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Biomedical subjects

Y Inamoto

Publications and source records attributed to Y Inamoto.

At least 37 records · Page 2Linked to original sources

[Studies on FK482 (Cefdinir). IV. Synthesis and structure-activity relationships of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]- 3-substituted cephalosporin derivatives].

The synthesis of 7 beta-[(Z)-2-(aminothiazol-4-yl)-2-hydroxyiminoacetamido] cephalosporins (Ia-i) modified at the C-3 position of a cephem nucleus and the effect of the C-3 substituents on the antibacterial activity and oral absorbability are discussed. The cephems (Ie, h and i) having a C-3 substituent such as 1-propenyl, ethylthio and vinylthio group as well as FK482 (cefdinir) exhibited excellent antibacterial activities against both gram-positive and gram-negative bacteria. However, those compounds showed poor absorption rate after oral administration in rats. It is concluded that the vinyl moiety at the 3-position is necessary to display fairly oral absorptivity in a series of 7 beta-[(Z)-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]c eph ems.

Animals

[Studies on FK482. II. Synthesis and structure-activity relationships of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-substituted acetamido]-3-vinyl-3-cephem-4-carboxylic acid derivatives].

Various 7 beta-[2-(2-aminothiazol-4-yl)-2-substituted acetamido]-3-vinyl-3-cephem-4-carboxylic acid derivatives (Ia--e, IIa--g) were synthesized in order to find a new orally active cephalosporin improving the antibacterial activity of cefixime (CFIX) against Staphylococcus aureus. These derivatives include three types of alpha-substituted 2-(2-aminothiazol-4-yl)acetyl side chain; i) mono or non substituted acetyl moiety, ii) carboxyalkoxyimino acetyl moiety, iii) phosphonomethoxyimino and hydroxyimino acetyl moiety. Their structure-activity relationships and urinary recoveries in rats were studied. As a result, the compound with a hydroxyimino acetyl side chain (IIg, FK482) showed good oral absorption and excellent antibacterial activity against both gram-positive and gram-negative bacteria and was selected as a candidate for clinical trial.

Animals

[Studies on FK482 (Cefdinir). III. Synthesis and structure-activity relationships of 7 beta-[(Z)-2-aryl-2-hydroxyiminoacetamido]-3-vinyl-3- cephem-4-carboxylic acid derivatives].

The synthesis, antibacterial activity and oral absorption of the 7 beta-[(Z)-2-aryl-2-hydroxyiminoacetamido]-3-vinylcephalosporins (Ia--e) are described. All of these compounds exhibited excellent activity against Staphylococcus aureus. Against Gram-negative bacteria FK482 exhibited more excellent activity than the other compounds (Ia--e). These compounds except Ie showed good oral absorption. The relationship between the oral absorption rates and the lipophilicity of these cephalosporins is discussed.

Animals

Synthesis and structure determination of FR109615, a new antifungal antibiotic.

The structure of FR109615, a new antifungal antibiotic, was determined to be (1R,2S)-2-aminocyclopentane-1-carboxylic acid ((-)-cis-2-ACPC: 8a) by X-ray analysis. (-)-cis-2-ACPC (8a) was also synthesized via optical resolution of 3a and 3b derived from (+/-)-cis-2-ACPC hydrochloride (1). 8a showed potent antifungal activity, while its antipode (+)-cis-2-ACPC (8b) had no activity.

Antifungal Agents

[A case of intermittent ventricular pre-excitation syndrome with a Mahaim fiber].

A 61 year-old woman with intermittent ventricular pre-excitation syndrome using a Mahaim fiber was reported. The electrocardiogram showed QRS-complex with small delta wave (100 msec in QRS width) or without small delta wave (80 msec in QRS width). On electrophysiological study, during sinus rhythm, A-H interval was 100 msec. H-V intervals were 25 msec in QRS-complex with small delta wave and 45 msec in QRS-complex without small delta wave. From these findings, it was considered that the small delta wave was produced by a Mahaim fiber.

Electrocardiography

Multiple myeloma in husband and wife.

A married couple with multiple myeloma (MM) is reported. Although we could not find any definite pathogenetic factors of MM in the spouses examined, the salient features of the 10 couples with MM reviewed, including ours, were summarized to obtain a better understanding of the pathogenesis of MM. The appearance of MM in spouses suggests that environmental factors are involved in the pathogenesis of MM.

Aged

Recurrent chromosome abnormalities in adult T-cell lymphomas of peripheral T-cell origin.

Cytogenetic studies were performed on 11 Japanese patients with adult T-cell lymphoma of peripheral T-cell origin. All patients had a histologic diagnosis of diffuse lymphoma, and were treated with intensive combination chemotherapy; their median survival was 6 months. Lymphomas were categorized on the basis of the classification proposed by the Lymphoma Study Group of Japan: 5 patients had the features of pleomorphic lymphoma; 3, mixed lymphoma; 2, large-cell lymphoma; and 1, medium-sized-cell lymphoma. The modal chromosome number of abnormal cells was near-diploid in 7, and hypotetraploid in 4 including 3 patients with pleomorphic lymphoma. Abnormalities of the clonal chromosomes were observed in all 11 patients. A translocation of the short arm of 19 at band 19p13 was found in 2 patients with pleomorphic lymphoma and in one patient each with mixed lymphoma and medium-sized-cell lymphoma. A translocation of the short arm of 14, with a break at band 14p12, occurred in 4 patients with pleomorphic lymphoma. In one patient each with mixed lymphoma and large-cell lymphoma, an extra chromosome 3 was found. The numerical change was unique because their lymphomas were further categorized as "angioimmunoblastic lymphadenopathy with dysproteinemia" and "large-cell immunoblastic lymphoma", respectively. Our findings suggest that characteristic chromosome abnormalities occur in adult T-cell lymphoma, and dividing cells in the tetraploid range tend to be predominant in pleomorphic lymphoma.

Adult

First report of case of congenital afibrinogenemia with successful delivery.

We report a case in which pregnancy was sustained in a woman with congenital afibrinogenemia with delivery by cesarean section. From this case it appears that a plasma fibrinogen level greater than 60 mg/dl would maintain implantation of the placenta and fetus even in the event of complications occurring during pregnancy.

Adult

Neurological control of fetal heart rate in 20 cases of anencephalic fetuses.

Fetal heart rate (FHR) is influenced by the central nervous system, cardiac automatism, biochemical factors, etc. Changes in FHR were correlated with the anatomic defect in autopsy material from 20 anencephalic infants, and, on this basis, the following hypotheses were formed, subject to later experimental proof. (1) The FHR baseline level is controlled by the medulla oblongata and vagus nerve. (2) The biphasic sleep-awake pattern is controlled by the cerebral cortex. (3) The midbrain is involved in the occurrence of acceleration. (4) A relative high level of short-term variability is shown when small lesions of the lesser central nervous system are present, but we cannot conclude that the cortex is critical for short-term variability. On the other hand, long-term variability seems to be correlated to the presence of the medulla oblongata and midbrain, and might be amplified by the cerebral cortex. (5) U-shaped decelerations are connected with the medulla oblongata, but V-shaped decelerations depend on intracardiac reflexes and myocardial stretch.

Anencephaly

A rare case of Capgras syndrome observed in wake-amine induced psychosis.

An adolescent girl showed the apparent Capgras syndrome in the course of wake-amine induced psychosis. The patient, then 18, committed homicide in close connection with the syndrome and also with the distorted judgment due to personality immaturity. As far as the syndrome was concerned, the extension was so extreme that it involved her neighbors and even her dwelling city. The detailed case history was reported along with a discussion about the psychodynamism.

Adolescent