184916-28-7Relevant articles and documents
Synthesis of a novel amino acid based dendrimer
Mulders, Suzanne J.E.,Brouwer, Arwin J.,Van Der Meer, Peter G.J.,Liskamp, Rob M.J.
, p. 631 - 634 (1997)
An easy accessible dendrimer monomer 3,5-bis(2-tert-butyloxycarbonyl aminoethoxy) benzoic acid methyl ester 1 was designed. The monomer was converted to both the 'surface' and 'braching' monomer in a versatile synthesis of a novel amino acid based dendrimer by the covergent method, using the well established and high-yielding BOP-peptide coupling method.
Bioinspired Amphiphilic Peptide Dendrimers as Specific and Effective Compounds against Drug Resistant Clinical Isolates of E. coli
Sowińska, Marta,Laskowska, Anna,Gu?piel, Adam,Solecka, Jolanta,Bochynska-Czyz, Marta,Lipkowski, Andrzej W.,Trzeciak, Katarzyna,Urbanczyk-Lipkowska, Zofia
, p. 3571 - 3585 (2018/10/24)
Evolution-derived natural compounds have been inspirational for design of numerous pharmaceuticals, e.g., penicillins and tetracyclines. Herein, we present a bioinspired strategy to design peptide dendrimers for the effective therapy of E. coli infections where the selection of appropriate amino acids and the mode of their assembly are based on the information gained from research on membranolytic natural antimicrobial peptides (AMP's). On the molecular level two opposite effects were explored: the effect of multiple positive charges necessary for membrane disintegration was equilibrated by the anchoring role of tryptophanes. Indeed, a series of Trp-terminated dendrimers exhibited high potency against clinical isolates of antibiotic resistant ESBL E. coli strains, stability in human plasma along with very low hemo- and genotoxicity. Investigation of the underlying antimicrobial mechanism indicated that the dendrimers studied at minimal inhibitory concentration showed weak permeability toward membranes. Solid-state 2D NMR studies revealed their presence on and inside the model membranes. Therefore, their biological properties might be explained by targeting of extra- or intracellular receptors. Our results point to a new approach to design novel branched antimicrobials with high therapeutic index.
Tetramaleimide connexin and application thereof
-
Paragraph 0371; 0372; 0373; 0374, (2018/03/26)
The invention relates to tetramaleimide connexin and application thereof. Particularly, the invention relates to a compound shown as a formula I and application of the compound serving as connexin inpreparing antibody drug conjugate. The antibody drug con
DENDRONIZED METALLIC OXIDE NANOPARTICLES, A PROCESS FOR PREPARING THE SAME AND THEIR USES
-
Page/Page column 96; 97, (2015/11/30)
The present invention relates to dendronized metallic oxide nanoparticles, a process for preparing the same and their uses.
OPTICAL IMAGING PROBES
-
Paragraph 0087; 0092; 0093, (2014/05/20)
The present invention relates to methods of visualising cells especially although not exclusively in vivo using a dye, such as a dendrimer-dye molecule or polybranched-dye molecule which is internalised by the cells and thus permits subsequent visualisation by confocal fluorescence endomicroscopy or other optical detectors. There is also provided internally quenched probes for use in visualising cells especially although not exclusively in vivo by confocal fluorescence endomicroscopy and the use of internally quenched probes in combination with confocal fluorescence endomicroscopy, for visualising cells by virtue of internalisation and dequenching of a probe by the cells. In a particular embodiment the cells are activated neutrophils, such as within the lung of a subject.
Efficient synthesis of small-sized phosphonated dendrons: Potential organic coatings of iron oxide nanoparticles
Garofalo, Antonio,Parat, Audrey,Bordeianu, Catalina,Ghobril, Cynthia,Kueny-Stotz, Marie,Walter, Aurlie,Jouhannaud, Julien,Begin-Colin, Sylvie,Felder-Flesch, Delphine
supporting information, p. 5226 - 5239 (2014/12/10)
We report herein the synthesis of biocompatible small-sized phosphonated monomers and dendrons used as functional coatings of metal oxide nanoparticles, more specifically superparamagnetic iron oxides (SPIOs) for magnetic resonance imaging (MRI) and therapy through hyperthermia. The molecules were engineered to modulate their size, their hydrophilic and/or biocompatible character (poly(amido)amine versus oligoethyleneglycol), the number of anchoring phosphonate groups (monophosphonate versus phosphonic tweezers) and the number of peripheral functional groups for further grafting of dyes or specific vectors. Such a library of hydrophilic phosphonic acids opens new possibilities for the investigation of dendronized nanohybrids as theranostics.
Highly specific, multi-branched fluorescent reporters for analysis of human neutrophil elastase
Avlonitis, Nicolaos,Debunne, Manuelle,Aslam, Tashfeen,McDonald, Neil,Haslett, Chris,Dhaliwal, Kevin,Bradley, Mark
supporting information, p. 4414 - 4418 (2013/08/23)
Human neutrophil elastase (HNE) is a serine protease implicated in the pathogenesis of acute and chronic inflammatory disease. Here a series of, internally quenched, single fluorophore fluorescent reporters were synthesised that allowed the rapid, highly specific and sensitive analysis of HNE activity over closely related proteases. The Royal Society of Chemistry 2013.
Synthesis of bifunctional hydroxamic acids as novel ligands for the hydrophilic stabilization of iron oxide nanoparticles
Hofmann, Andreas,Graf, Christina,Kung, Shih-Hao,Kim, Myeongseob,Peng, Xiaogang,El-Aama, Randa,Ruehl, Eckart
experimental part, p. 1150 - 1158 (2010/06/13)
A general method for synthesizing bifunctional hydroxamic acids containing carboxylic acid or amino functionalities is reported. Various products from simple alkyl to complex dendrimer-like structures are described. Such molecules have recently been used in ligand-exchange reactions for the hydrophilic stabilization of originally oleic acid protected iron oxide nanoparticles. Georg Thieme Verlag Stuttgart · New York.
Synthesis of DOTA-conjugated multivalent cyclic-RGD peptide dendrimers via 1,3-dipolar cycloaddition and their biological evaluation: Implications for tumor targeting and tumor imaging purposes
Dijkgraaf, Ingrid,Rijnders, Anneloes Y.,Soede, Annemieke,Dechesne, Annemarie C.,Van Esse, G. Wilma,Brouwer, Arwin J.,Corstens, Frans H. M.,Boerman, Otto C.,Rijkers, Dirk T. S.,Liskamp, Rob M. J.
, p. 935 - 944 (2007/10/03)
This report describes the design and synthesis of a series of αVβ3 integrin-directed monomeric, dimeric and tetrameric cyclo[Arg-Gly-Asp-d-Phe-Lys] dendrimers using "click chemistry". It was found that the unprotected N-ε-azido derivative of cyclo[Arg-Gly-Asp-d-Phe-Lys] underwent a highly chemoselective conjugation to amino acid-based dendrimers bearing terminal alkynes using a microwave-assisted Cu(i)-catalyzed 1,3-dipolar cycloaddition. The αVβ 3 binding characteristics of the dendrimers were determined in vitro and their in vivo αVβ3 targeting properties were assessed in nude mice with subcutaneously growing human SK-RC-52 tumors. The multivalent RGD-dendrimers were found to have enhanced affinity toward the αVβ3 integrin receptor as compared to the monomeric derivative as determined in an in vitro binding assay. In case of the DOTA-conjugated 111In-labeled RGD-dendrimers, it was found that the radiolabeled multimeric dendrimers showed specifically enhanced uptake in αVβ3 integrin expressing tumors in vivo. These studies showed that the tetrameric RGD-dendrimer had better tumor targeting properties than its dimeric and monomeric congeners. This journal is The Royal Society of Chemistry.
Use of an acrylic dendron-containing monomer in the synthesis of a macroporous polymeric material
Khimich,Tennikova
, p. 623 - 627 (2007/10/03)
A procedure was developed for preparing a monolithic macroporous material by photoinitiated co-polymerization of glycidyl methacrylate, ethylene glycol dimethacrylate, and an acrylic comonomer containing a dendron with protected terminal amino groups. The
