91130-83-5Relevant academic research and scientific papers
Membrane Phospholipid Analogues as Molecular Rulers to Probe the Position of the Hydrophobic Contact Point of Lysophospholipid Ligands on the Surface of G-Protein-Coupled Receptor during Membrane Approach
Aoki, Junken,Inoue, Asuka,Ohwada, Tomohiko,Otani, Yuko,Sayama, Misa,Sekijima, Masakazu,Uwamizu, Akiharu
, p. 1173 - 1201 (2020/04/10)
When lipid mediators bind to G-protein-coupled receptors (GPCRs), the ligand first enters the lipid bilayer, then diffuses laterally in the cell membrane to make hydrophobic contact with the receptor protein, and finally enters the receptor's binding pock
Twist-bend nematic liquid crystals based on thioether linkage
Arakawa, Yuki,Komatsu, Kenta,Tsuji, Hideto
supporting information, p. 6786 - 6793 (2019/05/10)
We developed twist-bend nematogens based on cyanobiphenyl dimers with thioether or sulfur linkage, as opposed to the commonly used methylene and ether linkages. Based on the smaller bond angle of thioether C-S-C than methylene C-CH2-C and ether
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ENHANCER OF ZESTE HOMOLOG 2 POLYPEPTIDE
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Paragraph 1106; 1107; 1108; 1289, (2018/07/15)
The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
ANTI-ENTEROVIRUS 71 THIADIAZOLIDINE DERIVATIVE
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Paragraph 0143-0145, (2017/03/28)
Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof; and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD
Li, Peng,Yu, Jun,Hao, Fei,He, Haiying,Shi, Xuyang,Hu, Jiao,Wang, Li,Du, Chunyan,Zhang, Xiao,Sun, Ya,Lin, Fusen,Gu, Zhengxian,Xu, Deming,Chen, Xinsheng,Shen, Liang,Hu, Guoping,Li, Jian,Chen, Shuhui,Xiao, Wei,Wang, Zhenzhong,Guo, Qingming,Chang, Xiujuan,Tian, Xuyang,Lin, Tianwei
supporting information, p. 841 - 846 (2017/08/16)
Enterovirus 71 (EV71) is a major causative agent of hand, foot, and mouth disease (HFMD), which can spread its infections to the central nervous and other systems with severe consequences. The viral caspid protein VP1 is a well-known target for antiviral efficacy because its occupancy by suitable compounds could stabilize the virus capsid, thus preventing uncoating of virus for RNA release. In this Letter, design, synthesis, and biological evaluation of novel anti-EV71 agents (aminopyridyl 1,2,5-thiadiazolidine 1,1-dioxides) are described. One of the most promising compounds (14) showed excellent antiviral activity against EV71 (EC50 = 4 nM) and exhibited excellent in vivo efficacy in the EV71 infected mouse model.
Toward the discovery of dual HCMV-VZV inhibitors: Synthesis, structure activity relationship analysis, and cytotoxicity studies of long chained 2-uracil-3-yl-N-(4-phenoxyphenyl)acetamides
Babkov, Denis A.,Khandazhinskaya, Anastasia L.,Chizhov, Alexander O.,Andrei, Graciela,Snoeck, Robert,Seley-Radtke, Katherine L.,Novikov, Mikhail S.
, p. 7035 - 7044 (2015/11/11)
The need for novel therapeutic options to fight herpesvirus infections still persists. Herein we report the design, synthesis and antiviral evaluation of a new family of non-nucleoside antivirals, derived from 1-[ω-(4-bromophenoxy)alkyl]uracil derivatives - previously reported inhibitors of human cytomegalovirus (HCMV). Introduction of the N-(4-phenoxyphenyl)acetamide side chain at N3 increased their potency and widened activity spectrum. The most active compounds in the series exhibit submicromolar activity against different viral strains of HCMV and varicella zoster virus (VZV) replication in HEL cell cultures. Inactivity against other DNA and RNA viruses, including herpes simplex virus 1/2, points to a novel mechanism of antiviral action.
Design, synthesis, and anti-HCV activity of thiourea compounds
Kang, Iou-Jiun,Wang, Li-Wen,Lee, Chung-Chi,Lee, Yen-Chun,Chao, Yu-Sheng,Hsu, Tsu-An,Chern, Jyh-Haur
scheme or table, p. 1950 - 1955 (2009/11/30)
A series of thiourea derivatives were synthesized and their antiviral activity was evaluated in a cell-based HCV subgenomic replicon assay. SAR studies revealed that the chain length and the position of the alkyl linker largely influenced the in vitro anti-HCV activity of this class of potent antiviral agents. Among this series of compounds synthesized, the thiourea derivative with a six-carbon alkyl linker at the meta-position of the central phenyl ring (10) was identified as the most potent anti-HCV inhibitor (EC50 = 0.047 μM) with a selectivity index of 596.
Efficient halogen-lithium exchange reactions to functionalize poly(alkyl aryl ether) dendrimers
Nithyanandhan, Jayaraj,Jayaraman, Narayanaswamy
, p. 6228 - 6235 (2007/10/03)
Poly(alkyl aryl ether) dendrimers were functionalized with bromophenyl groups at their peripheries, so as to have 3, 6, 12, and 24 groups in the zero, first, second, and third generation dendrimers, respectively. The new bromophenyl functionalized dendrim
