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NAOKI TSUJI, MASAAKI KOBAYASHI, KAZUO NAGASHIMA, YOSHIHARU WAKISAKA, K ...
1976 年 29 巻 1 号 p.
1-6
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
A new antibiotic, trichostatin, was isolated from the metabolites of strains of
Streptomyces hygroscopicus. It is active against trichophytons and some fungi. The structure was determined to be a derivative of a primary hydroxamic acid by chemical and spectroscopic evidences.
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ISOLATION AND CHARACTERIZATION
NAOKI TSUJI, MASAAKI KOBAYASHI, YOSHIHARU WAKISAKA, YOSHIMI KAWAMURA, ...
1976 年 29 巻 1 号 p.
7-9
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
New antibiotics, griseusins A and B were isolated from a strain of
Streptomyces griseus. Both antibiotics have a 5-hydroxy-1, 4-naphthoquinone chromophore and their molecular formulae were determined to be C
22H
20O
10 and C
22H
22O
10, respectively. The griseusins are active against gram-positive bacteria.
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NAOKI TSUJI, KAZUO NAGASHIMA, MASAAKI KOBAYASHI, YOSHIHARU WAKISAKA, Y ...
1976 年 29 巻 1 号 p.
10-14
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
Two new antibiotics, A-218 and K-41, were isolated from strains identified as
Streptomyces hygroscopicus. The antibiotics are characterized as polycyclic polyether compounds and are active against gram-positive bacteria.
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SADAFUMI OMURA, MICHINORI SHIBATA, SADAO MACHIDA, JIRO SAWADA, NOBORU ...
1976 年 29 巻 1 号 p.
15-20
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
A new polyether antibiotic, lonomycin, was isolated from the culture of
Streptomyces ribosidificus strain TM-481. The antibiotic obtained as a sodium salt is a colorless prism having a molecular formula of C
44H
75O
14Na (M.W. 850), m.p. 188-189°C, and has no absorption maxima in the ultraviolet region. The infrared and NMR spectra of the antibiotic suggest the presence of a carboxyl and four methoxyl groups. Lonomycin shows antimicrobial activity against gram-positive bacteria.
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CHAO-MIN LIU, RALPH Jr. EVANS, LUCY FERN, THERON HERMANN, EDWARD JENKI ...
1976 年 29 巻 1 号 p.
21-28
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
A new polyether antibiotic, Ro 21-6150, has been isolated from culture broths of
Streptomyces hygroscopicus, strain X-14563. Ro 21-6150 has ionophore properties and is active
in vitro against gram-positive bacteria.
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CYNTHIA H. O'CALLAGHAN, R. B. SYKES, D. M. RYAN, R. D. FOORD, P. W. MU ...
1976 年 29 巻 1 号 p.
29-37
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
βCefuroxime is a new broad spectrum cephalosporin antibiotic for administration by injection. It is stable to most β-lactamases. It is active against gram-positive organisms, including penicillinase-producing staphylococci, and has wide activity against gram-negative bacilli including
Enterobacter and many strains of indole-positive
Proteus spp. The substance is also highly active against
Haemophilus influenzae and
Neisseria gonorrhoeae. Studies on human volunteers showed that it produced high, long-lasting blood levels with virtually complete recovery of unchanged antibiotic in the urine. No evidence of toxicity due to cefuroxime was found. Slight, short-lived pain followed intramuscular injection, and the compound was well tolerated intravenously.
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THE SYNTHESIS AND MICROBIOLOGICAL PRODUCTION OF A NOVEL AMINO ACID, L-2-AMINO-4-(2-AMINOETHOXY) BUTANOIC ACID
JAMES P. SCANNELL, DAVID L. PRUESS, HELEN A. AX, ABRAHAM JACOBY, MARTH ...
1976 年 29 巻 1 号 p.
38-43
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
A novel amino acid, L-2-amino-4-(2-aminoethoxy)-butanoic acid, was isolated from a fermentation broth of
Streptomyces sp. X-11, 085. It was shown to be identical with the chemical reduction product of an antimetabolite antibiotic, L-2-amino-4-(2-aminoethoxy)-
trans-3-butenoic acid, a co-product in the fermentation. Addition of the title compound to the fermentation led to an enhanced yield of the antimetabolitesuggesting that the saturated amino acid serves as a precursor for the antimetabolite.
A de novo chemical synthesis and enzymatic resolution of the title compound are also reported.
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INA HAUPT, EDITH SCHUHMANN, RUDOLF GEUTHER, HEINZ THRUM
1976 年 29 巻 1 号 p.
44-49
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
The action of the polyene macrolide antibiotics mycotrienin, pimaricin, lucensomycin, tetramycin, rimocidin, nystatin, filipin, lagosin, pentaene antibiotic 2814P, flavomycoin, flavofungin, hexaene antibiotic 5001P, and candicidin, including perhydro derivatives of them, on wall-less stable protoplast type L-form and normal rod form cells of
E. coli W 1655F
+ was studied. No inhibition of the normal rod form cells was detected. In contrast to these results the growth of the L-form cells was inhibited by all of the substances tested, with the exception of pimaricin.
Further experiments have shown that the differences in sensitivity of normal and L-form cells cannot be explained by differences in sterol content, the target site of polyene antibiotics in sensitive eukaryotic cells. According to our results it is obvious that the cell wall of the normal cells functions as a penetration barrier to polyene antibiotics.
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JYOTIRMOY NANDI, S. K. BOSE
1976 年 29 巻 1 号 p.
50-57
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
Versicolin is mainly active against
Trichophyton rubrum. It is inactivated by serum. However, attainable blood level can be fifteen to twenty times higher than the fungicidal concentration for as long as 4 hours after a single intravenous administration of the maximum tolerable dose of 25 mg/kg body weight of mouse. It has no haemolytic activity like other polypeptide antibiotics. Skin does not show the presence of any measurable amount of the antibiotic. It is excreted through urine to the extent of 65 % of the maximum tolerable dose of the antibiotic administered intravenously. Versicolin is effective against experimental infection by
T. rubrum in guinea pigs at dose as low as 2.5 mg/kg body weight. The antibiotic shows no sign of subacute toxicity at these curative doses.
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THE REACTION OF EHRLICH CELLS AND TRITICUM PLANT ROOTS TO SOME ANTINEOPLASTIC DRUGS ALONE AND IN COMBINATION WITH HUMAN SERUM
JØRGEN HILDEN, FOLKE RØNNIKE, HENNING SCHOU
1976 年 29 巻 1 号 p.
58-64
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
In two growth tests, one employing EHRLICH ascites tumor cells in suspension culture, the other employing intact roots of wheat (
Triticum sativum LAM.), the growth inhibiting action of bleomycin (BLM) was shown to be intensified by human serum. Practical consequences of the finding are suggested. No such serum-drug interaction has been demonstrated with other anti-tumor compounds, including methotrexate (MTX) and threosulphan (TRSF). Isolation of the active factor(s) in serum has not yet been attempted.
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STRUCTURE-ACTIVITY STUDIES RELATED TO CEFATRIZINE (SK&F 60771)
G.L. DUNN, J.R.E. HOOVER, D.A. BERGES, J.J. TAGGART, L.D. DAVIS, E.M. ...
1976 年 29 巻 1 号 p.
65-80
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
The synthesis of a series of related broad-spectrum 7-phenylglycyl cephalosporins with 3-heterocyclicthiomethyl substituents is described. The effects of benzene-ring hydroxylation and 3-substituent variation on the
in vitro antibacterial activity, height and duration of mouse serum levels, and effectiveness in protecting against bacterial infection in the mouse are examined. Included for comparison are cephalexin, cephaloglycin and their
ortho-,
meta- and
para-hydroxy derivatives. The biological properties examined were influenced by the position of the hydroxyl group and by the nature of the 3-substituent. The 7-(
p-hydroxyphenylglycyl)-3-heterocyclicthiomethyl analogs were found to produce significantly higher serum levels on oral administration to mice than their unhydroxylated counterparts. This effect was not observed with the 7-(
m-hydroxyphenylglycyl)-3-heterocyclicthiomethyl cephalosporins, nor with the
p-hydroxyphenylglycyl analog of cephalexin. While
m- and
p-hydroxylation had little effect on
in vitro activity the
oNS-hydroxyphenylglycyl cephalosporins tested had very low antibacterial activities and were not examined further. One derivative, 7-[R-2-amino-2-(4-hydroxyphenyl)acetamido]-3-(1H-1, 2, 3-triazole-4(5)-ylthiomethyl)-3-cephem-4-carboxylic acid (SK&F 60771) was found to have outstanding
in vitro and
in vivo activities along with oral and subcutaneous serum levels in the mouse that were significantly higher than those obtained with cephalexin. This derivative which has been given the generic name cefatrizine was selected for extensive additional biological evaluation.
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YOICHI NAKAI, YOSHIO KANAI, TAKESHI FUGONO, SHIGEHARU TANAYAMA
1976 年 29 巻 1 号 p.
81-90
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
1. The metabolic fate of
14C-cephacetrile was studied in rats and rabbits. The plasma level of intravenously injected cephacetrile decreased with half-lives of 17 and 22 minutes in rats and rabbits respectively, this decline being associated with a rapid appearance of the active metabolite, desacetylcephacetrile. Intramuscularly injected cephacetrile was rapidly absorbed by rats with a maximum plasma level at 20 minutes and a half-life of 16 minutes. Cephacetrile and desacetylcephacetrile did not enter erythrocytes. Cephacetrile was weakly bound to the plasma protein in the rat, rabbit and man.
2. Both in rats and rabbits, almost all of the injected radioactivity was excreted in the urine within 72 hours as the intact antibiotic and desacetylcephacetrile, only small amounts appearing in feces
via bile. Neither the γ-lactone of desacetyl-7-cyanacetamidocephalosporanic acid nor the violet-reddish pigment (CGP-695) produced from cephacetrile were detectable in the plasma or urine of the animals.
3. In rats given the labeled antibiotic intravenously, the radioactivity was widely distributed with concentrations being high in the kidney, plasma and liver, and lowest in the brain. The radioactivity crossed the rat placenta and appeared in the fetus. Radioactivity in these tissues disappeared as the plasma level declined.
4. During daily intramuscular injection of
14C-cephacetrile to rats, no significant changes were observed in the peak level of the plasma radioactivity or in the half-lives. In addition, dosing of the labeled antibiotic for 7 days caused no increase in tissue levels of radioactivity.
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KEN'ICHI YAMAZAKI, KIMIHIKO ABE, MITSUJI SANO
1976 年 29 巻 1 号 p.
91-92
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
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TOMIO TAKEUCHI, MASASHI MIYAMOTO, MASAAKI ISHIZUKA, HIROSHI NAGANAWA, ...
1976 年 29 巻 1 号 p.
93-96
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
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HAMAO UMEZAWA, TAKAAKI AOYAGI, HIROYUKI SUDA, MASA HAMADA, TOMIO TAKEU ...
1976 年 29 巻 1 号 p.
97-99
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
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HIROYUKI SUDA, TOMOHISA TAKITA, TAKAAKI AOYAGI, HAMAO UMEZAWA
1976 年 29 巻 1 号 p.
100-101
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
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HIKARU NAKAMURA, HIROYUKI SUDA, TOMOHISA TAKITA, TAKAAKI AOYAGI, HAMAO ...
1976 年 29 巻 1 号 p.
102-103
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
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RYOSUKE YAHASHI, ISAO MATSUBARA
1976 年 29 巻 1 号 p.
104-106
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
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HIDEO OTSUKA, JUN'ICHI SHOJI, KEIICHI KAWANO, YOSHIMASA KYOGOKU
1976 年 29 巻 1 号 p.
107-110
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー
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HIROSHI MAEDA, JIRO TAKESHITA
1976 年 29 巻 1 号 p.
111-112
発行日: 1976年
公開日: 2006/04/12
ジャーナル
フリー