127299-69-8Relevant academic research and scientific papers
Carbohydrate-Based Nanocarriers Exhibiting Specific Cell Targeting with Minimum Influence from the Protein Corona
Kang, Biao,Okwieka, Patricia,Sch?ttler, Susanne,Winzen, Svenja,Langhanki, Jens,Mohr, Kristin,Opatz, Till,Mail?nder, Volker,Landfester, Katharina,Wurm, Frederik R.
, p. 7436 - 7440 (2015)
Whenever nanoparticles encounter biological fluids like blood, proteins adsorb on their surface and form a so-called protein corona. Although its importance is widely accepted, information on the influence of surface functionalization of nanocarriers on the protein corona is still sparse, especially concerning how the functionalization of PEGylated nanocarriers with targeting agents will affect protein corona formation and how the protein corona may in turn influence the targeting effect. Herein, hydroxyethyl starch nanocarriers (HES-NCs) were prepared, PEGylated, and modified on the outer PEG layer with mannose to target dendritic cells (DCs). Their interaction with human plasma was then studied. Low overall protein adsorption with a distinct protein pattern and high specific affinity for DC binding were observed, thus indicating an efficient combination of "stealth" and targeting behavior.
VANCOMYCIN DERIVATIVE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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, (2019/03/13)
Provided are a class of vancomycin derivatives with a structure as shown in the general formula below and pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition containing the compound thereof, and the use of these compounds in preparing drugs for treating and/or preventing bacterial infection diseases, in particular drugs for treating infection diseases caused by Gram-positive bacteria.
Extra Sugar on Vancomycin: New Analogues for Combating Multidrug-Resistant Staphylococcus aureus and Vancomycin-Resistant Enterococci
Guan, Dongliang,Chen, Feifei,Xiong, Lun,Tang, Feng,Faridoon,Qiu, Yunguang,Zhang, Naixia,Gong, Likun,Li, Jian,Lan, Lefu,Huang, Wei
, p. 286 - 304 (2018/02/10)
Lipophilic substitution on vancomycin is an effective strategy for the development of novel vancomycin analogues against drug-resistant bacteria by enhancing bacterial cell wall interactions. However, hydrophobic structures usually lead to long elimination half-life and accumulative toxicity; therefore, hydrophilic fragments were also introduced to the lipo-vancomycin to regulate their pharmacokinetic/pharmacodynamic properties. Here, we synthesized a series of new vancomycin analogues carrying various sugar moieties on the seventh-amino acid phenyl ring and lipophilic substitutions on vancosamine with extensive structure-activity relationship analysis. The optimal analogues indicated 128-1024-fold higher activity against methicillin-susceptible S. aureus, vancomycin-intermediate resistant S. aureus (VISA), and vancomycin-resistant Enterococci (VRE) compared with that of vancomycin. In vivo pharmacokinetics studies demonstrated the effective regulation of extra sugar motifs, which shortened the half-life and addressed concerns of accumulative toxicity of lipo-vancomycin. This work presents an effective strategy for lipo-vancomycin derivative design by introducing extra sugars, which leads to better antibiotic-like properties of enhanced efficacy, optimal pharmacokinetics, and lower toxicity.
Preparation of aminoethyl glycosides for glycoconjugation
Sardzik, Robert,Noble, Gavin T.,Weissenborn, Martin J.,Martin, Andrew,Webb, Simon J.,Flitsch, Sabine L.
supporting information; experimental part, p. 699 - 703 (2011/01/03)
The synthesis of a number of aminoethyl glycosides of cell-surface carbohydrates, which are important intermediates for glycoarray synthesis, is described. A set of protocols was developed which provide these intermediates, in a short number of steps, from commercially available starting materials.
Synthesis and biological evaluation of mannose-6-phosphate-coated multivalent dendritic cluster glycosides
Srinivas, Oruganti,Radhika,Bandaru, Narasimha Murthy,Nadimpalli, Siva Kumar,Jayaraman, Narayanaswamy
, p. 4252 - 4257 (2007/10/03)
The synthesis of multivalent dendritic cluster glycosides of mannopyranosyl-6-phosphate is presented. Poly(amido amine)-based dendrimers of 0.5-3.5 generations, containing carboxylic acid peripheral functionalities, were utilized so as to install 4, 8, 16
Synthesis of carbohydrate-containing dendrimers. 5. Preparation of dendrimers using unprotected carbohydrates
Jayaraman, Narayanaswamy,Stoddart, J Fraser
, p. 6767 - 6770 (2007/10/03)
Carbohydrate-containing dendrimers have been prepared using completely unprotected carbohydrates employing a convergent growth approach. The facile syntheses of lower generation dendrimers, using the amide bond forming methodology, opens up the possibilit
