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Biomedical subjects

K Sakagami

Publications and source records attributed to K Sakagami.

At least 109 records · Page 6Linked to original sources
PubMed1990

Synthetic cephalosporins. VI. Synthesis and antibacterial activity of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methyl) ethoxyiminoacetamido]- 3-(3-hydroxy-4-pyridon-1-yl)methyl-3-cephem-4-carboxylic acid and related compounds.

Synthesis and antibacterial activity of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methyl)ethoxyimin oacetamido]- 3-(3-hydroxy-4-pyridon-1-yl)-3-cephem-4-carboxylic acid (12) and its related compounds are described. Compound 12 exhibited excellent antibacterial activity against gram-negative bacteria, and its anti-pseudomonal activity was ten to fifteen times greater than that of ceftazidime.

Cephalosporins↗
PubMed1990

Synthetic cephalosporins. VII. Synthesis and antibacterial activity of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(3-(3-hydroxy-4-pyridon-1-yl)-3- carboxypropoxyimino)acetamido]-3-(1,2,3-thiadiazol-5-yl)-thiomethyl-3- cephem-4-carboxylic acid and its related compounds.

Synthesis and antibacterial activity of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(3-(3-hydroxy-4-pyridon-1-y l)-3- carboxypropoxyimino)acetamido]-3-(1,2,3-thiadiazol-5-yl)thio methyl-3-cephem-4-carboxylic acid (12a) and its related compounds are described. Compound 12a exhibited excellent antibacterial activity against gram-negative bacteria, including Pseudomonas aeruginosa.

Bacteria↗
PubMed1990

A new antipseudomonal cephalosporin CP6162 and its congeners.

The synthesis and biological activity of a series of 3-[2-(5-hydroxy-4-pyridon-2-yl)ethenyl]cephalosporin derivatives are described. They showed very potent activity against Gram-negative bacteria, especially Pseudomonas aeruginosa. (6R, 7R)-7-[(Z)-2-(2-Aminothiazol-4-yl)-2 -(1-carboxy-1-methyl)-ethoxyiminoacetamido]-3-[(Z)-2-(1,5-dihydrox y-4- pyridon-2-yl)ethenyl]ceph-3-em-4-carboxylic acid, CP6162 (8e), was selected for further evaluation as antipseudomonal chemotherapeutic agent.

Animals↗
PubMed1989

The effect of anti-interleukin 2 monoclonal antibody treatment on the survival of rat cardiac allograft.

The effect of anti-interleukin 2 monoclonal antibody (anti-IL2 MoAb) and the accumulation of intravenously administered 125I-labeled anti-IL2 MoAb were examined in heterotopic rat cardiac allografts. Mouse anti-human recombinant IL2 MoAb was obtained by the hybridoma technique. The anti-IL2 MoAb, termed 8H-10, was an IgG2a which inhibited IL2-driven [3H]TdR incorporation in cytolytic T lymphocyte line cells at a dilution of 2(6). 8H-10 was injected iv at a dose of 200 micrograms/day for 8 consecutive days, beginning on the day of transplantation. Hearts from F344 rats (RT11v1) were transplanted into ACI recipient rats (RT1av1). The mean survival time was 7.6 +/- 0.8 days in untreated controls, 9.0 +/- 1.2 days in additional controls treated with mouse anti-sheep red blood cell monoclonal antibody, and 25.3 +/- 18.4 days in the anti-IL2 MoAb (8H-10)-treated group (P less than 0.05). Furthermore, the accumulation of intravenously administered 125I-labeled anti-IL2 MoAb (8H-10) was specifically seen in the grafted heart. In conclusion, these results suggest that IL2 may play an important role in allograft rejection and that anti-IL2 MoAb may serve as a useful immunosuppressive agent in clinical transplantation.

Animals↗
PubMed1989

Induction of antiidiotypic antibodies by donor-specific blood transfusions. Establishment of a human-mouse hybridoma secreting the MLR-inhibiting factor.

We describe a patient transfused with 200 ml of donor fresh whole blood three times at 2-week intervals. Three weeks after the last transfusion, transplantation and splenectomy were done at the same time. Splenic cells from this DST pretreated patient were fused with murine myeloma cells (X63-Ag8, 653). With DST pretreatment, various clones were developed in vivo, and finally 69 human immunoglobulin-secreting clones were obtained. Modulation of the alloantigen-specific MLR by supernatants from 69 clones showed various degrees of suppression or augmentation. The hybridoma clone 7 and clone 2, which had been secreting IgG antibody for more than 6 months, showed some degree of suppression in the alloantigen-specific MLR (mean suppression = 63%, 46% respectively). According to the result of MLR, clone 7 antibody was directed against recipient lymphocytes and clone 2 antibody was against donor lymphocytes. Immunoprecipitation was carried out by clone 7-IgG and clone 2-IgG. Clone 7-IgG specifically precipitated 1 molecule from the recipient lymphocyte with a molecular weight of 120 KD, similar to the molecular weight range reported for T cell receptors. Clone 2-IgG precipitated a 20 KD molecule from the donor lymphocyte. The data suggest that DST induces antibodies directed against the blood donor alloantigen-specific receptors on the recipient's T lymphocytes--and, at the same time, induces antibodies against donor lymphocyte antigens. These antibodies may be essential to prolongation of kidney allograft survival following DST.

Blood Transfusion↗
PubMed1989

[Synthetic cephalosporins. V. Synthesis and antibacterial activity of 3-alkylthio-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)acetamido]cephalosporins and related compounds].

3-Alkylthio-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)acetamido]cephalosporins (6 and 7) and the 3-methoxy analogues (10) were prepared by coupling diphenylmethyl 7-amino-3-alkylthio-3-cephem-4-carboxylate (1 and 2) or diphenylmethyl 7-amino-3-methoxy-3-cephem-4-carboxylate with (Z)-2-(2-tritylaminothiazol-4-yl)-2-(O-substituted oxyimino)acetic acid (4), followed by deprotection and subjected to examination of antibacterial activities. The pivaloyloxymethyl esters (8 and 9) of the compounds (6 and 7) were also prepared and oral activities of these esters were compared with those of the parent compounds (6 and 7). The cephalosporins (6a-j and 7a-c) had potent and wide antibacterial spectra against Gram positive and Gram negative bacteria which were comparable to those of cefixime or cefteram. Among them, the cephalosporins (6f and 7c) and the pivaloyloxymethyl esters (8b and 9b) had good in vivo efficacy in mice against infections of Escherichia coli No. 29 and especially 8b showed high urinary recovery in mice.

Animals↗
PubMed1989

[Synthetic cephalosporins. IV. Synthesis and antibacterial activity of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)acetamido]-3-(1,2,3-triazol-1-yl)methyl-3-cephem-4-carboxylic acid and related compounds].

Synthesis and oral activity of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)-acetamido]-3-(1,2,3-triazol-1-yl)methyl-3-cephem-4 -carboxylic acid and its related compounds were described. 3-(1,2,3-Triazol-1-yl)methylcephalosporins have been prepared by the direct cycloaddition of acetylene to 3-azidomethylcephalosporins, which were obtained by nucleophilic substitution of 3-chloromethylcephalosporins with sodium azide in N,N-dimethylformamide. The cephalosporins (8a--c) had potent and wide antibacterial spectra against gram positive and gram negative bacteria which were comparable to those of cefixime or cefteram. Urinary recovery of 9a and 9b, pivaloyloxymethyl esters of 8a and 8b, were 9.2% and 3.5%, respectively, through oral administration in mice, exhibiting lower rate than that of cefteram pivoxyl (28%).

Animals↗
PubMed1989

[Synthetic cephalosporins. III. Synthesis and antibacterial activity of 7-[2-(2-Aminothiazol-4-yl)-3-carboxy-2-propenoamido]cep hal osporins and related compounds].

Synthesis and antibacterial activity of 7-[2-(2-aminothiazol-4-yl)-3-carboxy-2-propenoamido]cepha los porins and their derivatives are described. These compounds are of interest as carbon analogues of oximecephalosporins, 7-[2-(2-aminothiazol-4-yl)-2(Z)-oxyiminoacetamido]cephalo spo rins having remarkable antibacterial activity. The synthesized 7-[2-(2-aminothiazol-4-yl)-3(Z)-carboxy-2-propenoamido]-c eph alosporins (14, 19) show improved activity especially against the beta-lactamase-producing strains. A 7-[2-(2-aminothiazol-4-yl) maleimido]cephalosporin (15) has been also prepared by cyclization of 7-[3-(2-aminothiazol-4-yl)-2-ethoxycarbonyl-2(Z)-propenoamido++ +]cephalosporin.

Bacteria↗
PubMed1989

Effect of serum fractions obtained from cancer patients by double filtration plasmapheresis combined with natural tumor necrosis factors and cyclophosphamide on murine pulmonary metastases.

We investigated the effects of fractionated sera obtained from cancer patients by double filtration plasmapheresis (DFPP) plus antitumor agents on murine pulmonary metastasis. Fractions of the sera, in combination with natural human tumor necrosis factors (nTNF) and cyclophosphamide (Cy), were systemically administered to Lewis lung carcinoma-bearing mice. When the second filtrate (a plasma fraction containing substances composed of smaller molecular weight compounds) combined with low-dose nTNF (1,000 U/kg) and Cy (250 micrograms/kg) was administered to the mice, the degree of metastasis was significantly suppressed compared with the control group (p less than 0.01). In contrast, the discarded fluid (a plasma fraction containing larger molecular weight compounds) combined with the same doses of nTNF and Cy caused little inhibition of metastasis. Also, the discarded fluid significantly suppressed natural killer activity compared with normal sera (p less than 0.01). The results suggested that DFPP combined with nTNF and Cy is an efficient procedure to remove immunosuppressive factors from the sera of cancer-bearing hosts, to enhance the host antitumor immunity, and to suppress tumor proliferation.

Animals↗