A series of 3-Amantadinyl-2-[(4-amino-3-aryl-5-ylthio)-1,2,4-triazolo]methyl)quinazolin-4-one 5(a-i) were prepared by the reaction of 3-Amantadinyl-2-[(4-acetamido-3-aryl-5-ylthio)-1,2,4-triazolo]methyl)quinazolin-4-one 4(a-i) with various 3-aryl-4-acetamido-5-mercapto triazoles. The compounds 5(a-i) biologically evaluated for their antiinflammatory and antibacterial activities.Structures of th...

The specific deamidation of 2-acetamido-1,3,4,6-tetra-O-acetyl-alpha-D-glucopyranose is achieved by p-toluenesulfonic acid-promoted hydrolysis of 2-methyl-(3,4,6-tri-O-acetyl-1,2-dideoxy-alpha-D-glucopyrano)-[2,1 -d]-2- oxazoline 2 to give quantitative formation of the 1,3,4,6-tetra-O-acetyl-2-amino-2-deoxy-alpha-D-glucopyranose p-toluenesulfonate (5d). This two-step procedure provides an amino...

Several thymidine diphosphate sugar compounds have been isolated from Escherichia coli strains and other microorganisms. TDP-X, isolated from E. coli strain Y-10 by Strominger and Scott (1) and from other strains of E. coli (2) and TDP-X2 isolated from E. coli strain B, by Okazaki, Okazaki, and Kuriki (3) are unusual acetamido sugar-containing nucleotides (4). The sugars are 4-acetamido-4,6-did...

Proton magnetic resonance has been used to study the association of inhibitors and substrates with hen egg-white lysozyme. Changes in chemical shift, due to association, of acetamido methyl group resonances of the small molecules have been quantitated. This has allowed definition of magnetic parameters for three contiguous binding subsites on the enzyme surface. The relative modes of occupancy ...

Based on first principles and molecular mechanics calculations, we conclude that the mechanism of hevamine (a family 18 chitinase) involves an oxazoline ion intermediate stabilized by the neighboring C2' acetamido group. In this intermediate, the acetamido carbonyl oxygen atom forms a covalent bond to C1' of N-acetyl-glucosamine and has a transferred positive charge from the pyranose ring onto ...

Chalcones are very well known natural as well as synthetic compounds associated with diverse set of pharmacological activities. They have the potential to be developed as lead compounds for the discovery of antioxidant, anti-inflammatory and anticancer agents. Naturally occurring and synthetic chalcone compounds have shown safety profiles in clinical trials. To study impact of substitutions on ...

BACKGROUND The aim of our study was to determine the influence of routine ketone monitoring on hyperglycemic events (HE) and ketosis in youngsters with type 1 diabetes (T1D). METHODS Our single-site, controlled and randomized study was conducted on children and adolescents with T1D outside of remission phase. During two crossover periods of 6 months, patients (n = 22) experiencing HE tested k...

Three groups of male Wistar rats were pair fed NIH-31 diets for 14 days to which were added 30% of calories as corn starch, palm oil, or R-3-hydroxybutyrate-R-1,3-butanediol monoester (3HB-BD ester). On the 14th day, animal brains were removed by freeze-blowing, and brain metabolites measured. Animals fed the ketone ester diet had elevated mean blood ketone bodies of 3.5 mm and lowered plasma g...

The KEX2-encoded endoprotease was overproduced in yeast several hundred-fold and further purified to achieve a 10,000-fold enrichment in specific activity. The enzyme was (i) membrane-bound, but solubilized by detergents; (ii) able to cleave peptide substrates at both Lys-Arg and Arg-Arg sites; (iii) inhibited by EDTA and EGTA (but not o-phenanthroline), but fully reactivated by Ca2+; (iv) unaf...