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Biomedical subjects

H Tagawa

Publications and source records attributed to H Tagawa.

At least 109 records · Page 6Linked to original sources
PubMed1986

Synthesis and biological activity of resolved C-10 diastereomers of 10-methyl- and 10-ethyl-10-deazaminopterin.

Synthesis and evaluation of the antitumor drugs 10-methyl- and 10-ethyl-10-deazaminopterin (15a,b) were previously reported for the diastereomeric mixtures, lacking resolution at the C-10 position. In order to assess biological properties of the individual diastereomers, the C-10 isomers of 4-amino-4-deoxy-10-methyl- and 10-ethyl-10-deazapteroic acids (13a,b) were prepared by total synthesis. Coupling with L-glutamate afforded the appropriate diastereomers of the title compounds. Biochemical, transport, and cell growth inhibitory properties in L1210 cells and folate-dependent bacteria were measured. Differences were generally less than 2-fold between diastereomeric pairs, but a factor of 3 was noted for d,L-15b vs. l,L-15b in inhibition of DHFR from L1210 cells and in cytotoxicity toward L1210 cells. An in vivo comparison of the isomers of 15b with racemic compound against L1210 in mice did not show a significant efficacy difference (ILS) among the compounds. However, d,L-15b showed an acute toxicity about 2.5 times that of l,L-15b.

Aminopterin↗
PubMed1986

Semisynthetic beta-lactam antibiotics. I. Synthesis and antibacterial activity of 7 beta-[2-aryl-2-(aminoacetamido)acetamido]-cephalosporins.

The synthesis and in vitro structure-activity relationships of cephalosporins having dipeptides substituted with various aryl groups as the side chain at the C-7 position have been outlined. Of these compounds, 2-aminothiazol derivatives showed a broad spectrum of enhanced antibacterial activity, and 7 beta-[DL-2-(D-aminopropionamido)-2-(2-aminothiazol-4-yl)acet amido]-3- [(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxyli c acid was the most balanced of these active derivatives with respect to both Gram-positive and Gram-negative strains.

Bacteria↗
PubMed1986

Semisynthetic beta-lactam antibiotics. II. Synthesis and antibacterial activity of 7beta-[2-(acylamino)-2- (2-aminothiazol-4-yl)acetamido]cephalosporins.

Cephalosporin derivatives (I) substituted with a neutral, acidic or basic amino acid group as the terminal group attached to the 2-amino-2-(2-aminothiazol-4-yl)acetamido side chain at the C-7 position were synthesized, and the effect of each group on antibacterial activity was examined. The derivatives bearing an amidino or guanidino group showed broad spectra of antibacterial activity similar to those of cefotaxime, but they were relatively sensitive to beta-lactamases.

Bacteria↗
PubMed1986

Semisynthetic beta-lactam antibiotics. III. Synthesis and antibacterial activity of 7 beta-[2-(2-aminothiazol-4-yl)-2-(substituted carbamoylmethoxyimino)acetamido]cephalosporins.

Syntheses of cephalosporins modified with a 7 beta-[2-(2-aminothiazol-4-yl)-2-(substituted carbamoylmethoxyimino)acetamido] group at the C-7 position and with various hetero aromatics at the C-3 position are described. The effects of substituents on the carbamoyl group in the 7-side chain were investigated in order to improve antibacterial activity. Some of these compounds exhibited high antibacterial activity against Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa, as well as good resistance to beta-lactamase.

Bacteria↗
PubMed1985

Diffuse hepatic calcification as a sequela to shock liver.

A 31-yr-old Japanese woman who was on chronic hemodialysis for 3 yr died of intractable congestive heart failure. Three years before death, the patient was in a state of shock for 48 h due to ventricular tachycardia and gastrointestinal bleeding, which was followed by marked elevation of serum transaminase. Four months later, abdominal plain radiography demonstrated diffuse hepatic calcification. At autopsy, microscopic examination of the liver revealed parenchymal necrosis and tiny calcifications in the central to midzonal area of the lobule. Calcification in the degenerative area of the hepatic lobule occurred subsequent to parenchymal ischemia after overt shock that lasted for 2 days. Although a definitive explanation for the calcification was not obtained, it may be related to the disturbances of intracellular Ca2+ homeostasis as a result of ischemic liver injury or it may be related to an elevated calcium-phosphorus product in the uremic state.

Adult↗
PubMed1985

Aggregation of bovine serum albumin upon cleavage of its disulfide bonds, studied by the time-resolved small-angle X-ray scattering technique with synchrotron radiation.

A rapid mixing system of the stopped-flow type, used with small-angle X-ray scattering equipment using synchrotron radiation, is described. The process of aggregation of bovine serum albumin was traced with a time interval of 50 s, initiated upon cleavage of its disulfide bonds by reduction with dithiothreitol. The results indicate that a 218-fold molar excess of dithiothreitol over the number of moles of disulfide bonds in bovine serum albumin is sufficient to initiate the reaction immediately after mixing, which reaches equilibrium in about 15 min. On the other hand, half this amount is not sufficient to initiate the reaction, so that the reaction is delayed by about 150 s. Such a single-shot time-resolved experiment showed that experiments with a time interval of 100 ms are possible with repeated multi-shot runs.

Animals↗
PubMed1985

Retinal circulatory changes related to retinopathy progression in insulin-dependent diabetes mellitus.

To quantify the vascular deterioration of the diabetic retina, retinal circulatory changes in 45 insulin-dependent diabetic patients, and in 17 normal controls, were measured and divided into four groups according to severity of retinopathy. The noninvasive laser Doppler technique was used to measure the systolic/diastolic variation of red blood cell velocity (V) at sites along temporal retinal arteries. Flow pulsatility [V (systole)/V (diastole)] was 18% lower (P less than 0.00001) in the mild-retinopathy group than in normal controls, but 35% higher (P less than 0.001) in the severe-retinopathy group than in the mild-retinopathy group. Repeated measurements in three eyes during the progression from mild or moderate to severe retinopathy showed progressive increases in both flow pulsatility and mean retinal blood flow. Altered flow pulsatility appears to be a sensitive indicator of vascular alterations during the progression of diabetic retinopathy.

Adult↗
PubMed1984

Rotational acetabular osteotomy for the dysplastic hip.

A circumacetabular osteotomy of the acetabulum was initially done at the University of Tokyo Hospital by one of us (H. T.) in 1968. This procedure, which rotates the acetabulum, was designed to correct a dysplastic acetabulum in adolescents and adults. The surgical exposure combines both an anterior and a posterior approach. Between 1974 and 1982 this operation was performed on 103 patients (120 hips) with acetabular dysplasia, some showing early degenerative arthritis. The forty-five hips (forty-one patients) that form the basis of this report were followed for three years to eight years and ten months (average, four years and six months). Thirty hips showed only acetabular dysplasia, and fifteen were in the early stage of degenerative arthritis. The ages of the patients at the time of operation ranged from eleven to forty-two years, the majority being in the second or third decade of life. All of the forty-five hips had a preoperative center-edge angle of 10 degrees or less, but most of them had a nearly normal value after surgery. In the majority of the hips either limp or pain with exertion, or both, had disappeared, and a satisfactory range of motion had been restored.

Acetabulum↗