Cyclic guanidines. XVI. Synthesis and biological activities of tetracyclic imidazo[2,1-b]quinazolinone derivatives.
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Biomedical subjects
Publications and source records attributed to F Ishikawa.
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The presence of activated oncogenes in several rat hepatocellular carcinomas induced by 2-amino-3-methylimidazo[4,5-f]-quinoline (IQ) was examined by NIH 3T3 cell transfection assay and Southern blot analysis. In one tumor, IQ4, rat H-ras-1 and another oncogene that did not belong to the ras family were found to be activated.
A peptide was obtained from culture filtrates of a bacterium which was newly isolated and tentatively named Bacillus cereus SW. The peptide was composed of Asx, Ser, Glx, Leu, Tyr, Pro, and an unknown amino acid in a ratio of 2:1:1:1:1:1:1, but, unless hydrolyzed with HCI, it was ninhydrin reaction negative. The peptide effectively inhibited the growth of all fungi and yeasts so far examined, whereas it inhibited none of the bacteria tested.
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A method was devised for enzyme labeling goat antibody to rabbit immunoglobulin G with beta-D-galactosidase (EC 3.2.1.23) using a heterobifunctional cross-linker, N-(gamma-maleimidobutyryloxy)-succinimide. Labeling of the purified antibody was by a continuous 2-step process and including a chromatographic purification procedure could be completed within one day. The partially purified anti-rabbit IgG was coated on Amino-Dylark cylinders, a new solid support, using glutaraldehyde as the coupling reagent. With enzyme-labeled antibody and the solid-phase anti-rabbit IgG, a sandwich enzyme immunoassay for rabbit IgG was developed with a lower limit of detection at 3.5 pM (0.1 ng/tube). The specificity of the assay was excellent and all 4 types of IgG tested showed 0.0001% or less cross-reactivity with rabbit IgG.
A series of novel 1,2,3,5-tetrahydroimidazo[1,2-a]thieno[2,3-d]-, -[3,2,-d]-, and -[3,4-d]pyrimidin-2-one derivatives has been prepared and tested for the activity of inhibiting platelet aggregation in rats in vitro and ex vivo. These compounds were synthesized through the following reactions: sodium borohydride reduction of 2,4-dichlorothienopyrimidines, followed by ethoxycarbonylmethylation and successive amination. Most of the compounds were found to be potent inhibitors of blood and platelet aggregation. Structure-activity relationships have indicated the essential contribution of the lactam structure and lipophilic substituents on the thiophene ring to the effective interaction of the compounds with a receptor site on the platelet. Among the compounds studied, 1,2,3,5,6,7,8,9-octahydro-[1]benzothieno[2,3-d]imidazo[1,2-a]pyrimidin-2-one (9m) exhibited the most favorable activity.
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Dental care for the physically and mentally handicapped ought to be a normal part of the responsibilities of the pedodontist. In the case of severe handicap, however, it may be difficult to achieve an acceptable standard of care under general practice conditions. An account is given of the regimen followed in the Tokyo Metropolitan Rehabilitation Institute for the Severely Handicapped where a team approach to dental care has been in existence for the past 10 years. Data are presented which demonstrate the incidence of dental disease in various categories of handicap and examples are given of the improvement in the quality of life of the institutionalized handicapped as a result of regular, high quality dental care.
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In order to analyze the host-parasite interactions in experimental trichomoniasis, the growth of Trichomonas foetus in the peritoneal cavity and changes in the peritoneal exudate cells were followed in mice treated with dextran sulfate 500 (DS 500), a known macrophage-toxic agent. Light microscopic observation showed that DS 500 treatment induced degeneration of peritoneal macrophages within about 48 hr after the treatment and the damaged macrophages did not phagocytize the parasites, whereas peritoneal neutrophils and lymphocytes were not affected by the drug. In the DS 500-treated mice, growth of parasites in the peritoneal cavity was accelerated and a high susceptibility of the mice to T. foetus infection was observed. These results indicate that macrophages play the most important role among the peritoneal exudate cells in resistance to T. foetus infection, especially during the early stage of infection.
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A hemagglutinin was produced by strains of Conidiobolus which also produce beta-N-acetylglucosaminidase. Activity of the hemagglutinin was inhibited by D-glucosamine, N-acetyl-D-glucosamine, D-mannosamine, and beta-N-acetyl-D-glucosaminides but not by D-glucose, D-mannose, and alpha-N-acetyl-D-glucosaminides.
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