Search results for "Spar"
showing 10 items of 1739 documents
A practical entry to β-aryl-β-alkyl amino alcohols: application to the synthesis of a potent BACE1 inhibitor
2012
The 1,2-addition of alkyl Grignard reagents to readily available N-tert-butanesulfinyl ketimines, bearing an α-silyloxy substituent, proceeds in high yields and excellent diastereocontrol. The utility of the present method was demonstrated by the synthesis, in enantiomerically pure form, of one recently disclosed β-secretase (BACE1) inhibitor.
Influence of functionalization on interaction and drug release from α,β-polyaspartylhydrazide derivatives to a biomembrane model: evaluation by diffe…
2004
Abstract A comparative study on the ability of various polymers to interact with a biomembrane model was carried out by differential scanning calorimetry (DSC). The investigated samples were a water soluble polymer, the α,β-polyaspartylhydrazide (PAHy) and its derivatives containing polyethylene glycol (PEG2000) (sample PAHy–PEG2000), or hexadecylamine (C16) (sample PAHy–C16) or both compounds (sample PAHy–PEG2000–C16). Some samples are able to arrange themselves as micellar structures and to interact potentially with the membrane surface so as to favor the release of the drug near the target membrane and consequently to improve drug adsorption processes. First, the interaction of all polym…
Synthesis of C1-[18F]fluoroethylamnino asparagine for imaging cancer
2001
C1-[18F]fluoroethylamino asparagine was synthesised from N1-t-boc C1-p-nitrophenol asparagine and the radiolabelled precursor [18F]flouroethylamine in a one-pot-synthesis. The yield of this synthesis was 22% referring to [18F]fluoride, including the removal of the protection groups. The in vivo tests are in progress.
Thermal inactivation at high temperatures and regeneration of green asparagus peroxidase
2019
A spectrophotometric method was developed for determining the peroxidase activity of green asparagus in small samples. The optimum conditions for the analysis in the cuvette were 45 mM of H2O2 36 mM of guaiacol, and pH 7. The method can be used to determine enzyme activity at up to two decimal reductions. A study was performed of the regeneration and inactivation kinetics of the enzyme when heated between 90 and 125°C. Regenerated asparagus peroxidase reached its maximum activity after being stored 6 days at 25°C. The regenerated enzyme followed first-order inactivation kinetics, showing an Ea = 13.62 kcal/mol and k100°C = 2.07 min-1.
Synthese von geschützten Asparagin-Glycopeptiden durch N-terminale Peptidketten- Verlängerung. _ Teilsequenzen der Rinder-Desoxyribonuclease A und de…
1983
N-[2-(Triphenylphosphonio)ethoxycarbonyl] -[Peoc-]asparaginsaure-benzylester (8h) und -tert-butylester (8i) werden mit 2-Acetamido-3,4,6-tri-O-acetyl-2-desoxy-β -D-glucopyranosylamin (2) zu den N4-Glycosylasparagin-Derivaten 19 verknupft. Aus diesen kann die Peoc-Gruppe selektiv mit Diethylamin/tert-Butylalkohol oder Morpholin/Methylendichlorid abgespalten werden, wobei in den entstandenen N4-Glycosylasparaginestern 22 alle anderen Schutzgruppen und die glycosidische Bindung erhalten bleiben. Durch Kondensation von 22 mit Peoc-Aminosauren 8 entstehen die voll geschutzten N4-Glycosylasparagin-Dipetide 24 und 30. Bei Kondensation der N2 deblockierten N4-Glycosylasparaginester 22 mit den Peoc-…
o-Boronato- and o-Trifluoroborato-Phosphonium Salts Supported by L-α-Amino Acid Side Chain.
2015
The synthesis of o-boronato- and o-trifluoroborato-phosphonium salts supported by the L-amino acid side chain is described. The synthesis of these new class of amino acid derivatives was achieved by stereoselective quaternization of o-(pinacolato)boronatophenylphosphine with β- or γ-iodo amino acid derivatives which are prepared from L-serine or L-aspartic acid, respectively. The quaternization of the phosphine was performed using either iodo amino ester or carboxylic acid derivatives. In addition, free carboxylic acid and amine derivatives were obtained by saponification or HCl acidolysis of o-boronato-phosphonium amino esters, respectively. The usefulness of these compounds in peptide cou…
Chemical conjugation of dexamethasone to a polyaspartamide and in vitro evaluation studies
2004
Two macromolecular conjugates of dexamethasone containing different drug amounts were synthesized using PHEA as the polymeric carrier and a succinic group as spacer. The content of linked drug was equal to 25.3% w/w (conjugate A) and 12.7% w/w (conjugate B). Both polymeric conjugates, unlike the free drug, were water-soluble and the amount of unlinked drug was evaluated to be approximately about 0.01% w/w. Both conjugates were relatively stable in vitro at pH 7.4 whereas in the presence of esterase only the conjugate B was able to release drug under the used experimental conditions. This dissimilar behavior has been attributed to the distinct macromolecular conformations assumed in aqueous …
N-glycosylation efficiency is determined by the distance to the C-terminus and the amino acid preceding an Asn-Ser-Thr sequon
2010
N-glycosylation is the most common and versatile protein modification. In eukaryotic cells, this modification is catalyzed cotranslationally by the enzyme oligosaccharyltransferase, which targets the β-amide of the asparagine in an Asn-Xaa-Ser/Thr consensus sequon (where Xaa is any amino acid but proline) in nascent proteins as they enter the endoplasmic reticulum. Because modification of the glycosylation acceptor site on membrane proteins occurs in a compartment-specific manner, the presence of glycosylation is used to indicate membrane protein topology. Moreover, glycosylation sites can be added to gain topological information. In this study, we explored the determinants of N-glycosylati…
Mechanical Characterization of Polysaccharide/polyaminoacid Hydrogels as Potential Scaffolds for Tissue Regeneration
2011
The mechanical properties of hydrogel scaffolds based on hyaluronic acid (HA) that were chemically crosslinked with α,β-poly(N-2-hydroxyethyl)(2-aminoethylcarbamate)-D,L-aspartamide (PHEA-EDA) were investigated. Variation of these properties as a function of three different PHEA-EDA amounts used to crosslink HA has been related to the reaction efficiency evaluated using a colorimetric assay. Moreover, the amount of unreacted amino groups that was still present in the hydrogels was related to the attachment behavior of human dermal fibroblasts to the hydrogel surface. The mechanical data and biological results suggest the suitability of the investigated hydrogels as scaffolds for the regener…
pH-sensitive hydrogel based on a novel photocross-linkable copolymer.
2004
A pH sensitive hydrogel has been prepared by a UV irradiation technique. Starting polymer was the PHM (poly hydroxyethylaspartamide methacrylated) obtained from polyaspartamide (PHEA) partially derivatized with methacrylic anhydride (MA). This new copolymer has been further derivatized with succinic anhydride (SA) to obtain PHM-SA that has been cross-linked by UV irradiation to form a pH sensitive hydrogel. The network, recovered after washing as a powder, has been been characterized by FT-IR spectrophotometry and particle size distribution analysis. Moreover, to have information about water affinity of the prepared sample, swelling measurements have been carried out in aqueous media mimick…