Quality Control of 2-(4-Aminophenyl)ethanol. Utsugi, Y; Kobuchi, H; Kawamura, Y; Atito, ASA; Nagao, M; Isoda, H; Miyamae, Y in [Utsugi, Yuki] Univ Tsukuba, Coll Agrobiol Resources Sci, Tsukuba, Ibaraki 3058572, Japan; [Utsugi, Yuki; Atito, Ahmed Salahelden Aboelhamd; Isoda, Hiroko; Miyamae, Yusaku] Univ Tsukuba, Sch Integrat & Global Majors, Masters Doctoral Program Life Sci Innovat, Tsukuba, Ibaraki 3058572, Japan; [Kobuchi, Hirona; Kawamura, Yukio] Kyoto Womens Univ, Fac Home Econ, Dept Food & Nutr, Kyoto 6058501, Japan; [Nagao, Masaya; Miyamae, Yusaku] Kyoto Univ, Grad Sch Biostudies, Kyoto 6068502, Japan; [Isoda, Hiroko] Univ Tsukuba, Alliance Res Mediterranean & North Africa, Tsukuba, Ibaraki 3058572, Japan; [Isoda, Hiroko; Miyamae, Yusaku] Univ Tsukuba, Fac Life & Environm Sci, Tsukuba, Ibaraki 3058572, Japan published Importance of the Proximity and Orientation of Ligand-Linkage to the Design of Cinnamate-GW9662 Hybrid Compounds as Covalent PPAR Agonists in 2019.0, Cited 27.0. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9.
Covalent agonists of PPAR cause unique receptor conformational changes and behave as selective PPAR modulators, whereas there are few covalent agonists other than endogenous unsaturated fatty acids metabolites. Previously, we established a cell-based strategy to identify new PPAR ligands and synthesized a new-type of covalent agonist that possesses the hybrid structure of a plant-derived cinnamic acid derivative and GW9662, a covalent antagonist. Herein, we report six analogues that differ in how the two fragments are linked together. Compounds with a simplified linker showed potent agonistic activity with improved EC50 values (less than 5 nM), indicating that close proximity between the two fragments improves binding affinity. When the position of cinnamic acid moiety was placed at 4 carbon of aniline ring, PPAR agonist activity was completely abolished. Docking studies suggested that the activation profile likely depends on interaction with the cavity around helix 3, -sheet, and -loop region in the ligand-binding domain. Furthermore, a cell-based assay revealed that agonist-type compounds activate PPAR transcription in a manner dependent on covalent linkage with the Cys285 residue leading to prolonged transactivation. This activation feature reflects pharmacological benefits of covalent drugs, suggesting that these hybrid compounds may serve as potential leads for a new-class of covalent PPAR ligands.
Quality Control of 2-(4-Aminophenyl)ethanol. Welcome to talk about 104-10-9, If you have any questions, you can contact Utsugi, Y; Kobuchi, H; Kawamura, Y; Atito, ASA; Nagao, M; Isoda, H; Miyamae, Y or send Email.
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