Synthesis of GN8 derivatives and evaluation of their antiprion activity in TSE-infected cells
摘要:
A series of GN8 derivatives were synthesized from various diamines, carboxylic acid derivatives, and nitrogen nucleophiles, and their antiprion activity was tested in TSE-infected mouse neuronal cells. We found that two ethylenediamine units, hydrophobic substituents on the nitrogen atoms, and the diphenylmethane scaffold were essential structural features responsible for the activity. Seven derivatives bearing substituents at the benzylic position exhibited an improved antiprion activity with the IC50 values of 0.51-0.83 mu M. Conformational analysis of model compounds suggested that the introduction of the substituent at the benzylic position restricted the conformational variability of the diphenylmethane unit. (C) 2011 Elsevier Ltd. All rights reserved.
[EN] BIS(2-HALOACETAMIDO)-COMPOUNDS FOR USE AS LINKING AGENTS AND RESULTANT PRODUCTS WHICH COMPRISE ANTIBODIES, HALF-ANTIBODIES AND ANTIBODY FRAGMENTS [FR] COMPOSÉS BIS(2-HALOACÉTAMIDO) DESTINÉS À ÊTRE UTILISÉS EN TANT QU'AGENTS DE LIAISON ET PRODUITS RÉSULTANTS QUI COMPRENNENT DES ANTICORPS, DES DEMI-ANTICORPS ET DES FRAGMENTS D'ANTICORPS
Coordination Behavior of
<i>N</i>
,
<i>N′</i>
‐Bis(diisopropylphosphinoacetyl)‐
<i>o</i>
‐phenylenediamide with Ni
<sup>II</sup>
and Cu
<sup>I</sup>
Ions
The reaction of N,N′-bis(diisopropylphosphoniumacetyl)-o-phenylenediamide dibromide (H4L·2Br) with NiII[ClO4]·6H2O in the presence of Et3N resulted in the formation of N,N′-bis(diisopropylphosphinoacetyl)-o-phenylenediamidate nickel(II) ([NiII(L)]). The single-crystal X-ray diffraction analysis of [NiII(L)] revealed that each pair of N and P atoms in L2– coordinates in a tetradentate fashion to afford
Provided herein are, inter alia, methods for linking an mRNA molecule to a polypeptide (e.g., a peptide or a protein) by linking the mRNA molecule to a linking amino acid in the polypeptide, or by linking the mRNA molecule to a linking tRNA to which the polypeptide is attached, via reactions not catalyzed by the ribosome, and methods for making polypeptide libraries. Also provided are mRNA-protein complexes and mRNA-tRNA-protein complexes, libraries containing these complexes, and methods of using these complexes.
Method of catalytic crosslinking of polymers and two-pack composition used therein
申请人:ROHM AND HAAS COMPANY
公开号:EP0950669A2
公开(公告)日:1999-10-20
A method of crosslinking an oxidative polymer having oxidatively crosslinkable functional groups and a two-pack composition used therein. The oxidatively crosslinkable functional groups on the oxidative polymer are crosslinked by contacting the oxidative polymer with a catalytic amount of an oxidizing enzyme, such as horseradish peroxidase. The present invention is further directed to a two-pack coating composition which includes a polymeric component and a catalytic component, which are mixed together prior to use.
NEW AMIDE DERIVATIVES OF CINCHONA ALKALOIDS, METHOD FOR THE PREPARATION THEREOF AND USE THEREOF IN ASYMMETRIC PHASE TRANSFER REACTIONS
申请人:Instytut Chemii Organicznej Polskiej Akademii Nauk
公开号:EP3705479A1
公开(公告)日:2020-09-09
The object of the invention relates to a Cinchona alkaloid amide derivative of Formula 1 and Formula 3. The invention also relates to methods for the preparation of the Cinchona alkaloid amide derivative of Formula 1 and Formula 3, as well as its application as a catalyst in an asymmetric reaction under phase transfer conditions (PTC).