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Volume 56, Issue 10
Displaying 1-29 of 29 articles from this issue
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Review
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Takeaki NaitoArticle type: Review
2008 Volume 56 Issue 10 Pages 1367-1383
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSNitrogen-containing compounds are core parts not only of natural and synthetic medicines but also of biologically active compounds including natural products. This review focuses on the development of new synthetic reactions for nitrogen-containing compounds via three methodologies: the reductive photocycloaddition reaction of enamides, radical addition reaction, and nucleophilic addition reaction. Newly developed reactions were successfully applied to the synthesis of various types of nitrogen-containing compounds including medicines, lead compounds to new drugs, natural alkaloids, and others.View full abstractDownload PDF (1085K)
Regular Articles
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Takuma Koseki, Hiraku Onishi, Yuri Takahashi, Minoru Uchida, Yoshiharu ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1384-1388
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSIt was attempted to produce novel furosemide (FS) fast-disintegrating tablets by direct compression. The combination of FS, microcrystalline cellulose, croscarmellose sodium and xylitol was used as the basic formulation, and sucrose stearic acid ester (SSE) was chosen as an additional additive. The tablets with SSE were prepared by the simple addition of SSE, using a lyophilized mixture of FS and SSE or using a FS/SSE mixture obtained by evaporation of their ethanol solution. Only the tablets, produced using the FS/SSE mixture obtained by organic solvent (ethanol) evaporation, showed hardness of more than 30 N and a disintegration time of less than 20 s, which were the properties suitable for fast-disintegrating tablets. These properties were considered to result from well-mixed and fine-powdered SSE and FS.View full abstractDownload PDF (663K) -
Toshihiko Ishizaka, Sachie Okada, Emi Tokuyama, Junji Mukai, Takahiro ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1389-1394
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThe objective of the study was to evaluate the bitterness, grittiness and uniformity of drug loading as measures of the quality of 12 formulations of clarithromycin dry syrup (CAMDS), comprising one branded and 11 generic products. Some of the generic CAMDS formulations were more bitter than the branded product while others had similar bitterness when tested as aqueous suspensions. Only one generic product was less bitter than the branded product when tested as a suspension in acidic sports drink. The usual dissolution test described in JP XV could not be used to evaluate the bitterness of the products. A brief dissolution test using only 12.5 ml of water was used to evaluate the bitterness of the products in aqueous suspensions. There were considerable variances in the grittiness of the various products, which were independent of particle size. Changes in grittiness level seemed to be correlated with changes in the intensity of bitterness due to the disintegration of the formulation. Finally, there was less variation in the uniformity of drug loading for the branded product than for the generic products. These data may be useful when selecting which CAMDS formulation to prescribe.View full abstractDownload PDF (1099K) -
Toshihiko Ishizaka, Sachie Okada, Emi Tokuyama, Junji Mukai, Takahiro ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1395-1399
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThe aim of the study was to suppress the bitterness and improve the palatability of pediatric prednisolone powder (PP) by the addition of simple sucrose syrup (SS) and various beverages and foods. Bitterness suppression was evaluated using the human gustatory sensory test. The suppression of the bitterness and improvement of palatability of PP by addition of SS solutions was investigated using standard taste substances: sucrose for sweetness, tartaric acid for sourness, and sodium chloride as saltiness. Dilution with SS solutions of up to 50% (w/w) was successful in bitterness-suppression and improvement of palatability, but at 80% (w/w) SS, the palatability of the diluted solution was reduced. The kinematic viscosities of SS solutions were therefore evaluated using the Uberorde viscosity meter, to see whether the high viscosity of the more concentrated solutions was responsible for the reduced palatability. The kinematic viscosity of the 80% SS was 16.60 mm2/s. Judging from above information, the palatability might become worse when the kinematic viscosity of syrup exceeded 15 mm2/s. Finally, the ability of various beverages and foods with low viscosity to suppress the bitterness and improve the palatability of PP were examined. The additions of orange juice or a carbonated lemon drink to simple syrup solution were most effective in suppressing bitterness and improving palatability of PP.View full abstractDownload PDF (196K) -
Qingang Yang, Lili Chen, Xuchang He, Zhenting Gao, Xu Shen, Donglu BaiArticle type: Regular Article
2008 Volume 56 Issue 10 Pages 1400-1405
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThe severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC50 of 1.06 μM.View full abstractDownload PDF (541K) -
Yukihiro Ikeda, Junko Ban, Tomoyasu Ishikawa, Shohei Hashiguchi, Shini ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1406-1411
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSTAK-599 (known as ceftaroline fosamil) is a novel N-phosphono type prodrug of a cephalosporin compound, T-91825, that exhibits strong activity against methicillin resistant Staphylococcus aureus (MRSA). The stability and stabilization of TAK-599 were investigated by kinetic analysis focused on crystallinity and moisture content. Initially it was planned to develop TAK-599 as an injectable formulation using the amorphous solid powder prepared by lyophilization. However, amorphous of TAK-599 free form was found to be chemically unstable even when stored at 8 °C, and thus development was focused on the crystalline material. After exhaustive screening of crystallization condition, the monoacetic acid solvate was found to yield TAK-599 in a crystalline form. Physicochemical properties were studied to identify the key factors affecting the stabilization of TAK-599 in order to improve long-term stability, and the results indicated that the crystallinity of TAK-599 correlated with stability. Furthermore, moisture content was also identified in our studies as an important factor in stabilizing TAK-599. TAK-599 containing about 3% moisture was found to be the most stable form. It was concluded that both sufficient crystallinity and strict moisture control of TAK-599 were essential to maintain long-term stability at 25 °C.View full abstractDownload PDF (233K) -
Shoichi Higo, Hirofumi Takeuchi, Hiromitsu Yamamoto, Tomoaki Hino, Yos ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1412-1416
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSTreatment composed of a gastric mucoadhesive antibiotic with slow release drug delivery is expected to be effective for the eradication of Helicobacter pylori (H. pylori). In this study, we evaluated the slow release property of the tetracycline–sucralfate acidic complex. Tetracycline was the antibiotic selected because of its complexation capacity with sucralfate. Sustained release was tested using two different dissolution test methods: paddle and flow-through cell. The adhesive paste formed from the acidic complex displayed a longer sustained release profile of tetracycline using flow-through cell method. The milder conditions of the flow-through cell method better mimicked the fasted state of the stomach, suggesting that the oral administration with fasting is appropriate for the acidic complex. Furthermore, the paste formation protected the tetracycline from decomposition under an acidic condition, which apparently contributes to long-term release. Change in the zeta potential of the acidic complex particles was helpful in clarifying the release mechanisms of the tetracycline. The data indicated that the immediate release of tetracycline in the early stage of the test was indispensable to the subsequent paste formation that enables slow release. If administrated orally with fasting, the acidic complex rapidly adheres to the gastric mucosa and sustains long-term release of the tetracycline to the gastric lumen or mucus layer. This antibiotic delivery mechanism, which requires only a minimum dosage, may be effective for efficient eradication of H. pylori.View full abstractDownload PDF (279K) -
Xiangli Liu, Hossam Hefesha, Hideji Tanaka, Gerhard Scriba, Alfred Fah ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1417-1422
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSWe propose a reversed phase HPLC (RP-HPLC) with an alkaline-resistant silica-based stationary phase, XBridgeTM Shield RP18, for the determination of the lipophilicity of drugs with diverse chemical nature ranging from acidic to basic. A set of 40 model compounds with well-defined solvatochromic parameters was selected to allow a broad distribution of structural properties. The chromatographic results showed that the lipophilicity index log kw obtained with XBridgeTM Shield RP18 was well correlated with experimental log Poct values (r2=0.96). Linear solvation free-energy relationship (LSER) analyses revealed that the retention mechanism of the stationary phase and 1-octanol/water partitioning were controlled by almost the same balance of intermolecular forces (hydrophobicity as expressed by the van der Waals volume Vw, H-bond acceptor basicity β, and dipolarity/polarizability π*). The results showed that XBridgeTM Shield RP18 phase overcomes the shortcomings of the silica-based stationary phases, the application of which to lipophilicity measurements had been limited to neutral and acidic compounds.View full abstractDownload PDF (189K) -
Magdalena Piętka-Ottlik, Halina Wójtowicz-Młochowska, ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1423-1427
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSDifferent N-substituted benzisoselenazol-3(2H)-ones, analogues of ebselen were designed as new antiviral and antimicrobial agents. We report their synthesis, chemical properties as well as study on biological activity against broad spectrum of pathogenic microorganisms (Staphylococcus aureus, Staphylococcus simulans, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Candida albicans, Aspergillus niger) and viruses (herpes simplex virus type 1 (HSV-1), encephalomyocarditis virus (EMCV), vesicular stomatitis virus (VSV)), in vitro. Most of them exhibited high activity against viruses (HSV-1, EMCV) and gram-positive bacteria strains (S. aureus, S. simulans), while their activity against gram-negative bacteria strains (E. coli, P. aeruginosa, K. pneumoniae) was substantially lower. Some of tested compounds were active against yeast C. albicans and filamentous fungus A. niger.View full abstractDownload PDF (124K) -
Herve Martial Poumale Poumale, Rivoarison Randrianasolo, Jeannot Victo ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1428-1430
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSTwo new flavonoid glycosides, namely 3′-(2″,4″-dihydroxybenzyloxy)acanthophorin B (1b) and β,2,3′,4,4′,6-hexahydroxy-α-(α-L-rhamnopyranosyl)dihydrochalcone (2) were isolated from the leaves of Psorospermum androsaemifolium together with quercetin (1), acanthophorin B (1a), α- (3) and β-amyrine (3a), vismiaquinone (4), 12-hentriacontanol and hentriacontane. The structures of these secondary metabolites were established using detailed spectroscopic analysis and by comparison with published data. Compounds 1, 1a, 1b, 2, 3, 3a and 4 showed weak antifungal and antibacterial activities.View full abstractDownload PDF (113K) -
Shouhei Aikawa, Naomi Fujita, Hidetoshi Myojo, Takashi Hayashi, Tadats ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1431-1435
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSA newly developed mini-scale high shear granulator was used for scale-up study of wet granulation process from 0.2 to 200 L scales. Under various operation conditions and granulation bowl sizes, powder mixture composed of anhydrous caffeine, D-mannitol, dibasic calcium phosphate, pregelatinized starch and corn starch was granulated by adding water. The granules were tabletted, and disintegration time and hardness of the tablets were evaluated to seek correlations of granulation conditions and tablet properties. As the granulation proceeded, disintegration time was prolonged and hardness decreased. When granulation processes were operated under the condition that agitator tip speed was the same, similar relationship between granulation time and tablet properties, such as disintegration time and hardness, between 0.2 L and 11 L scales were observed. Likewise, between 11 L and 200 L scales similar relationship was observed when operated under the condition that the force to the granulation mass was the same. From the above results, the mini-scale high shear granulator should be useful tool to predict operation conditions of large-scale granulation from its mini-scale operation conditions, where similar tablet properties should be obtained.View full abstractDownload PDF (4546K) -
Taichi Kusakabe, Keisuke Kato, Satoshi Motodate, Satoshi Takaishi, Hir ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1436-1437
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSA total synthesis of (+)-bakkenolide-A was carried out via the key intermediate 4, which was prepared based on an asymmetric cyclization-carbonylation reaction established in our laboratory. Diastereoselective construction of the spirolactone moiety was achieved using Mitsuhashi's protocol as a key step.View full abstractDownload PDF (96K) -
Toshio Morikawa, Haihui Xie, Tao Wang, Hisashi Matsuda, Masayuki Yoshi ...Article type: Regular Article
2008 Volume 56 Issue 10 Pages 1438-1444
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSFrom the methanolic extract of the whole plant of Sinocrassula indica (Crassulaceae), six new flavonol glycosides, sinocrassosides B4 (1), B5 (2), C1 (3), D1 (4), D2 (5), and D3 (6), were isolated together with 30 compounds. The structures of 1—6 were elucidated on the basis of chemical and physicochemical evidence. In addition, several constituents were found to show inhibitory effects on aminopeptidase N and aldose reductase.View full abstractDownload PDF (225K) -
Tsutomu Warashina, Toshio MiyaseArticle type: Regular Article
2008 Volume 56 Issue 10 Pages 1445-1451
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSTwelve new sesquiterpene and sesquiterpene glycosides were obtained along with eleven known compounds from the roots of Cichorium endivia (Compositae). The compounds were identified as guaianolide, germacrenolide and elemanolide, based on spectroscopic methods and chemical evidence.View full abstractDownload PDF (191K)
Notes
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Suk Woo Kang, Min Cheol Kim, Chul Young Kim, Sang Hoon Jung, Byung Hun ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1452-1454
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThe use of hyphenated LC-NMR and LC-MS techniques for the purpose of directly identifying the major constituents of Belamcanda chinensis was investigated. Reversed-phase isocratic chromatography was performed using an acetonitrile–water solvent system on a C18 column. The NMR spectrum yielded five main peaks, whose analysis revealed them to be 5, 6, 7, 3′-tetrahydroxy-4′-methoxyisoflavone (1), tectorigenin (2), iristectorigenin A (3), irigenin (4), and irisflorentine (5). The identification of these constituents was confirmed by performing LC-ESI-MS experiment. This study shows that hyphenated LC-NMR and LC-MS can be used for the rapid (70 min) identification of the isoflavonoids.View full abstractDownload PDF (182K) -
Jayabalan Nirmal, Srinivasan Saisivam, Chintalapati Peddanna, Selvadur ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1455-1458
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThe objective of the study is to formulate bilayer tablets consisting of atorvastatin calcium (AT) as an immediate release layer and nicotinic acid (NA) as an extended release layer. The immediate release layer was prepared using super disintegrant croscarmellose sodium and extended release layer using hydroxypropylmethyl cellulose (HPMC K100M). Both the matrix and bilayer tablets were evaluated for hardness, friability, weight variation, thickness, and drug content uniformity and subjected to in vitro drug release studies. The amount of AT and NA released at different time intervals were estimated by HPLC method. The bilayer tablets showed no significant change either in physical appearance, drug content or in dissolution pattern after storing at 40 °C/75% relative humiding (RH) for 3 months. The release of the drug from the tablet was influenced by the polymer content and it was much evident from thermogravimetry/differential thermal analysis (TG/DTA) analysis. The results indicated that the bilayer tablets could be a potential dosage form for delivering AT and NA.View full abstractDownload PDF (76K) -
Liang Zhou, Yaochun Zhang, Leslie Adell Gapter, Hui Ling, Rajesh Agarw ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1459-1462
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSA new lanostane-type triterpene, 29-hydroxypolyporenic acid C (8), was isolated from the dried sclerotia of Poria cocos together with eight other known compounds pachymic acid (1), dehydropachymic acid (2), 3-acetyloxy-16α-hydroxytrametenolic acid (3), polyporenic acid C (4), 3-epi-dehydropachymic acid (5), 3-epi-dehydrotumulosic acid (6), tumulosic acid (7), and dehydrotumulosic acid (9). The compounds were identified by spectral analysis and comparison with spectroscopic data reported in the literatures. Although none of the nine (1 to 9) compounds showed promising antioxidant activity, 1 through 6 and 8 showed good cytotoxicity against human lung cancer cell line A549 and human prostate cancer cell line DU145. Interestingly, all these compounds exhibited better cytotoxicity towards A549 than DU145 cells.View full abstractDownload PDF (97K) -
Xing-Guo Yan, Jing-Ming Jia, Ling Tang, Li-Ying Shi, Yong-Qi Wang, Bao ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1463-1465
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSStudies on the chemical constituents of roots of Urtica triangularis HAND-MASS have led to the isolation of four new compounds. The structures, including the absolute configurations, of these constituents have been elucidated through spectral studies including 1H-NMR, 13C-NMR, 2D-NMR experiments (heteronuclear single-quantum coherence, heteronuclear multiple bonding connectivity and nuclear Overhauser effect spectroscopy), high resolution mass spectroscopy (HR-MS) and circular dichroism as (−)-4-methoxy-8′-acetyl olivil, (−)-4-methoxy-8′-acetyl olivil-4-O-α-arabinopyronosyl-(1→6)-β-glucopyranoside, (−)-olivil-9-O-β-glucopyranoside and cyclo-olivil-9-O-β-glucopyranoside.View full abstractDownload PDF (88K) -
Joseph Ngoupayo, Turibio Kuiate Tabopda, Muhammad Shaiq Ali, Etienne T ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1466-1469
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSIn our continuous search for α-glucosidase inhibitors from plants, four new depsidones named brevipsidones A—D (1—4) were isolated from stem bark of Garcinia brevipedicellata together with known damnacanthal, scopoletin and a mixture of stigmasterol and β-sitosterol. Structural elucidations were made by spectroscopic analyses including 2D-NMR data.View full abstractDownload PDF (92K) -
Hiroyasu Imai, Kensuke Misawa, Hiroki Munakata, Yoshio UemoriArticle type: Notes
2008 Volume 56 Issue 10 Pages 1470-1472
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThe binding of amino acids to water-soluble zinc porphyrins in basic aqueous solution was spectrophotometrically analyzed. The amino acids were bound to the porphyrins through the coordination of the N atom with the central zinc ion. Additional attractions arise due to Coulomb interactions between the –COO− anion of the amino acids and the –N(CH3)3+ cation of the porphyrin substituents and due to hydrophobic interactions between the porphyrin plane and the hydrophobic substituents of the amino acids. These attractions could be explained based on the binding data. The compensatory relationships of ΔS and ΔH were also discussed.View full abstractDownload PDF (125K) -
Yusuke Hirasawa, Tomoyuki Tanaka, Jun'ichi Kobayashi, Nobuo Kawahara, ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1473-1476
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSA novel C19N-type Lycopodium alkaloid, malycorin A (1) consisting of a serratinane skeleton with 2-propanol unit has been isolated from the club moss Lycopodium phlegmaria, together with two new C16N-type alkaloids, malycorins B (2) and C (3), and the structures and relative stereochemistry were elucidated on the basis of spectroscopic data.View full abstractDownload PDF (330K) -
Yan Li, Chun-Lan Wang, Shun-Xing Guo, Jun-Shan Yang, Pei-Gen XiaoArticle type: Notes
2008 Volume 56 Issue 10 Pages 1477-1479
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSTwo new compounds were isolated from the stems of Dendrobium candidum: (R)-3,4-dihydroxy-5,4′,α-trimethoxybibenzyl (1), named dendrocandin A; and 4-[2-[(2S,3S)-3-(4-hydroxy-3,5-dimethoxyphenyl)-2-hydroxymethyl-8-methoxy-2,3-dihydrobenzo[1,4]dioxin-6-yl]ethyl]-1-methoxyl benzene (2), dendrocandin B. Five previously known bibenzyls were also identified: 4,4′-dihydroxy-3,5-dimethoxybibenzyl (3), 3,4-dihydroxy-5,4′-dimethoxybibenzyl (4), 3-O-methylgigantol (5), dendrophenol (6), and gigantol (7).View full abstractDownload PDF (92K) -
Ahmad Shaabani, Ali Hossein Rezayan, Marjan Heidary, Afshin SarvaryArticle type: Notes
2008 Volume 56 Issue 10 Pages 1480-1482
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSMeldrum's acid catalyzed the reaction of tetracyanoethylene with aromatic, heteroaromatic, and conjugated aldehydes led to arylidenemalononitrile in water in good yields at 80 °C. The work-up of reactions is very simple and the crude products are sufficiently pure to be used without further purification. The procedure provides an alternative method for the synthesis of arylidenemalononitrile.View full abstractDownload PDF (117K) -
In-Kyoung Lee, Jeong-Hyung Lee, Eui Il Hwang, Bong-Sik YunArticle type: Notes
2008 Volume 56 Issue 10 Pages 1483-1485
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThree new guaiane type sesquiterpenes were isolated from the methanolic extract of the fruits of Torilis japonica together with a known compound, torilin (1). Their structures were established as 11-acetoxy-8-isobutyryl-4-guaien-3-one (2), 11-acetoxy-8-methacrylyl-4-guaien-3-one (3), and 11-acetoxy-8-propionyl-4-guaien-3-one (4) by spectroscopic methods. These compounds inhibited lipopolysaccharide (LPS)-induced nitric oxide production in murine macrophages RAW 264.7 cells.View full abstractDownload PDF (61K) -
Avula Balakrishna, Mudamala Veera Narayana Reddy, Sandip Kumar Nayak, ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1486-1489
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESS4-Amino-5-phenyl-4H-1,2,4-triazole-3-thiol (1) underwent facile condensation with various phosphorus dichlorides (2a—j) in the presence of triethylamine in dry tetrahydrofuran at 60—65 °C and afforded corresponding thiadiazaphosphol-2-ones (3a—j). Their chemical structures were characterized using IR, 1H-, 13C-, 31P-NMR and Mass spectral studies. All the title compounds were screened for antioxidant properties by radical scavenging methods such as 1,1-diphenyl-2-picryl hydrazyl (DPPH), hydroxyl and lipid peroxidation. They exhibited potent in vitro antioxidant activity dose dependently. Their bioassay showed them to possess significant antibacterial activity.View full abstractDownload PDF (152K) -
Takashi Misawa, Hiroshi Aoyama, Taniyuki Furuyama, Kosuke Dodo, Morihi ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1490-1495
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSBenzhydrol-type analogs of 1′-acetoxychavicol acetate (ACA) were developed as inhibitors of human leukemia HL-60 cell growth based on quantitative structure–activity relationship (QSAR) analysis. An analog containing an anthracenyl moiety (8) was a potent inhibitor with the IC50 value of 0.12 μM.View full abstractDownload PDF (228K) -
Hui Xu, Ling-Ling FanArticle type: Notes
2008 Volume 56 Issue 10 Pages 1496-1498
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSA series of dibenzofurans were efficiently and conveniently synthesized via one-pot consecutive C(sp2)–O bond formation reaction (SNAr) in the presence of anhydrous K2CO3, followed by C(sp2)–C(sp2) bond formation reaction (intramolecular palladium-catalyzed aryl–aryl coupling reaction) between aryl halides and ortho-bromophenols. The desired dibenzofurans were obtained in 32—99% isolated yields.View full abstractDownload PDF (105K) -
Masateru Ono, Yuki Shiono, Yoshihiro Yanai, Yukio Fujiwara, Tsuyoshi I ...Article type: Notes
2008 Volume 56 Issue 10 Pages 1499-1501
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSA new steroidal glycoside and a new phenyl glycoside have been isolated from a ripe cherry tomato [Lycopersicon esculentum var. cerasiforme (DUNAL) ALEF., Solanaceae] along with two known steroidal alkaloid glycosides, esculeoisides A and B, and five aromatic compounds, zizibeoside I, benzyl alcohol β-gentiobioside, rutin, methyl caffeate, and phenylalanine. Their chemical structures were determined on the basis of spectroscopic data as well as chemical evidence.View full abstractDownload PDF (135K)
Communicatins to the Editor
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Naoki Kakusawa, Jyoji KuritaArticle type: Communications to the Editor
2008 Volume 56 Issue 10 Pages 1502-1504
Published: October 01, 2008
Released on J-STAGE: October 01, 2008
JOURNAL FREE ACCESSThe rhodium-catalyzed reaction of Sb-aryl-1,5-azastibocines with α,β-unsaturated ketones and esters is described. Exclusive formation of 1,4-conjugate adduct was achieved in aqueous NMP (N-methyl-2-pyrrolidinone) in the presence of 5 mol% of [RhCl(cod)]2, and no formation of Heck adduct was observed in this condition. Reactions with various enones and enoates were also demonstrated to prove generality of the 1,4-conjugate addition.View full abstractDownload PDF (110K)
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