A novel Bodipy-Dipyrrin fluorescent probe: Synthesis and recognition behaviour towards Fe (II) and Zn (II)
摘要:
We present the design, synthesis, characterization and spectral studies for a new Zn (II) and Fe (II) selective fluorescent probe, 4,4-Difluoro-8-{3-[(4-phenoxy-dipyrromethene)propoxy]}-4-bora-3a,4a-diazaindacene (DPYBODPY). DPBODPY consists of a terminal fluorophore and a selective ligand and was designed to detect significant changes in absorbance and/or fluorescence on metal ion binding. The fluorophore is based on the Bodipy unit due to its excellent photophysical properties, while the dipyrrin unit has specific recognition abilities for Fe2+ and Zn2+ ions. The combination of these two structures is optimised to achieve significant spectral changes in the presence of Fe2+ and Zn2+ ions. (C) 2012 Elsevier Ltd. All rights reserved.
A novel Bodipy-Dipyrrin fluorescent probe: Synthesis and recognition behaviour towards Fe (II) and Zn (II)
摘要:
We present the design, synthesis, characterization and spectral studies for a new Zn (II) and Fe (II) selective fluorescent probe, 4,4-Difluoro-8-{3-[(4-phenoxy-dipyrromethene)propoxy]}-4-bora-3a,4a-diazaindacene (DPYBODPY). DPBODPY consists of a terminal fluorophore and a selective ligand and was designed to detect significant changes in absorbance and/or fluorescence on metal ion binding. The fluorophore is based on the Bodipy unit due to its excellent photophysical properties, while the dipyrrin unit has specific recognition abilities for Fe2+ and Zn2+ ions. The combination of these two structures is optimised to achieve significant spectral changes in the presence of Fe2+ and Zn2+ ions. (C) 2012 Elsevier Ltd. All rights reserved.
Tethered indoles as functionalizable ligands for the estrogen receptor
作者:Bridget G. Trogden、Sung Hoon Kim、Shuyi Lee、John A. Katzenellenbogen
DOI:10.1016/j.bmcl.2008.11.043
日期:2009.1
To create ligands for the estrogen receptor that contain pendant groups for tethering to a poly(amido)amine (PAMAM) dendrimer, we have explored a class of N-substituted 2-phenyl indoles. Attachment of tethers of different length and chemical nature to this non-steroidal indole scaffold gave high affinity ligand-tether conjugates that can be easily functionalized. To further explore the utility of this system, an indole-conjugated dendrimer was prepared and evaluated as an estrogen receptor ligand. (C) 2008 Elsevier Ltd. All rights reserved.
[EN] NOVEL ANTAGONISTS OF THE GLUCAGON RECEPTOR<br/>[FR] NOUVEAUX ANTAGONISTES DU RÉCEPTEUR AU GLUCAGON
申请人:METABASIS THERAPEUTICS INC
公开号:WO2008098244A1
公开(公告)日:2008-08-14
[EN] The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistence and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same. [FR] La présente invention propose de nouveaux composés de formule (I) et les sels et co-cristaux pharmaceutiquement acceptables de ceux-ci qui ont une activité antagoniste ou agoniste inverse du récepteur au glucagon. La présente invention propose en outre des compositions pharmaceutiques les comprenant ainsi que des procédés de traitement, de prévention, de retardement de la durée avant la déclaration ou de réduction du risque de développement ou de progression d'une maladie ou d'une condition pour laquelle un ou plusieurs antagonistes du récepteur au glucagon est indiqué, y compris le diabète de type I et II, l'insulinorésistance et l'hyperglycémie. La présente invention propose également des procédés de préparation des composés de formule I, y compris les sels et co-cristaux de ceux-ci, et des compositions pharmaceutiques les comprenant.