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T Nishimura

Publications and source records attributed to T Nishimura.

At least 55 records · Page 3Linked to original sources
PubMed1992

Studies on condensed-heterocyclic azolium cephalosporins. III. Synthesis and antibacterial activity of 7 beta-[2-(2-amino-5-substituted-thiazol-4-yl)-2 (Z)-alkoxyiminoacetamido]-3-(condensed-heterocyclic azolium)methyl-3-cephem-4- carboxylates.

As a part of our research on the synthesis of cephalosporins bearing condensed-heterocyclic azolium groups at the 3 position in the cephalosporin nucleus, we describe herein the synthesis of 7 beta-[2-(2-amino-5-halogeno-, methylthio-, methylsulfinyl-, methylsulfonyl- and sulfothiazol-4-yl)-2(Z)-alkoxyiminoacetamido] cephalosporins and their antibacterial activity. Among the compounds prepared, 7 beta-[2-(2-amino-5-chlorothiazol-4-yl)-2(Z)- methoxyiminoacetamido]-3-(imidazo[1,5-a]-pyridinium-1-yl)methyl-3-cephem -4-carboxylate (14) showed good antibacterial activity against both Staphylococcus aureus including methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa, whereas the antibacterial activity against other Gram-negative bacteria was a slightly lower than that of 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoxyiminoacetamido]-3-(im ida zo [1,2-a]pyridinium (I-1) and imidazo[1,5-a]pyridinium (I-4)-1-yl)methyl-3-cephem-4-carboxylates.

Anti-Bacterial Agents↗
PubMed1992

Studies on condensed-heterocyclic azolium cephalosporins. IV. Synthesis and antibacterial activity of 7 beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2(Z)- alkoxyiminoacetamido]-3-(condensed-heterocyclic azolium)methyl cephalosporins including SCE-2787.

The synthesis and in vitro antibacterial activity of 7 beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2(Z)-alkoxyiminoacetami do] cephalosporins bearing various condensed-heterocyclic azolium groups at the 3 position in the cephalosporin nucleus are described. The thiadiazolyl cephalosporins showed good antibacterial activity against both Gram-positive and Gram-negative bacteria and the MICs of the thiadiazolyl cephalosporins against Pseudomonas aeruginosa was more potent than that of the corresponding 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-alkoxyiminoacetamido]-3- (condensed-heterocyclic azolium)methyl cephalosporins. Also, the thiadiazolyl cephalosporins bearing (imidazo[1,2-b]-pyridazinium-1-yl)methyl groups at the 3 position showed antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). Among the cephalosporins tested, 7 beta-[2-(5- amino-1,2,4-thiadiazol-3-yl)-2(Z)-methoxyiminoacetamido]-3-(imidaz o[1,2- b]pyridazinium-1-yl)methyl-3- cephem-4-carboxylate (4, SCE-2787) which exhibited the most potent antibacterial activity and the broadest antibacterial spectrum was selected as a parenteral cephalosporin candidate for further biological evaluation.

Cephalosporins↗
PubMed1992

Studies on condensed-heterocyclic azolium cephalosporins. V. Synthesis and antibacterial activity of 3-(condensed-triazolo-pyridinium, -pyrimidinium, and -pyridazinium)-methyl cephalosporins.

As a part of our studies on cephalosporins bearing condensed-heterocyclic azolium methyl groups at the 3 position in the cephalosporin nucleus, we describe here the synthesis and antibacterial activity of 7 beta-[2-(2-aminothiazol-4-yl)2(Z)-methoxyiminoacetamido] cephalosporins (1-16, 7 beta-[2-(2-amino-5-chlorothiazol-4-yl)-2(Z)- methoxyiminoacetamido] cephalosporins (17,18) and 7 beta-[2-(5-amino- 1,2,4-thiadiazol-3-yl)-2(Z)-methoxyiminoacetamido) cephalosporins (19-23) containing a variety of condensed-heterocyclic triazolium methyl groups at the 3 position in the cephalosporin nucleus. These cephalosporins exhibited potent antibacterial activity, and it appears that condensed-heterocyclic triazolium as well as condensed-heterocyclic imidazolium rings are effective moieties for improving antibacterial activity and the spectrum of activity. Among the cephalosporins tested, 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoxyiminoacetamido]-3-(5- methyl[1,2,3]triazolo-[1,5-alpha]pyridinium-1-yl)methyl-3-cephem-4- carboxylate (9) and 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoxyiminoacetamido]-3-(6- methoxy[1,2,4]triazolo[1,5-alpha]pyridinium-1-yl)methyl-3-cephem-4- carboxylate (11) showed good antibacterial activity.

Cephalosporins↗
PubMed1992

[Laser photocoagulation of experimentally produced choroidal neovascularization. 2. Comparison of effects by dye and argon blue-green lasers].

Choroidal neovascularization was produced in 18 eyes of 12 rhesus monkeys by application of intense krypton laser photocoagulation. Eight weeks or later, a total of 34 choroidal neovascularizations were treated either by dye laser at wavelengths of 577 or 630 nm or by argon blue-green laser. The treated lesions were evaluated clinically and histopathologically from 24 hours to 3 months after treatment. All the treated lesions were apparently healed by each of the 3 laser modalities. Histopathologically, all the treated choroidal neovascularizations were occluded 24 hours after treatment. At 2 weeks to 3 months after treatment, newly-formed choroidal vessels were present in 3 of 9 lesions (33%) after 577 nm dye laser treatment, in 8 of 9 lesions (89%) after 630 nm dye laser treatment, and in 5 of 8 lesions (62%) after argon blue-green laser. These results seemed to show the clinical superiority of 577 nm dye laser in treating choroidal neovascularization.

Animals↗
PubMed1992

Intraarterial lymphocyte-injection therapy for lymphedema of the leg: an examination using indium-111 oxine labeled autologous lymphocytes.

A 58-year-old female patient with lymphedema of the left leg was treated by repeated intraarterial lymphocyte-injection therapy. To elucidate whether the injected lymphocytes act at the affected site of the leg, we examined the distribution of the In-111 oxine labeled lymphocytes injected into the proximal artery to the affected leg in comparison with the distribution in the other, healthy, leg. The radioactivity of the affected leg was almost two times higher than that of the healthy leg during the first 30 min after injection, and it remained higher even after 24 hours. The circumference of the affected leg of the patient decreased steadily during her hospital stay. These results, together with the clinical findings, suggest that some of the intraarterially-injected lymphocytes remained in the affected leg at least 24 hours and might play some role in reducing the volume of lymphedematous fluid.

Blood Component Transfusion↗
PubMed1992

[A case of hepatoma patient who showed an abnormally high level of serum IRI with the beads method].

A fifty four years old hepatoma patient admitted to the hospital for a surgical operation. Preoperative laboratory examination demonstrated that his serum IRI level was very high (423 microU/ml) when measured with a beads method, however RIA or a microplate method demonstrated normal values. We studied the mechanism of the discrepancy of IRI values. 1) Both the beads and microplate methods demonstrated the same IRI values when the patient's serum insulin was roughly purified with Sep-Pak. The beads method showed high IRI values in serum which passed through Sep-Pak, therefore contained no insulin. 2) The similar results were observed when the patient's serum fractionated by a gel-chromatography (Biogel P-30). The beads method demonstrated high IRI values in both insulin fractions and the fractions containing serum proteins bigger than 40,000 molecular weight. The microplate method demonstrated only one large peak of insulin. 3) When non-specific IgG of guinea pig was used as a fixed antibody instead of human insulin antibody of guinea pig that was used in the beads method, the patient's serum showed the similar values as that obtained with the beads method. We thereby concluded that the abnormal level of IRI by the beads method was derived from the unknown substance reacting with IgG of guinea pig in the patient's serum. After the surgical resection of hepatoma, the levels of IRI measured by the beads method decreased significantly, suggesting that the substance is related to hepatoma cells.

Animals↗
PubMed1992

[Pulmonary uptake of thallium-201 in patients with congenital heart disease: comparison between total anomalous pulmonary venous connection and tetralogy of Fallot].

To evaluate the pulmonary extravascular space in patients with congenital heart disease, lung uptake of thallium-201 (T1-201) was quantitatively studied. A total of 50 T1-201 imagings were performed in 33 patients with total anomalous pulmonary venous connection (TAPVC); 4 preoperatively, 22 postoperatively in the early stage (within 6 months), and 24 in the late stage (7 months or later). The images consisted of 17 supracardiac TAPVC (type-I), 13 paracardiac (type-II) and 3 infracardiac (type-III). In patients with tetralogy of Fallot (T/F), T1-201 imaging was performed 15 times preoperatively, 12 in the early stage and 15 in the late stage, postoperatively. Furthermore, 29 patients with ventricular septal defect (VSD) or patent ductus arteriosus (PDA) were also studied preoperatively, and 21 in the late postoperative stage. Twenty-five patients with arrhythmias or a history of Kawasaki disease without perfusion defects were studied on T1-201 myocardial imaging. Lung uptake of T1-201 was analyzed with a computer using the anterior image of the chest, and the average count ratio of the right lung (P) to the left ventricular wall (LV) was calculated. P/LV values were compared between the patients before and after surgery, and differences in anatomical types in TAPVC were also evaluated. In TAPVC, P/LV values decreased gradually in the postoperative state, but were significantly higher than those of controls even in the late stage. In the late postoperative stage, type-I TAPVC had significantly higher P/LV values than those of type-II.(ABSTRACT TRUNCATED AT 250 WORDS)

Heart Defects, Congenital↗
PubMed1992

[Laser photocoagulation for experimental choroidal neovascularization. 1. Mild dye laser photocoagulation].

The author treated experimentally produced choroidal neovascularization (ChNV) with mild dye laser photocoagulation (PHC). We treated these ChNVs with 590 nm wavelength, 200 microns spot size, 0.2 second duration and 50 mW of power. Eleven eyes of nine rhesus monkeys were used. Then these ChNVs were examined clinically and histopathologically at 24 hours, 2 weeks and a month after therapeutic PHC. Small ChNVs, less than 1/3 disc diameter healed successfully and histopathologically most of them were coagulated and disappeared. A few poorly developed ChNVs remained, but were well enveloped by the proliferating retinal pigment epithelial (RPE) cells. On the other hand, ChNVs of more than 1/3 disc diameter did not respond to weak PHC, grew actively over a month, and were not completely surrounded by proliferating RPE cells. These results suggest that by mild PHC, small ChNVs may be treatable, however, in large ChNVs, mild PHC may rather accelerate their activity.

Animals↗
PubMed1992

[Dipyridamole-thallium myocardial imaging in patients unable to exercise adequately: comparison with arm and bicycle ergometer].

We assessed the usefulness of dipyridamole-thallium myocardial imaging in patients unable to exercise adequately, compared with arm-ergometer and standard (bicycle) ergometer. Fifty-six patients with arteriosclerosis obliterans, aortic aneurysm, aortic dissection and so on, who were revealed normal imaging, were studied. Only one of 13 cases with arm-ergometer and two of 14 with bicycle ergometer reached target heart rate. Lung thallium uptake in the cases with arm-ergometer (37 +/- 9%) is higher than that with dipyridamole (29 +/- 5%). This elevation may be confused with pectoralis muscle uptake. Washout rate is 45 +/- 9% with dipyridamole and 46 +/- 12% with bicycle ergometer, respectively, though there was no significant differences. Myocardial/background counts ratio with dipyridamole (4.6 +/- 0.8%) is significantly higher than that with arm and bicycle ergometer (arm-ergometer; 3.5 +/- 0.7, bicycle ergometer; 4.2 +/- 0.9). Then, myocardial image with dipyridamole have superior quality. We concluded that dipyridamole-thallium myocardial imaging is very useful in the patients who have suboptimal exercise efforts.

Aged↗
PubMed1992

[Influence of hypertensive left ventricular hypertrophy on detection of ischemic area with exercise thallium-201 myocardial scintigraphy].

Sixty-four patients with single left anterior descending artery disease having effort angina (group A: 40 patients without hypertension, group B: 10 patients with hypertrophic hypertension, group C: 14 patients with non-hypertrophic hypertension) were assessed the influence of hypertensive left ventricular (LV) hypertrophy on detection of ischemic area. The criterion of hypertrophy by two-dimensional echocardiography was > 12 mm in the wall thickness of interventricular septal or posterior wall. Population in Group B might show low detectability in ischemic area by 201Tl myocardial scintigraphy (positive thallium rate 60%, defect score 2.7 +/- 3.6), and high lung thallium uptake and high frequence of ECG positive among three groups. In semiquantitative analysis, the washout rate of the posterolateral wall and %RD (delayed %uptake-initial %uptake) of the septal wall in patients with Group B were lowest among three groups. However, the washout rate in the septal wall against the posterior wall, and the initial %uptake and the delayed %uptake of the septal wall were not significantly different among three groups. We could conclude that the decreased washout rate in nonischemic area with hypertensive LV hypertrophy might make the ischemic area masked.

Aged↗
PubMed1992

[Metabolite of 15-p-iodophenyl-3(R,S)-pentadecanoic acid (123I) in blood and urine].

We analyzed metabolites of 123I-BMIPP in blood and urine using rats, rabbits and human, while human samples were obtained from normal volunteers of Phase I clinical study. We estimated metabolic pathway of 123I-BMIPP as a myocardial metabolic imaging agent. Radioactivity accumulated in heart after administration gradually decreased and was mainly excreted to bladder via kidneys. The main radioactive component in blood was 123I-PIPA for any species and the urinary components were metabolic conjugates of 123I-PIPA. As results of these studies, we considered that 123I-BMIPP was metabolized to 123I-PIPA by alpha-oxidation process for the first step, follow by beta-oxidation process, then 123I-PIPA was released to blood from tissues. Moreover, 123I-PIPA in blood was conjugated with other compounds and excreted to the bladder.

Animals↗
PubMed1992

[Laboratory and clinical studies of cefprozil in pediatric field].

Laboratory and clinical studies were done on cefprozil (CFPZ, BMY-28100). The results are summarized as follows. CFPZ was administered through the oral route to 2 children at a single dose of 7.5 mg/kg. After administration, peak serum levels of CFPZ obtained in the 2 cases were 6.71 micrograms/ml at 1 hour and 6.45 micrograms/ml at 2 hours, respectively and half-lives were 1.28 hours and 0.92 hour, respectively. The urinary excretion rates of CFPZ were 58.9% and 59.4%, respectively. Treatment with CFPZ was made in 37 cases of pediatric bacterial infections: 1 case of pharyngitis, 16 cases of tonsillitis, 16 cases of scarlet fever, 3 cases of impetigo, 1 case of UTI. Results obtained were excellent in 24 cases, good in 13 cases. No significant side effects due to the drug were observed, except 1 case of loose stool, 3 cases of eosinophilia, and 1 case each of elevated GOT and GPT.

Bacteria↗
PubMed1992

[Clinical studies on panipenem/betamipron in pediatric field].

We have carried out clinical studies on panipenem/betamipron (PAPM/BP, CS-976). The results are summarized as follows. Treatment with PAPM/BP was made in 21 cases of pediatric bacterial infections including 2 cases of tonsillitis, 15 cases of pneumonia and 1 case each of bronchitis, scarlet fever, urinary tract infection and otitis media. Results obtained were excellent in 15 cases, good in 6 cases. No significant side effects due to the drug were observed in any cases.

Age Factors↗
PubMed1992

[Clinical studies of meropenem in pediatric field].

We have carried out clinical studies on meropenem (MEPM, SM-7338), the results are summarized as follows. Treatment with MEPM was made in 13 cases of pediatric bacterial infections including 9 cases of pneumonia and 2 cases of colitis and 1 case each of purulent tonsillitis, and pharyngitis. Results obtained were excellent in 10 cases, good in 3 cases. No significant side effects due to the drug were observed in any cases, except in 1 case each of eosinophilia, elevated gamma-GTP, elevated total bilirubin and elevated GPT.

Adolescent↗
PubMed1992

[Clinical studies on Kock continent urinary reservoir and Indiana continent urinary reservoir].

Recently, the continent urinary reservoir which provides the patient with a better quality of life has become popular. Many types of reservoirs have been reported, but the optimal procedure remains to be established. From July 1987 through November 1988, we performed Kock pouch construction on 11 patients (ages 39 to 76 years). Between July 1989 and March 1991, 9 patients (ages 44 to 66 years) underwent Indiana pouch operation. The first 4 patients underwent ileal patch type, and the subsequent 5 underwent Heineke-Mikulicz type procedure. A one-stage radical cystectomy and continent urinary reservoir construction was performed on 19 patients, and bilateral cutaneous ureterostomy was converted to Kock pouch in one patient. There were no perioperative deaths, but reoperation was required for urinary leakage from the reservoir on one patient in each group. As the late complications in the Kock pouch group, one patient required revisional operation of the continent valve mechanism, 2 patients experienced intermittent prolapse of the nipple valve of the efferent limb, and 2 had malfunction of the afferent nipple valve. In the Indiana pouch group unilateral hydronephrosis was noticed in one patient, and 4 had mild difficulty of catheterization. Although 3 patients in both groups had mild urinary leakage, all patients had good quality of life with capacity of reservoir over 500 ml and with good renal function. We changed the type of operative procedure from Kock pouch to Indiana pouch because of the high complication ratio in the former.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1992

[Diagnostic accuracy of coronary artery lesion by 99mTc-MIBI exercise myocardial scintigraphy--containing the utility of simultaneous assessment of left ventricular function].

To determine whether technetium-99m hexakis-2-methoxy isobutyl isonitrile (99mTc-MIBI) myocardial scintigraphy is a superior method in the detection of coronary artery disease, exercise and rest 99mTc-MIBI planar and SPECT scintigraphy were performed on 27 patients with coronary artery disease. When 99mTc-MIBI (555 MBq (15 mCi)) was injected, first-pass radionuclide angiography (FPRNA) was simultaneously performed by a new mobile multicrystal gamma camera (SIM-400), and LV function (LVEF) was evaluated quantitatively. Visual semiquantitative detection of coronary lesions using 99mTc-MIBI images showed superior accuracy to that obtained using 201TlCl images. 99mTc-MIBI SPECT images were particularly useful in diagnosing LCX and RCA lesions. Moreover, the simultaneous assessment of perfusion and left ventricular function by 99mTc-MIBI FPRNA proved to be useful in the diagnosis of multi-vessel disease. In summary, 99mTc-MIBI SPECT scintigraphy with simultaneous assessment of left ventricular function showed better diagnostic accuracy than 201TlCl myocardial scintigraphy.

Aged↗