134847-73-7Relevant academic research and scientific papers
Discovery of Diphenoxy Derivatives with Flexible Linkers as Ligands for β-Amyloid Plaques
Jia, Jianhua,Zhang, Longfei,Song, Jia,Dai, Jiapei,Cui, Mengchao
, p. 4089 - 4100 (2020/12/13)
The highly rigid and planar scaffolds with π-conjugated systems have been widely considered to be indispensable for β-amyloid (Aβ) binding ligands. In this study, a library of diphenoxy compounds with different types of more flexible linkers as Aβ ligands were synthesized and evaluated. Most of them displayed good affinity (Ki1-42aggregates, and some ligands even showed values of Kiless than 10 nM. Structure-activity relationship analysis revealed that modification on the linkers or substituents tolerated great flexibility, which challenged the long-held belief that rigid and planar structures are exclusively favored for Aβ binding. Three ligands were labeled by iodine-125, and they exhibited good properties in vitro and in vivo, which further supported that this flexible scaffold was potential and promising for the development of Aβ imaging agents.
Diphenoxyl flexible molecules with high affinity with A[beta] plaque and preparation method and applications thereof
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Paragraph 0073; 0074; 0087; 0088, (2017/12/09)
The invention discloses diphenoxyl flexible molecules with high affinity with A[beta] plaque and a preparation method and applications thereof. After the molecules are labeled by radionuclide, the molecules can be used as an A[beta] plaque developing agen
Hybrid ortho/allosteric ligands for the adenosine A1 receptor
Narlawar, Rajeshwar,Lane, J. Robert,Doddareddy, Munikumar,Lin, Judy,Brussee, Johannes,Ijzerman, Adriaan P.
supporting information; experimental part, p. 3028 - 3037 (2010/09/07)
Many G protein-coupled receptors (GPCRs), including the adenosine A 1 receptor (A1AR), have been shown to be allosterically modulated by small molecule ligands. So far, in the absence of structural information, the exact location of
Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1
Folkes, Adrian,Brown,Canne, Lynne E.,Chan, Jocelyn,Engelhardt, Erin,Epshteyn, Sergey,Faint, Richard,Golec, Julian,Hanel, Art,Kearney, Patrick,Leahy, James W.,Mac, Morrison,Matthews, David,Prisbylla, Michael P.,Sanderson, Jason,Simon, Reyna J.,Tesfai, Zerom,Vicker, Nigel,Wang, Shouming,Webb, Robert R.,Charlton, Peter
, p. 1063 - 1066 (2007/10/03)
We have synthesized and evaluated a series of tetramic acid-based and hydroxyquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These studies resulted in the identification of several compounds which showed excellent potency against PAI-1. The design, synthesis and SAR of these compounds are described.
Bifunctional Reactivity of the Nitrophenoxyl Group in Intramolecular Photoreactions
Mutai, Kiyoshi,Tukada, Hideyuki,Nakagaki, Ryoichi
, p. 4896 - 4903 (2007/10/02)
The photochemical behavior of a homologous series of compounds, p-O2NC6H4O(CH2)nNHPh (n = 2-10, 12, and 16) in acetonitrile is reported.The lower (n = 2-6) homologues undergo an apparently nucleophilic type rearrangement to give ω-((p-nitrophenyl)amino)al
