4-azido-2-nitrophenyl albumin (ANP-albumin) was prepared by reacting 4-fluoro-3-nitrophenyl azide with albumin. The thermal decomposition kinetics of phenyl azide of ANP-albumin was studied at various temperatures by Fourier-Transform Infrared (FTIR) spectroscopy. The decomposition rate of the phenyl azide increased with temperature. The activation energy for the first-order decomposition of the phenyl azide was 128.0 kJ/mol. Albumin was grafted on to polypropylene (PP) films by thermolysis of the azido groups of ANP-albumin with no premodification of the PP surface. The albumin-grafted surface was characterized by electron spectroscopy for chemical analysis (ESCA) and by quantitative determination of platelet adhesion and activation. The bulk concentration of ANP-albumin used for adsorption varied from 0.001 to 30 mg ml-1, and the albumin-adsorbed PP films were incubated at 100 degrees C for up to 7 h. The carbon and nitrogen peaks resulting from the grafted albumin were used to compare the surface albumin concentrations as a function of the concentration of ANP-albumin in the adsorption solution. When the PP film was adsorbed with ANP-albumin at the concentration of 5 mg ml-1 or higher and incubated at 100 degrees C for longer than 5 h, the surface became resistant to platelet adhesion. The ANP-albumin can be grafted on to chemically inert surfaces such as PP surface through simple thermolysis of azido groups to prevent platelet adhesion and activation.
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http://dx.doi.org/10.1016/0142-9612(93)90060-f | DOI Listing |
J Nucl Med
January 2025
Center for Systems Biology, Massachusetts General Hospital, Boston, Massachusetts;
Radionuclides used for imaging and therapy can show high molecular specificity in the body with appropriate targeting ligands. We hypothesized that local energy delivered by molecularly targeted radionuclides could chemically activate prodrugs at disease sites while avoiding activation in off-target sites of toxicity. As proof of principle, we tested whether this strategy of radionuclide-induced drug engagement for release (RAiDER) could locally deliver combined radiation and chemotherapy to maximize tumor cytotoxicity while minimizing off-target exposure to activated chemotherapy.
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December 2024
Scientific and Production Center "Armbiotechnology" of NAS RA, 14 Gyurjyan Str, 0056, Yerevan, Armenia.
A synthesis of new enantiomerically enriched derivatives of (S)-α-aminopropionic acid, containing in the β-position 1,2,3-triazole groups coupled with a o-, m- and p-substituted phenyl residue, was developed based on Cu(I) catalyzed [3 + 2] cycloaddition of azides with alkynes. As the starting materials was used the square-planar Ni(II)complex of the Schiff base of propargylglycine with the chiral auxiliary BPB (Benzylprolylbenzophenone) and 1,4-substituted phenyl azides. The assignment of the (S)-absolute configuration of the α-carbon atom of the amino acid residue of the main diastereomeric complexes of the cycloaddition products was carried out on the basis of positive Cotton effects in the region of 480-580 nm of the circular dichroism spectra.
View Article and Find Full Text PDFMacromol Rapid Commun
November 2024
Laboratory of Organic and Macromolecular Chemistry (IOMC), Friedrich Schiller University Jena, Humboldtstr. 10, 07743, Jena, Germany.
The cyclooctyne-functionalized alcohol (1R,8S,9S)-bicyclo-[6.1.0]non-4-yn-9-ylmethanol (BCN-OH) is applied as initiator for the organo-catalyzed ring-opening polymerization (ROP) of morpholine-2,5-diones based on the l-amino acids valine, isoleucine, and phenylalanine.
View Article and Find Full Text PDFChem Asian J
November 2024
Department of Chemistry, Faculty of Science, Niigata University, Nishi-ku, Niigata, 950-2181, Japan.
Despite the significant development and extensive application of phthalocyanine and related azaporphyrins, little attention has been paid to meso-N-substituted azaporphyrinoids. Here, we report new derivatives of 5,10,20-triaryl-5,15-diazaporphyrinoids (ArDAP), which are reversibly redox-switchable between the 18π- and 19π-electron state. Four kinds of metal(II) complexes and free bases of ArDAP were prepared by metal-templated cyclization of metal(II) complexes of 5,10,15-triaryl-10-azabiladiene-ac with sodium azide or copper-catalyzed N-phenylation of 10,20-diaryl-5,15-diazaporphyrins (ArDAP) with diphenyliodonium hexafluorophosphate.
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November 2024
Department of Natural Products, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University Dammam 1982 Saudi Arabia.
We have designed 17 new 2-oxo-3-phenylquinoxalines the chemoselective Michael reaction of 3-phenylquinoxalin-2(1)-one with acrylic acid derivatives. The ester, ethyl 3-(2-oxo-3-phenylquinoxalin-1(2)-yl)propanoate, was reacted with hydroxylamine and hydrazine to produce -hydroxy-3-(2-oxo-3-phenylquinoxalin-1(2)-yl)propanamide and hydrazide, respectively. Further modifications were made through reactions with isothiocyanates and azide coupling with amines, yielding thiosemicarbazides and -alkyl derivatives.
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