Platelet aggregation inhibiting and anticoagulant effects of oligoamines, XX: 4,4',4'-(1,3,5)-benzene-tris-sydnone imines

The synthesis of ten tris-sydnone imine derivatives, unknown up to now, is described. All compounds are alkyl or arylalkyl substituted in 3-position of the sydnone imine. The most powerful agent was the 3-propyl derivative 6c. It inhibits the aggregation of human platelets induced by collagen in a concentration of 1 mumol/L half maximally. Its N-ethoxycarbonyl derivative 7c, which was designed as a prodrug, showed only small antithrombotic effects in rats. The reason for this low degree of activity is discussed.     

Modified surface-active monomers for adhesive bonding to dentin

PMGDM, a PMDM-type adhesive monomer, was synthesized from pyromellitic dianhydride and glycerol dimethacrylate. Only the para isomer of PMDM, a solid, is used in dental adhesives. The adhesive monomer PMGDM is a liquid and consists of a mixture of para- and meta isomers. This study shows that PMGDM has several advantages over PMDM. For example, the adhesive can be applied at a greater thickness, and additives and/or additional initiators for improved curing can be incorporated. Use of the liquid monomer PMGDM also provided a convenient means of varying the thickness of the adhesive layer between dentin and composite. The adhesive bonds were tested in both shear and tensile modes. PMDM was used as the control. The reliability of the bonds, as judged from the Weibull modulus and Weibull characteristic strength, was improved by (1) use of more concentrated solutions of PMGDM adhesive, (2) use of an adhesive thickness of about 25 microns, and (3) modification of PMGDM with a diluent monomer which is expected to enhance the degree of cure and/or the dentin-wetting properties of the adhesive resin.     

Two cell-wall-associated aminopeptidases from Lactobacillus helveticus and the purification and characterization of APII from strain ITGL1

Lactobacillus helveticus ITGL1 is able to hydrolyse many amino-acyl and dipeptidyl-p-nitroanilides. Analysis of heat inactivation kinetics, metal ion and protease inhibitor effects, and the subcellular location of aminopeptidase activities in both the parental strain and mutants deficient in lysyl-p-nitroanilide hydrolysis, led to the characterization of two cell-wall-associated aminopeptidases, APII and APIV. APII, which catalysed L-lysine p-nitroanilide hydrolysis, was purified about 28-fold to homogeneity from cell-wall extracts of L. helveticus ITGL1 and characterized. The purified enzyme appeared to be monomeric, with a molecular mass of 97 kDa. Aminopeptidase activity was greatest at pH 6.5 and 50 degrees C. APII was completely inhibited by bestatin, chelating agents such as EDTA or 1,10-phenanthroline and the divalent cations Zn2+ and Cu2+. The activity of the EDTA-treated enzyme was restored by Co2+, Ca2+ or Mn2+. Although APII was able to degrade several dipeptides and tripeptides with hydrophobic N-terminal amino acid (Leu, Ala), it was inactive on peptides containing Pro or Gly, and may thus contribute to the development of cheese flavour by processing bitter peptides.     

The use of patent titles for identifying the topics of invention and forecasting trends

Co-word analysis applied to patents through WPIL normalized title words appears to give a useful picture of a given field: we obtain both qualitative (themes) and quantitative information (weight of themes). It also gives information about the strategic aspects of the themes. Furthermore, in some cases, it is an indication of the future of certain themes that may help forecasting and management studies. Finally, it provides information about what could be a real technology growth process, in relation to the so-called translation model used in co-word analysis.     

A study of phase equilibria of nitrogen for constructing a medium value pressure scale

Translated from Izmeritel'naya Tekhnika, No. 3, pp. 40–42, March, 1993.