All issues
Volume 44, Issue 12
Displaying 1-30 of 30 articles from this issue
- |<
- <
- 1
- >
- >|
-
Hiroaki TAKAYANAGI, Toshitsugu KAI, Shin-ichi YAMAGUCHI, Kazuyoshi TAK ...1996 Volume 44 Issue 12 Pages 2199-2204
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe crystal and molecular structures of the title compounds have been elucidated by X-ray structure analysis.All compounds are formed through ionic and hydrogen bondings in the crystal state. The picrates of N-methylanine and m-phenylenediamine have additional π-bondings. The picrates are 1 : 1 complex except for o-phenylenediamine picrate, in which the picrate consists of one o-phenylenediamine and two picric acid molecules.View full abstractDownload PDF (764K) -
Hiroshi HARADA, Toshiya MORIE, Yoshimi HIROKAWA, Shiro KATO1996 Volume 44 Issue 12 Pages 2205-2212
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSwern oxidation of 2-substituted amino-1, 3-propanediols 20a-d, 38, 41, and 42 smoothly proceeded to give the oxidative dehydration products, 2-substituted aminopropenals 17a-d, 43, 45 and 46, respectively. Reaction of the intriguing 2- substituted aminopropenals 17a-d with N-benzyl-N'-methyl- or N, N'-dimethylethylenediamine(12o or 12p) followed by NaBH4 reduction of the iminium salt intermediates afforded the corresponding 6-substituted aminohexahydro-1H-1, 4-diazepines 16 and 24-28. The similar ring formation of 1H-indazole derivatives 43 and 45 employing 12o directly furnished the 1H-dindazole-3-carboxamide 4, which showed a potent serotonin-3(5-HT3) receptor antagonistic activity.View full abstractDownload PDF (1105K) -
Takeshi ITABASHI, Nobuko OGASAWARA, Koohei NOZAWA, Ken-ichi KAWAI1996 Volume 44 Issue 12 Pages 2213-2217
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new azaphilone derivatives designated falconensins E5 (5), F (6), and G (7) were isolated from the mycelium o Emericella falconensis, along with falconensins A (1), B (2), C (3), D (4), and H (8), and three hopane-type triterpenes, zeorin (9), hepane-7β, 22-diol (10), and hopane-6α, 7β, 22-triol (11). The structures of 5-7 were confirmed by spectroscopic investigation and chemical correlations. The absolute stereochemistry of falconensins A (1) to G(7) was also established.View full abstractDownload PDF (785K) -
Kunihiko MOHRI, Junko MAMIYA, Yuka KASAHARA, Kimiaki ISOBE, Yoshisuke ...1996 Volume 44 Issue 12 Pages 2218-2222
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe oxidative decarboxylation reactions of arylacetic acids to arylcarbinols were compared for Mn(III) acetate, Ce(IV) ammonium nitrate and a combination reagent of Co(III) acetate-Cu(II) acetate. The reaction with Mn(III)acetate in acetic acid gave the corresponding arylcarbinyl acetate usually in good yield. The reaction was particularly easy when the substrate carried an electron-donating group at the para position of the aromatic ring, or when the acid was secondary or tertiary. In contrast, the product generated with the other reagents was either a mixture containing over-oxidation products or products formed via a different route.View full abstractDownload PDF (694K) -
Hitoshi ABE, Akira YAMASAKI, Hiroyuki FUJII, Takashi HARAYAMA1996 Volume 44 Issue 12 Pages 2223-2226
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of benzyl alcohol with a new reagent system, benzene- or methaneselenolate anion-aluminum chloride, yielded the corresponding selenide. The one-pot conversion of benzaldehyde into benzyl selenide was also achieved by this system.View full abstractDownload PDF (629K) -
Hideyuki TAKAHASHI, Koohei NOZAWA, Ken-ichi KAWAI1996 Volume 44 Issue 12 Pages 2227-2230
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree new yellow pigments, designated epurpurins A-C (1-3), were isolated along with variecolin and emindole PA from the dichloromethane extract of rice fermented with Emericella purpurea. Compounds of 1-3 were established as 2, 3-dicyano-1, 4-di(4-hydroxyphenyl)-1, 3-butadiene derivatives by spectroscopic and chemical investigation and X-ray analysis of the dimethyl ether of epurpurin C (4).View full abstractDownload PDF (655K) -
Chihiro ITO, Hideki OHTA, Hugh T.-W. TAN, Hiroshi FURUKAWA1996 Volume 44 Issue 12 Pages 2231-2235
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeven new carbazole alkaloids, named clauszolne-A (1), -B (2), -C (3), -D (4), -E (5), -F (6), and -G (7), and a new coumarin named 5-geranyloxy-7-hydroxycomarin (8) were isolated from stem bark of Clausena excavata(Rutaceae) collected in Singapore, and their structures were elucidated by means of spectral methods.View full abstractDownload PDF (822K) -
Takashi TANAKA, Nobuko UEDA, Hideo SHINOHARA, Gen-ichiro NONAKA, Toshi ...1996 Volume 44 Issue 12 Pages 2236-2242
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHPLC comparison of tannins in the bark, sapwood and heatwood of Castanea crenata showed striking differences of composition. The major tannin of the bark is hamamelitannin, whereas vescalagin and castalagin are dominant in the wood. Inner heatwood contained three new C-glycosidic ellagitannin metabolites, castacrenins A, B and C. Outer heartwood contained dimeric, trimeric (castanenin A), tetrameric (castaneanins B and C) and pentameric (castaneanin D) C-glycosidic ellagitannins composed of vescalagin and castalagin units. Castacrenins and castaneanins are derived from vescalagin and castalagin by intramolecular and intermolecular dehydration, respectively.View full abstractDownload PDF (1090K) -
Kazuko YOSHIKAWA, Nahoko OKADA, Yukiko KAN, Shigenobu ARIHARA1996 Volume 44 Issue 12 Pages 2243-2248
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structural elucidation of seven related oxypregnane-oligoglycosides stephanosides K (1), L (2), M (3), N(4), O (5), P (6), and Q (7) from the fresh stem of Stephanotis lutchuensis var. japonica (Asclepiadaceae) was achieved through on a detailed study of their high-field 1H- and 13C-NMR spectra. The results show that all the sugars are β (1→4)-linked. The aglycones of stephanosides K, M, and O, and stephanosides L, N, and P were identified as 12-O-cinnamoyl-20-O-(E)-2-methyl-2-butenoyl, and 12-O-cinnamoyl-20-O-nicotinoyl derivatives of(20S)-pregn-6-ene-3β, 5α, 8β, 12β, 14β, 17β, 20-heptaol, respectively. The aglycone of stephanoside Q was 12-O-cinnamoyldeacetylmetaplexigenin (kidjoranin).View full abstractDownload PDF (839K) -
Motomasa KOBAYASHI, Taifo MAHMUD, Naoki YOSHIOKA, Kazuyuki HORI, Hirot ...1996 Volume 44 Issue 12 Pages 2249-2253
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new stilbeno-phenylpropanoid named kompasinol A (1), together with four known compounds, was isolated from the bark of Koompassia malaccensis (Fabaceae), an Indonesian medicinal plant collected in Sumatra Island, Indonesia. The chemical structure of kompasinol A (1) has been elucidated on the bases of its chemical and physicochemical properties.View full abstractDownload PDF (705K) -
Ken-ichi SAEKI, Masato TOMOMITSU, Yutaka KAWAZOE, Kunitaka MOMOTA, Hir ...1996 Volume 44 Issue 12 Pages 2254-2258
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThirteen kinds of fluorinated derivatives of benzo[h]quinoline and benzo[f]quinoline were synthesized by means of the Schiemann reaction or Skraup reaction, or by an electrolytic method. The synthesized derivatives carry one or two fluorine atoms at the bay-region, the K-region, and/or on the pyridine moiety of the molecules. These compounds can be used as models to examine the effect upon genotoxicity of fluorine substitution at appropriate sites on aromatic rings. Physicochemical and spectroscopic data of the fluorinated derivatives are given.View full abstractDownload PDF (847K) -
Yoshio OKADA, Hiroaki TAGUCHI, Toshio YOKOI1996 Volume 44 Issue 12 Pages 2259-2262
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2(1H)-Pyrazinone ring-containing natural products, flavocol, deoxymuta-aspergillic acid and finally optically active deoxyaspergillic acid, were easily synthesized by a newly developed procedure for preparation of 2(1H)-pyrazinone derivatives from dipeptidyl aldehyde hydrochlorides. The absolute configuration of natural deoxyaspergillic acid was synthetically determined as S.View full abstractDownload PDF (738K) -
Vilma M. DE AMBROSINI, Silvia GONZALEZ, Gabriela PERDIGON, Aida P. DE ...1996 Volume 44 Issue 12 Pages 2263-2267
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to examine the relationship between biological activities and the cell wall content, the murein type and the teichoic acid of the cell wall from five strains of bacteria were studied. Two of these Lactobacillus casei CRL 431 and L. acidophilus CRL 730, are used in a commercial fermented milk (BIO MILK), which is believed to be beneficial for bealth. The other strains, Lactococcus lactis CRL 526, Pediococcus pentosaceus CRL 923 and Propionibacterium acidipropionici CRL 1198 were included in order to compare the cell wall structures of active and inactive strains.A method was designed to confirm the amino acids of the peptidoglycan in impure substrates.Four of the studied strains, L. casei, L. acidophilus, L. lactis and P. acidipropionici, contained glycerol teichoic acids. L. casei, L. acidophilus, P. pentosaceus and L. lactis contained A4α type murein, while P. acidipropionici contained A3γ type.The capacity of orally administered peptidoglycans of the studied strains to stimulate phagocytosis by mouse peritoneal macrophages was analyzed. Only the PG of L. casei showed this activity. No differences were observed between active and inactive strains with respect to the chemical composition of the peptidoglycan. Therefore the biological activity is unlikely to be due to the peptidoglycan structure.View full abstractDownload PDF (711K) -
Keisuke MIYAJIMA, Kiyoshi IKEDA, Kazuo ACHIWA1996 Volume 44 Issue 12 Pages 2268-2273
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNew N-acylated L-serine-containing non-phosphorylated and phosphorylated D-glucosamine derivatives structurally corresponding to the lipid A disaccharide backbone were synthesized. Compounds 2, 4 and 5 exhibited potent mitogenic activity. Further, compound 5 showed nitric oxide (NO) productivity.View full abstractDownload PDF (972K) -
Tochiro TATEE, Aya NARITA, Kazuhisa NARITA, Giichi IZUMI, Takashi TAKA ...1996 Volume 44 Issue 12 Pages 2274-2279
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWater-soluble forskolin and 7-deacetylforskolin derivatives with an aminoacetyl, a 3-aminopropionyl, or a 4-aminobutyryl group at the 6- or 7-position were prepared, and their positive inotropic as well as vasodilative activities were evaluated in anesthetized dogs.7-Deacetylforskolin (2) and 7-deacetyl-1-silylforskolin (6) were converted to the corresponding 7-chloroacylderivatives (3, 7, 10), which were reacted with amines to obtain 7-aminoacyl-7-deacetylforskolins (4a-f, 9a, b, 11). The 7-acyl substituents migrated to the 6-position with sodium hydroxide in acetonitrile-water to afford 6-aminoacyl-7-deacetylforskolins (12a-f). The 7-position of 12a, d-f was selectively acetylated with acetyl chloride to obtain the corresponding 6-aminoacylforskolins (13a-d).Among the 6-aminoacylforskolins, 6-(3-dimethylaminopropionyl)forskolin (13b) and 6-(4-dimethylaminobutyryl)forskolin (13d) exhibited potent positive inotropic and vasodilative activities comparable to those of forskolin (1).The activities of 13b and 13d were approximately ten times more potent than those of 7-aminoacyl- and 6-aminoacyl-7-deacetylforskolins (4a-f, 9a, 12a-c, f). 6-Dimethylaminoacetylforskolin (13a) and 6-(3-diethylaminopropionyl)forskolin (13c) were less potent than 1. The effects of the soluble forskolins on adenylate cyclase activity were also examined in vitro. 6-Aminoacylforskolins (13a-d) exhibited potent adenylate cyclase-stimulating activity, comparable to that of 1.View full abstractDownload PDF (785K) -
Hiroyoshi WATANABE, Susumi HATAKEYAMA, Kazuki TAZUMI, Seiichi TAKANO, ...1996 Volume 44 Issue 12 Pages 2280-2286
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs putative metabolites of 1α, 25-diydroxy-22-oxavitamin D3 (OCT), 24-hydroxylated OCT in 24(R) and 24(S) forms, 24-ketoOCT, 26-hydroxylated OCT in 25(S) and 25(R) forms, pentanorOCT and pentanor-ketoOCT were synthesized from the steroidal 20(S)-alcohol. Their antiproliferation activities towards human promyelocytic leukemia cells (HL-60 cells) are also reported. Oxidized derivatives at the C-24 position, 24-ketoOCT, 24(R)-hydroxylated OCT and 24(S)-hydroxylated OCT, showed activities comparable to or slightly weaker than that of OCT, while 26-hydroxylated OCT was less active than OCT. Truncated OCT, pentanor OCT and pentanor-ketoOCT, were inactive at 10-7-10<-10> M.View full abstractDownload PDF (1121K) -
Hiroharu MATSUOKA, Noriaki MARUYAMA, Hiroshi SUZUKI, Toshio KUROKI, Ke ...1996 Volume 44 Issue 12 Pages 2287-2293
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNovel methotrexate (MTX) derivatives with either a mono- or dialkyl-substituted benzene ring were synthesized and initially tested for in vitro anti-proliferative activities using human perpheral blood mononuclear cells (hPBMC)derived from healthy volunteers and synovial cells (hSC) derived from patients with rheumatoid arthritis (RA).Compounds with potent activities were further evaluated in an in vivo adjuvant arthritis model. In comparison with MTX, a glutamate derivative 3a was more potent as a suppressor of the in vitro cell proliferation and the in vivo experimental arthritis, and a homoglutamate derivative, 3e, exhibited fairly good activities in vitro and considerable activity in vivo in a dose-dependent manner. As expected, 3e did not act as a substrate of folylpolyglutamate synthetase (FPGS), and thus did not undergo polyglutamation, which is thought to be responsible for side-effects that occur during MTX therapy.View full abstractDownload PDF (1057K) -
Hatsuo MAEDA, Munenori ITAMI, Yuji YAMAUCHI, Hidenobu OHMORI1996 Volume 44 Issue 12 Pages 2294-2299
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe surface conditions of glassy carbon (GC) electrodes anodized in n-CnH2n+1OH (2=2, 4, 6, 8 : electrodes 1-4), HO(CH2)nOH (n=2-5 : electrodes 5-8), and HO(CH2CH2O)2CH2CH2OR (R=H, Me : electrodes 9 and 10) were explored by measuring the wettability and capacitance as well as the voltammetric response to Fe(CN)3-6;wetting properties were evaluated by the contact angle formed by a drop of water; the ratio between the values of capacitance obtained before and after the anodic modification was used instead of the capacitance itself. The data have revealed that LiClO4 is recommended rather than conc. H2SO4 as a supporting electrolyte to fix 1-alkanol molecules more effectively to GC electrode surfaces in the anodic modification. The surface conditions of electrodes 1-10 have reflected the indentities of the modifer remarkably : electrodes 1-4 have surfaces with hydrophobicity and thickness correlated to the length of carbon chains of the modifiers; on the other hand, the surfaces of electrodes 5-10 are hydrophilic, which seemed to allow each of the modified electrodes, except for electrode 8, to have a double layer with a thickness similar to a bare GC electrode. The suppression in the electrode reaction of Fe(CN)3-6 was stronger at electrodes 6 and 8 than at electodes 5 and 7, which can be explained by the invocation of an"odd-even" effect.View full abstractDownload PDF (945K) -
Kaoru UMEHARA, Mitsuhiro NAKAMURA, Toshio MIYAKE, Masanori KUROYANAGI, ...1996 Volume 44 Issue 12 Pages 2300-2304
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the previous paper, we reported the differentiation inducing activities of lignoids from Arctium Fructus (the fruits of Arctium lappa L., Compositae) against mouse myeloid leukemia cells (M1). We reinvestigated the active components of this extract and isolated three new dilignans. Furthermore, structure modifications were carried out using the most active lignan (arctigenin, 1) and its structure-activity relationship was investigated. Its aliphatic esters were more effective in inducing the differentiation of M1 cels than its aromatic esters. Especially, n-decanoate, which was the most active derivative, induced more than half of the M1 cells into phagocytic cells at a concentration of 2 μM.View full abstractDownload PDF (676K) -
Yoshiki MINO, Katsuki YAMADA, Toyonori TAKEDA, Osamu NAGASAWA1996 Volume 44 Issue 12 Pages 2305-2308
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA manganese-containing component from the water-extract of Theae folium (green tea) was found to exert an augmentative effect in magnetic resonance imaging (MRI) contrast and may possibly be a manganese(II) complex with a pectin-like polysaccharide capable of shortening the spin-lattice relaxation time (T1) of water protons. Even though only the manganese(II) ion with S=5/2 is active in T1-shortening ability, which should enhance contrast, complexation of this ion with the polysaccharide causes a marked increase in its activity. This manganese-containing pectin-like polysaccharides should prove useful as a low-toxic oral gastrointestinal contrast material in MRI.View full abstractDownload PDF (757K) -
Katsuhiko YANO, Atsushi KAJIYAMA, Shigeru YAMAZAKI, Yoshisuke MATSUMUR ...1996 Volume 44 Issue 12 Pages 2309-2313
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWe investigated the physicochemical and pharmaceutical properties of a solid dispersion (SD) derived from a solution of the poorly water-soluble drug (R)-1-[2, 3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1, 4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), hydroxypropylmethylcellulose 2910 (TC-5E) and polyoxyethylene hydrogenated caster oil 60 (HCO-60). Colloidal particles produced when the SD was dispersed into water had a mean diameter of 160 nm and contained 67-77% YM022. Powder X-ray diffractometr showed that YM022 existed in the colloidal particles in an amorphous state. The particle diameter and YM022 content remained unchanged during storage for 7 d, confirming that the colloidal solution was stable. On oral administration to rats, good absorption was observed for both the colloidal solution prepared immediately before and the sample stored for 7 d before administration. Thus, the stability of this colloidal solution of SD was confirmed by in vitro storage tests and by in vivo absorption experiments in rats.View full abstractDownload PDF (717K) -
Ryuji NIWA, Hitoshi KAMADA, Eiki SHITARA, Jiro HORIUCHI, Nobuyuki KIBU ...1996 Volume 44 Issue 12 Pages 2314-2317
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of cyanogen bromide (1) with primary amines (2a-p), including arylmethylamines (2l-p), gave the corresponding cyanamides (3a-p). Trimerization of 3a-p gave 1, 3, 5-trisubstituted 2, 4, 6-triiminohexahydro-1, 3, 5-triazines (isomelamines) (4a-p), which were treated with hydrochloric acid to give the corresponding 1, 3, 5-trisubstituted 2, 4, 6-trioxohexahydro-1, 3, 5-triazines (isocyanurates) (5a-c, f) and 1, 3, 5-trisubstituted 2-imino-4, 6-dioxohexahydro-1, 3, 5-triazines (5b'-e'). Biological evaluation of 4a-p, 5a-c, f, and 5b'-e' was carried out, and some of these compounds showed bronchodilator and positive inotropic activities.View full abstractDownload PDF (572K) -
Taisuke ITAYA, Yasutaka TAKADA, Tae KANAI, Tozo FUJII1996 Volume 44 Issue 12 Pages 2318-2321
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn treatment with boiling 2 N hydrochloric acid for 48 h, N6-methyl-8-oxoadenosine (1), 1-methyl-8-oxoadenosine (5), and 7-methyl-8-oxoadenosine (8) underwent glycosidic hydrolysis, though much more slowly than the corresponding 8-unsubstituted compounds, furniching the aglycons (2, 6, and 9) in 45%-63% yields. Under these conditions, N6-methyl-8-oxoadenine (2) rearranged to 9-methyl-8-oxoadenine (3) (8% yield), presumably through fission and reclosure of the imidazole ring. Apparent methyl migration also occurred with 3-methyl-8-hydroxyadenine (7), which afforded 1-methyl-8-oxoadenine (6) in 9% yield on treatment with hydrochloric acid under similar conditions.View full abstractDownload PDF (605K) -
Tadashi SHIRAIWA, Hideya MIYAZAKI, Atsushi OHTA, Yukitaka WAKI, Masahi ...1996 Volume 44 Issue 12 Pages 2322-2325
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS(RS)-α-Amino-γ-butyrolactone hydrochloride [(RS)-ABL·HCl] was found to exist as a conglomerate based on the infrared spectrum, solubility, and melting point. Optical resolution by preferential crystallization of(RS)-ABL·HCl was achieved to yield (R)- and (S)-ABL·HCl. The obtained (R)- and (S)-ABL·HCl were recrystallized, taking into account the solubility of (RS)-ABL·HCl to give optically pure (R)- and (S)-ABL·HCl.View full abstractDownload PDF (627K) -
Hong-Woo LEE, Eung-Nam KIM, Hoe-Joo SON, Soon-Kil AHN, Koo-Hun CHUNG, ...1996 Volume 44 Issue 12 Pages 2326-2330
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of new carbapenem derivatives, which have a pyrrolidin-4-ylthio group substituted with a hydroxyalkyl or carbamoyl group at the 2' position as the C-2 side chain, have been prepared. The antibacterial activity and the stability to renal dehydropeptidase-I of these compounds were investigated, and the structure-activity relationships were studied. Among these new carbapenems, (1R, 5S, 6S)-2-[(2S, 4S)-2-{(2-hydroxy)ethylmercaptomethyl}pyrrolidin-4-ylthio]-6-[(1R)-1-hydroxyethyl]-1-methyl-1-carbapen-2-em-3-carboxylic acid (1a) showed the most potent and well balanced activity and was selected as a candidate for further evaluation.View full abstractDownload PDF (686K) -
Synthesis and Antiviral Activity of 6-Chloropurine Arabinoside and Its 2'-Deoxy-2'-fluoro DerivativeTokumi MARUYAMA, Yoshiko SATO, Yuri OTO, Yuka TAKAHASHI, Robert SNOECK ...1996 Volume 44 Issue 12 Pages 2331-2334
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS6-Chloropurine arabinoside (3a) was obtained by treatment of the 2'-O-acetylated congener (2) with ammonia in methanol. The 3', 5'-di-O-tritylated riboside (6) was allowed to react with diethylaminosulfur trifluoride (DAST)in the presence of pyridine to give the 2'-deoxy-2'-fluoroarabinoside (7), from which 6-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)purine (3b) was obtained. The antiviral effects of 3a and 3b were assayed against several DNA and RNA viruses. Only 3a displayed potent activity against varicella-zoster virus (VZV). This antiviral activity was dependent on phosphorylation by the VZV-induced thymidine kinase (TK). Compound 3a showed moderate activity against other DNA viruses, herpes simplex type 1 (HSV-1) and type 2 (HSV-2), and vaccinia virus. They were equally active against TK- and TK+ strains of HSV-1, which suggests that the HSV-1-encoded TK does not play a role in the anti-HSV-1 activity. No activity was noted with any of the compounds against various RNA viruses, including human immunodeficiency virus, at subtoxic concentrations.View full abstractDownload PDF (606K) -
Masahiro FUKAHORI, Sakae AKATSU, Hiroshi SATO, Toshihisa YOTSUYANAGI1996 Volume 44 Issue 12 Pages 2335-2337
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effects of the structures of non-ionic sufactants on the uptake of butyl p-hydroxybenzoate (BP) into Escharichia coli cells and its antibacterial activity were systematically studied using polyoxyethylene alkyl ethers(PAEs) poseessing various oxyethylene and hydrocarbon chain lengths. The uptake of BP into bacterial cells in an aqueous PAE solution was proportional to free BP in an aqueous phase, depending on the structures of PAEs. The antibacterial activity of BP decreased in the presence of PAEs, whereas it was greather than that anticipated from free BP. However, only PAE with 12 carbons in the hydrophobic group caused unusual increases in the uptake and antibacterial activity of BP, and the surfactant was more extensively incorporated into bacterial cells, differing from other PAEs, which were much less incorporated.The PAEs were thus concluded to increase the susceptibility of bacteria against BP due to direct interactions with the cells. Particularly, the PAE with 12 carbons in the hydrophobic group, which penetrated abundantly into the cells, might result in an increase in the fluidity of the cellular lipid matrix and a decrease in the resistance of drug permeation.View full abstractDownload PDF (552K) -
Rdahila BORISSOVA, Elena KIROVA1996 Volume 44 Issue 12 Pages 2338-2339
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt has been proposed that the parameter of relative effectiveness coefficient (REC) be used for the qualitative assessment of toothpastes containing active ingredients. REC is the ratio between the concentration of the active component in water eluates obtained after three minutes and adequately prolonged (up to the reaching of equilibrium state) dispersion of the toothpaste in distilled water at a 1 : 4 ratio (condition simulating the use of toothpaste in the oral cavity). The change in REC after storage following its production, as well as testing the toothpaste stability at high and low temperatures, provides an evidence for deviations in its quality. REC was applied for the assessment of toothpastes containing 0.5% zinc citrate as an active ingredient.View full abstractDownload PDF (433K) -
Akira KAJI, Ryo SAITO, Yukako SHINBO, Noriki KIRIYAMA1996 Volume 44 Issue 12 Pages 2340-2341
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAsterriquinone (ARQ) diacetate : 2, 5-bis[1-(1, 1-dimethyl-2-propenyl)-1H-indol-3-yl]-3, 6-diacetoxy-2, 5-cyclohexadiene-1, 4-dione (3), was converted into ARQ monoalkyl ether (6) by treatment with a mixture of alcohol and K2CO3 under heating, followed by acidification. The reaction was shown to proceed via ARQ monoacetate monoalkyl ether (4) and ARQ monoacetal monoalkyl ether (5).View full abstractDownload PDF (370K) -
Shinzo HOSOI, Masakazu SATO, Motoyoshi NAGAO, Yoshisuke TSUDA1996 Volume 44 Issue 12 Pages 2342-2343
Published: December 15, 1996
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOxidation of (±)-demethylerysotramidine (2) with mCPBA gave the α-1, 2-epoxide (3) as a single product, which was methylated to 4, then treated with SmI2 in THF-MeOH to give 8-oxoerythratidine (5) in good yield. Finally, 5 was reduced with a LiAlGH4-AlCl3 combination to the natural alkaloid, (±)-erythratidine (1).View full abstractDownload PDF (367K)
- |<
- <
- 1
- >
- >|