relationships and a molecular docking study demonstrated that the sulfonamide moiety and 2,5-dimethyl-substituted thiophene as the core structure played significant roles in the anti-influenza activity. Among the derivatives, compound 11k exhibited excellent antiviral activity against H5N1 virus with an EC50 value of 0.47 μM and selectivity index of 119.9, which are comparable to those of the reference drug amantadine.
Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents
Sijm, Maarten,Siciliano de Araújo, Julianna,Ramos Llorca, Alba,Orrling, Kristina,Stiny, Lydia,Matheeussen, An,Maes, Louis,de Esch, Iwan J. P.,de Nazaré Correia Soeiro, Maria,Sterk, Geert Jan,Leurs, Rob
supporting information, p. 1662 - 1668 (2019/08/30)
Chagas disease is becoming a worldwide problem; it is currently estimated that over six million people are infected. The two drugs in current use, benznidazole and nifurtimox, require long treatment regimens, show limited efficacy in the chronic phase of infection, and are known to cause adverse effects. Phenotypic screening of an in-house library led to the identification of 2,2′-methylenebis(5-(4-bromophenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one), a phenyldihydropyrazolone dimer, which shows an in vitro pIC50 value of 5.4 against Trypanosoma cruzi. Initial optimization was done by varying substituents of the phenyl ring, after which attempts were made to replace the phenyl ring. Finally, the linker between the dimer units was varied, ultimately leading to 2,2′-methylenebis(5-(3-bromo-4-methoxyphenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one (NPD-0228) as the most potent analogue. NPD-0228 has an in vitro pIC50 value of 6.4 against intracellular amastigotes of T. cruzi and no apparent toxicity against the human MRC-5 cell line and murine cardiac cells.