著者

MASAO MIYAUCHI OSAMU KANNO ISAO KAWAMOTO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.50, no.9, pp.794-796, 1997-09-25 (Released:2006-11-25)

参考文献数

19

被引用文献数

7 8

著者

MASAO MIYAUCHI ROKURO ENDO MASAFUMI HISAOKA HIROSHI YASUDA ISAO KAWAMOTO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.50, no.5, pp.429-439, 1997-05-25 (Released:2006-11-25)

参考文献数

23

被引用文献数

16 25

---

We have studied an ester prodrug of a carbapenem to develop a potent orally active β-lactam antibiotic. A variety of 1β-methylcarbapenem derivatives have been synthesized. We have found that some derivatives having an amide group in the C-2 side chain show potent and well balanced antibacterial activities as well as high stability against dehydropeptidase-I. Oral absorption of derivatives has been optimized by modifying the C-3 ester promoiety. Pivaloyloxymethyl (1R, 5S, 6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(R)-5-oxopyrrolidin-3-ylthio]-1-carbapen-2-em-3-carboxylate, CS-834, has been selected as the most promising compound for further evaluation.

著者

IWAO YAMAZAKI YOSHIHIRO SHIRAKAWA TAKESHI FUGONO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.34, no.11, pp.1476-1485, 1981 (Released:2006-04-12)

参考文献数

18

被引用文献数

2 3

---

The renal excretory mechanism of cefmenoxime in rabbits was compared with that of 6 other cephalosporins (cefotaxime, deacetylcefotaxime, cefotiam, cefazolin, cephaloridine, and cefsulodin). The clearance ratios (Cf-Drug/CInulin=CRf) of cefmenoxime (337) and cefazolin (73) were considerably higher than those of the 5 other cephalosporins (0.9-20). When p-aminohippurate (PAH) was administered concurrently with each of the cephalosporins, the CRf values of the cephalosporins except for cefsulodin were significantly decreased. These findings indicate that cefmenoxime and the 5 other cephalosporins except cefsulodin are actively incorporated in the proximal tubular cells and secreted into the tubular lumen. In the case of cefotiam and cefsulodin, glomerular filtration tended to exceed urinary excretion with the highest dose of PAH (40 mg/kg/minute), suggesting the possibility of tubular reabsorption of these drugs. On the other hand, glomerular filtration of cefmenoxime and the 4 other cephalosporins did not exceed urinary excretion. The drug concentration ratio of the cortex to medulla indicated that the tubular cell level of cefmenoxime was lower than, higher than, and similar to those of cephaloridine, cefotaxime, and the remaining cephalosporins, respectively. These results demonstrate that the renal excretory mechanism of cefmenoxime is similar to that of cefazolin but not to that of the remaining cephalosporins.

著者

KOZO ODA TAKAHIDE NISHI

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.50, no.5, pp.446-448, 1997-05-25 (Released:2006-11-25)

参考文献数

10

被引用文献数

2 2

著者

TREW SALLY J. WRIGLEY STEPHEN K. PAIRET LYDIE SOHAL JESS SHANU-WILSON PATRICK HAYES MARTIN A. MARTIN STEVEN M. MANOHAR RAVI N. CHICARELLI-ROBINSON M. INÊS KAU DAVID A. BYRNE COLIN V WELLINGTON ELIZABETH M. H. MOLONEY JANET M. HOWARD JUDITH HUPE DONALD OLSON ERIC R.

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.53, no.1, pp.1-11, 2000

被引用文献数

33

---

A series of halogenated pyrrolo [2, 1-b] [1, 3] benzoxazines (<b>1</b>-<b>9</b>) was isolated from fermentations of an actinomycete strain X10/78/978 (NCIMB40808), identified as <i>Streptomyces rimosus</i>, during a microbial extract screening programme to identify inhibitors of bacterial histidine kinase. The structures of these compounds were elucidated by spectroscopic methods including the HMQC, HMBC and INADEQUATE NMR experiments. The structure of <b>1</b> was confirmed by X-ray crystallographic studies. Compounds <b>5</b> and <b>6</b> were produced in fermentations in the presence of NaBr and Nal respectively. The most abundant member of the series, streptopyrrole, <b>1</b>, inhibited the nitrogen regulator II (NRII) histidine kinase from <i>Escherichia coli</i> with an IC₅₀ of 20μM and exhibited antimicrobial activity against a range of bacteria and fungi.

著者

HAMAO UMEZAWA MASAYA IMOTO TSUTOMU SAWA KUNIO ISSHIKI NAOKO MATSUDA TAKESHI UCHIDA HIRONOBU IINUMA MASA HAMADA TOMIO TAKEUCHI

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.39, no.1, pp.170-173, 1986 (Released:2006-04-19)

参考文献数

15

被引用文献数

123 159

著者

TAKASHI IWASA TOYOKAZU KISHI KAZUHO MATSUURA OSAMU WAKAE

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.30, no.1, pp.1-10, 1977 (Released:2006-04-12)

参考文献数

18

被引用文献数

23 50

---

A taxonomic study of Streptomyces strain T-36496, which produces an antibiotic effective against rice blast, revealed that it represented a new taxon and it was named Streptomyces novoguineensis sp. nov. The antibiotic, which was named amipurimycin, showed antifungal activity in vitro and considerable curative effect on leaf blast both in green house and field tests at concentrations ranging from 10 to 20 ppm. It was also effective against neck and panicle blast at the same concentration range.

著者

SETSUO HARADA TOYOKAZU KISHI

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.30, no.1, pp.11-16, 1977 (Released:2006-04-12)

参考文献数

11

被引用文献数

25 43

---

A new antibiotic amipurimycin, active against Pyricularia oryzae in vitro and in vivo, was isolated from the culture filtrate of Streptomyces novoguineensis nov. sp. The antibiotic was purified by a combination of ion-exchange and adsorption chromatography based on its amphoteric water-soluble characteristics. Its molecular formula was estimated to be C20H27-31N7O8.H2O. Characteristic maxima in the UV spectrum and signals in the PMR and CMR spectra were similar to those of 2-aminopurine 9-(β-D)-riboside. These findings indicated that amipurimycin is a new nucleoside antibiotic and the first example of a natural product containing 2-amino-purine.

著者

CHIEKO KUNUGITA FUSAHIRO HIGASHITANI AKIO HYODO NORIO UNEMI MATSUHISA INOUE

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.48, no.12, pp.1453-1459, 1995-12-25 (Released:2006-04-19)

参考文献数

27

被引用文献数

2 5

---

A new extended spectrum β-lactamase was detected in Serratia marcescens 42039 that was isolated from urine of patients with complicated urinary tract infection in Japan. This strain produced three different β-lactamase types (TEM-1, a cephalosporinase, and a new β-lactamase: CKH-1). The TEM-1 and CKH-1 encoding genes were conjugated from S. marcescens 42039 to Escherichia coli K-12 at frequencies of 10-5 to 10-6. The MICs of β-lactams against the transconjugant were: ampicillin >1600, piperacillin 800, cephalothin 1600, ceftazidime 6.25, cefotaxime 100, and ceftriaxone 200μg/ml. The CKH-1 enzyme was purified to more than 90% by ion-exchange chromatography. The molecular weight of purified CKH-1 was 30 K dalton and the isoelectric point was 8, 2, Relative Vmax/Km values (cephaloridme=100) of penicillin G, cephalothin, and oxyiminocephalosporins such as cefuroxime, ceftriaxone, and cefotaxime, were 256, 226, 116, 87, and 49, respectively. The I50 values of tazobactam, BRL-42715, and clavulanic acid against CKH-1 enzyme were 0.0011, 0.0002, and 0.097μM, respectively. The enzymatic activity of CKH-1 was not inhibited by EDTA and anti-TEM-1 serum. These findings indicate that CKH-1 is a member of the groups of class A β-lactamases. This is the first report of a plasmid-mediated oxyiminocephalosporin hydrolyzing broad-spectrum β-lactamase from clinical isolates of S. marcescens.

著者

EDUARDO L. SETTI NARENDER A. V. REDDY OLUDOTUN A. PHILLIPS DAVID P. CZAJKOWSKI KEVIN ATCHISON HARNINDER ATWAL RONALD G. MICETICH SAMARENDRA N. MAITI CHIEKO KUNUGITA AKIO HYODO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.49, no.9, pp.944-946, 1996-09-25 (Released:2006-11-21)

参考文献数

6

被引用文献数

4 5

著者

EDUARDO L. SETTI CHARLES FIAKPUI OLUDOTUN A. PHILLIPS DAVID P. CZAJKOWSKI KEVIN ATCHISON RONALD G. MICETICH SAMARENDRA N. MAITI CHIEKO KUNUGITA AKIO HYODO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.48, no.11, pp.1320-1329, 1995-11-25 (Released:2006-04-19)

参考文献数

19

被引用文献数

3 6

---

A series of 2β-[(4-substituted)-l, 2, 3-triazol-l-yl]methyl penicillanic acid sulfones was synthesized as β-lactamase inhibitors. Many of these compounds showed good in vitro inhibitory activity against penicillinase, cefotaximase and plasmid-mediated class III TEM enzymes, but exhibited weaker cephalosporinase inhibition. One member in this series-2β-[(4-pyridiniummethyl)-l, 2, 3-triazol-lyl]methyl-6, 6-dihydropenicillanate 1, 1-dioxide (12a), when tested in combination with piperacillin, showed excellent synergistic activity against microorganisms producing plasmid-mediated enzymes, but had insufficient activity against microorganisms producing chromosomally mediated class I enzymes.

著者

CHAEUK IM SAMARENDRA N. MAITI RONALD G. MICETICH MOHSEN DANESHXALAB KEVIN ATCHISON OLUDOTUN A. PHILLIPS CHIEKO KUNUGITA

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.47, no.9, pp.1030-1040, 1994-09-25 (Released:2006-04-19)

参考文献数

15

被引用文献数

31 42

---

The synthesis of β-lactamase inhibitory activity of a series of sodium 6-[(1-heteroarylthioethyl-1, 2, 3-triazol-4-yl)methylene]pemcillanate 1, 1-dioxides are described. Their activity was compared with tazobactam and sulbactam. The Z-isomers were more active than the E-isomers. The in vitro activity of the Z-isomers of the phenylthiadiazole derivatives (13a and 15a) was better than sulbactam against the tested β-lactamases and comparable to tazobactam especially against TEM-2 and cephalosporinase. But their synergistic activity with five antibiotics was inferior to tazobactam.

著者

NAO-AKI WATANABE KANEMASA KATSU

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.45, no.8, pp.1335-1345, 1992-08-25 (Released:2006-04-19)

参考文献数

33

被引用文献数

1 1

---

The bactericidal activity of cefclidin (E1040), a new cephalosporin, against a clinical strain of Citrobacter freundii was compared with that of ceftazidime in a two-compartment in vitro pharmacokinetic model system designed to simulate plasma concentrations in humans for 12 hours after intravenous administration of a 1 g dose. Both cefclidin and ceftazidime showed rapid bactericidal activity against C. freundii. However, during the simulation of ceftazidime treatment, regrowth was observed after two hours and a subpopulation emerged which was resistant to ceftazidime. Neither regrowth nor the emergence of resistant mutants was observed with cefclidin during the 12-hour simulation. The ceftazidime-resistant mutants constitutively overproduced β-lactamase at levels which were about 500-fold higher than that of the parent wild-type strain. Against this β-lactamase overproducing mutant, no bactericidal activity of ceftazidime was observed in the in vitro model system, whereas the bactericidal activity of cefclidin was observed during the 12-hour period. The emergence of Enterobacter cloacae mutants derepressed for β-lactamase production was also observed with ceftazidime but not cefclidin. The affinity of cefclidin for the β-lactamase isolated from these mutants was lower than that of ceftazidime, and the kinetic parameters of enzymatic hydrolysis showed that cefclidin was hydrolyzed more slowly at a low concentration (0.2μM) than was ceftazidime. It is suggested that the high activity of cefclidin against strains derepressed for β-lactamase plays a major role in the absence of emergence of resistant mutants.

著者

KUNIAKI TATSUTA HIROSHI MUKAI MASAAKI TAKAHASHI

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.53, no.4, pp.430-435, 2000-04-25 (Released:2008-09-19)

参考文献数

14

被引用文献数

13 29

著者

YUKIHIKO KANIEDA NAOKI ASANO MASANORI TERANISHI KATSUHIKO MATSUI

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.33, no.12, pp.1573-1574, 1980 (Released:2006-04-12)

参考文献数

4

被引用文献数

32 42

著者

YUKIHIKO KAMEDA NAOKI ASANO MICHIYO YOSHIKAWA KATSUHIKO MATSUI

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.33, no.12, pp.1575-1576, 1980 (Released:2006-04-12)

参考文献数

5

被引用文献数

41 52

著者

AKIRA ENDO

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.32, no.8, pp.852-854, 1979 (Released:2006-04-12)

参考文献数

3

被引用文献数

146 522

著者

BRIGITTE SCHLEGEL UDO LUHMANN ALBERT HÄRTL UDO GRÄFE

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.53, no.9, pp.973-974, 2000-09-25 (Released:2008-09-19)

参考文献数

4

被引用文献数

6 15

著者

YASUHIRO IGARASHI KATSUYUKI FUTAMATA TSUYOSHI FUJITA AKIRA SEKINE HISATO SENDA HIDEO NAOKI TAMOTSU FURUMAI

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.56, no.2, pp.107-113, 2003-02-25 (Released:2009-01-27)

参考文献数

9

被引用文献数

38 91

---

In the screening of novel antifungal compounds, yatakemycin was found in the culture broth of Streptomyces sp. TP-A0356. Yatakemycin was obtained by solvent extraction of the fermentation broth and chromatographic purification using ODS column and preparative HPLC. The structure of yatakemycin was elucidated by NMR and CID-MS/MS experiments as a novel antibiotic belonging to a family of CC-1065 and duocarmycins known to be DNA alkylating agents. Yatakemycin inhibited the growth of pathogenic fungi such as Aspergillus fumigatus and Candida albicans with the MIC values of 0.01-0.03μg/ml, more potent than amphotericin B (MIC: 0.1-0.5μg/ml) or itraconazole (MIC: 0.03-0.2μg/ml). It also showed potent cytotoxicity against cancer cell lines with the IC50 of 0.01-0.3μg/ml.

著者

KATSUTOSHI TAKAHASHI HISAO EKIMOTO SHOKO AOYAGI AKIKO KOYU HIROSHI KURAMOCHI OSAMU YOSHIOKA AKIRA MATSUDA AKIO FUJII HAMAO UMEZAWA

出版者

JAPAN ANTIBIOTICS RESEARCH ASSOCIATION

雑誌

The Journal of Antibiotics (ISSN:00218820)

巻号頁・発行日

vol.32, no.1, pp.36-42, 1979 (Released:2006-04-12)

参考文献数

12

被引用文献数

30 31

---

Pepleomycin (PEP), 3-[(S)-1'-phenylethylamino]propylaminobleomycin has potent activity and is less pulmonary toxic than bleomycin (BLM). Biological activity and toxicity of the following degradation products of PEP have been studied in detail: the product of carbamoyl migration (ISO), the product of decarbamylation (DC), the product of ring closure of the side chain on the pyrimidine moiety (RC), the depyruvamide product (DP) and the product of an enzymatic inactivation (DA). These degradation products showed much lower activity than PEP in vitro: antimicrobial and anti-HeLa activities, inhibition of DNA synthesis in AH66 cells and the DNA strand cleavage. Acute toxicity and pulmonary toxicity were tested in mice. Results indicated much lower acute toxicity corresponding to the decreased in vitro activity when compared to PEP. DP and RC did not cause lung fibrosis in mice, while ISO and DC showed 1/2.6 and 1/5.7 degree of pulmonary toxicity, respectively, in comparison with PEP.