Synthesis of biologically active acycloAZT derivatives and related compounds.


:The synthesis of optically active acyclic analogues of 3'-azido-3'-deoxythymidine, which lack only the 2'-CH2 of the sugar, is described. The synthesis of some nucleoside analogues that contain the N-acetyl-D-neuraminic acid moiety is also described.


Murata M,Achiwa K




Has Abstract


1990-03-01 00:00:00












  • Six new triterpenoidal glycosides including two new sapogenols from Albizziae Cortex. V.

    abstract::Six new triterpenoid glycosides called julibrosides A1-A4, B1 and C1 were isolated from Albizziae Cortex, the dried stem bark of Albizzia julibrissin Durazz. Their structures were determined based on spectral and chemical evidence. Julibrosides B1 and C1 had new sapogenols, designated julibrogenin B and C, respectivel...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kinjo J,Araki K,Fukui K,Higuchi H,Ikeda T,Nohara T,Ida Y,Takemoto N,Miyakoshi M,Shoji J

    更新日期:1992-12-01 00:00:00

  • Schisandrosides A-D, Dibenzocyclooctadiene Lignan Glucosides from the Roots of Schisandra chinensis.

    abstract::Four new dibenzocyclooctadiene lignan glucosides, schisandrosides A-D (1-4), as well as two known rare nortriterpenoids, micrandilactone C (5) and propindilactone Q (6), were isolated from the roots of Schisandra chinensis BAILLON (Schisandraceae). The structure of compounds 1-4 were elucidated by physical and spectro...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kim HM,Ryu B,Lee JS,Choi JH,Jang DS

    更新日期:2015-01-01 00:00:00

  • New oleanan-type triterpene and cincholic acid glycosides from Peruvian "Uña de Gato" (Uncaria tomentosa).

    abstract::A new oleanan-type triterpene and three new cincholic acid glycosides were isolated from Peruvian "Una de Gato" (Cat's claw, plant of origin: Uncaria tomentosa), a traditional herbal medicine in Peru. Their structures were determined by spectroscopic analysis. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kitajima M,Hashimoto K,Sandoval M,Aimi N,Takayama H

    更新日期:2004-10-01 00:00:00

  • Preparation and biological activity of 24-epi-26,26,26,27,27,27-hexafluoro- 1 alpha,25-dihydroxyvitamin D2.

    abstract::A new fluorinated analog of vitamin D2, 24-epi-26,26,26,27,27,27-hexafluoro- 1 alpha,25-dihydroxyvitamin D2, was efficiently synthesized starting from (R)-4-isopropyl-3-propionyl-2- oxazolidinone with high stereochemical control. In all four physiological test systems, the fluorinate vitamin D2 analog was found to be ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Iseki K,Oishi S,Namba H,Taguchi T,Kobayashi Y

    更新日期:1995-11-01 00:00:00

  • The new method for introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one and its application to chiral Wieland-Miescher type compound synthesis.

    abstract::The stereoselective introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one was accomplished using Birch reduction and an enolate trapping reaction. It was determined that the allyl group was introduced via an unexpected conformation-flipped from the initi...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Hiroya K,Takahashi T,Shimomae K,Sakamoto T

    更新日期:2005-02-01 00:00:00

  • Synthetic studies of the lichen macrolide lepranthin. Stereoselective synthesis of the diolide framework based on regioselective epoxide-opening reactions.

    abstract::Stereoselective synthesis of the 16-membered diolide 27, a fully functionalized congener of lepranthin (1), is described. The requisite five asymmetric carbon centers in monomer 23 were constructed in a highly stereoselective manner by using different epoxide-opening reactions of α,β-unsaturated γ,δ-epoxy esters and e...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Takada H,Nagumo S,Yasui E,Mizukami M,Miyashita M

    更新日期:2011-01-01 00:00:00

  • Synthesis and evaluation of 2-Nonylaminopyridine derivatives as PPAR ligands.

    abstract::To find novel PPAR ligands, we prepared several 3-{3 or 4-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}propanoic acid derivatives which were designed based on the structure of our previous PPARgamma ligand 1. In PPAR binding affinity assays, compound 4, which had an ethoxy group at the C-2 position of the propanoic acid o...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Usui S,Fujieda H,Suzuki T,Yoshida N,Nakagawa H,Ogura M,Makishima M,Miyata N

    更新日期:2007-07-01 00:00:00

  • Synthesis and affinities for dopamine (D2) and 5-hydroxytryptamine (5-HT2A) receptors of 1-(benzoylpropyl)-4-(1-oxocycloalkyl-2-ethyl)-piperazines as cyclic butyrophenone derivatives.

    abstract::Starting from benzo- or thienocycloalkaneacetic acids, we have prepared a series of 1-(3-p-fluorobenzoylpropyl)-4-(1-oxo-benzo- or thienocycloalkyl-2-ethyl)piperazines 8a-e containing both semirigid and linear butyrophenones pharmacophores. The affinities of these compounds for dopamine (D2) and 5-hydroxytryptamine (5...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Raviña E,Fueyo J,Masaguer CF,Negreira J,Cid J,Loza I,Honrubia A,Tristán H,G-Ferreiro T,Fontenla JA,Rosa E,Calleja JM,De Ceballos ML

    更新日期:1996-03-01 00:00:00

  • Benzylidene 2-aminoimidazolones derivatives: synthesis and in vitro evaluation of anti-tumor carcinoma activity.

    abstract::A series of benzylidene 2-aminoimidazolones derivatives were synthesized. Most compounds displayed strong inhibitory activity on the proliferation of human HepG2 cells in vitro. The active compounds were further evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against five human ca...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ling Y,Wang ZQ,Xiao YA,Zhu C,Shen L,Wang XM,Hui Y,Wang XY

    更新日期:2013-01-01 00:00:00

  • MRI Monitoring of the Mixed State of Admixtures Consisting of Moisturizing Cream and Steroid Ointment during the Mixing Process by a Revolution/Rotation-Type Hybrid Mixer.

    abstract::The admixture of a steroid ointment and a moisturizing cream is frequently prescribed to patients suffering from atopic dermatitis. For the mixing operation, a revolution/rotation-type hybrid mixer is widely used in pharmacy. The purpose of this study was to monitor the mixed state of the admixtures during the mixing ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yokokawa M,Setoyama H,Okada K,Hayashi Y,Machida Y,Onuki Y,Obata Y

    更新日期:2018-01-01 00:00:00

  • First total syntheses of (+/-)-isopiline, (+/-)-preocoteine, (+/-)-oureguattidine and (+/-)-3-methoxynordomesticine and the biological activities of (+/-)-3-methoxynordomesticine.

    abstract::A convenient and economical synthesis of 4-hydroxy-2,3-dimethoxybenzaldehyde has been developed. This was used as the starting material for the first total syntheses of (+/-)-isopiline, (+/-)-preocoteine, (+/-)-oureguattidine and (+/-)-3-methoxynordomesticine in which the key step involved formation of ring C of the a...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Nimgirawath S,Udomputtimekakul P,Taechowisan T,Wanbanjob A,Shen Y

    更新日期:2009-04-01 00:00:00

  • Improvement of dissolution properties of a new Helicobacter pylori eradicating agent (TG44) by inclusion complexation with beta-cyclodextrin.

    abstract::The interaction of a newly developed Helicobacter pylori eradicating agent (TG44, 4-methylbenzyl-4'-[trans-4-(guanidinomethyl)cyclohexylcarbonyloxy]biphenyl-4-carboxlylate monohydrochloride) with beta-cyclodextrin (beta-CyD) in aqueous solution and in solid state was studied to gain insight into the high in-vivo H. py...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Anzai K,Mizoguchi J,Yanagi T,Hirayama F,Arima H,Uekama K

    更新日期:2007-10-01 00:00:00

  • Six new presenegenin glycosides, reiniosides A--F, from Polygala reinii root.

    abstract::Six new oleanane-type triterpene saponins, called reiniosides A-F, were isolated from the roots of Polygala reinii Fr. et Sav. and their structures were elucidated by spectroscopic and chemical means. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Miyase T,Saitoh H,Shiokawa K,Ueno A

    更新日期:1995-03-01 00:00:00

  • Novel hypotensive peptides from the body of Elaphe climacophora.

    abstract::Four hypotensive peptides called elapherine-A, -B, -C and -D were isolated from the body of Elaphe climacophora after removal of the internal organs. Elapherine-A, which had the lowest molecular weight, exhibited a prolonged fall for 5 min in the blood pressure of spontaneously hypertensive rats, whereas elapherin-B, ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tsujibo H,Sato H,Taniguchi T,Kamatani Y,Kenny PT,Nomoto K,Inamori Y

    更新日期:1990-04-01 00:00:00

  • Synthesis and anticancer evaluation of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles, 1,2,4-triazoles and Mannich bases.

    abstract::A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted-1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Megally Abdo NY,Kamel MM

    更新日期:2015-01-01 00:00:00

  • Intermediate state during the crystal transition in aspartame, studied with thermal analysis, solid-state NMR, and molecular dynamics simulation.

    abstract::Aspartame (L-alpha-aspartyl-L-phenylalanine methyl ester) is a dipeptide sweetener about 200 times as sweet as sugar. It exists in crystal forms such as IA, IB, IIA, and IIB, which differ in crystal structure and in the degree of hydration. Among these, IIA is the most stable crystal form, and its crystal structure ha...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ebisawa K,Nagashima N,Fukuhara K,Kumon S,Kishimoto S,Suzuki E,Yoneda S,Umeyama H

    更新日期:2000-05-01 00:00:00

  • Synthesis and structure-activity relationships of thienylcyanoguanidine derivatives as potassium channel openers.

    abstract::In our series of studies on potassium channel openers, several thienylcyanoguanidine derivatives were synthesized and evaluated for smooth muscle relaxation activity in vitro. Among the newly synthesized compounds, N-cyano-N'-(5-cyano-3-thienyl)-N"-tert-pentylguanidine (4b) and N-(5-bromo-3-thienyl)-N'-cyano-N"-tert-p...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yoshiizumi K,Ikeda S,Nishimura N,Yoshino K

    更新日期:1997-12-01 00:00:00

  • Analysis of the phase solubility diagram of a phenacetin/competitor/beta-cyclodextrin ternary system, involving competitive inclusion complexation.

    abstract::The competitive inclusion complexations in the ternary phenacetin/competitors/beta-cyclodextrin (beta-CyD) systems were investigated by the solubility method, where m-bromobenzoic acid (m-BBA) and o-toluic acid (o-TA) were used as competitors. The solubility changes of the drug and competitors as a function of beta-Cy...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ono N,Hirayama F,Arima H,Uekama K

    更新日期:2001-01-01 00:00:00

  • Lembehsterols A and B, novel sulfated sterols inhibiting thymidine phosphorylase, from the marine sponge Petrosia strongylata.

    abstract::Lembehsterols A (1) and B (2), two novel sulfated sterols, were isolated from the marine sponge Petrosia strongylata. Both sterols showed inhibitory activity against thymidine phosphorylase, which is an enzyme related to angiogenesis in solid tumors. The structures of these sulfated sterols were established on the bas...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Aoki S,Naka Y,Itoh T,Furukawa T,Rachmat R,Akiyama S,Kobayashi M

    更新日期:2002-06-01 00:00:00

  • Megistoquinones I and II, two quinoline alkaloids with antibacterial activity from the bark of Sarcomelicope megistophylla.

    abstract::Two alkaloids, megistoquinone I (1) and megistoquinone II (2), were isolated from the bark of Sarcomelicope megistophylla. Their structures have been elucidated on the basis of MS and NMR data. Both belong to quinoline alkaloid series and should be considered as oxidation products of a furo[2,3-b]quinoline precursor. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Fokialakis N,Magiatis P,Chinou I,Mitaku S,Tillequin F

    更新日期:2002-03-01 00:00:00

  • Protection of a new heptapeptide from Carapax trionycis against carbon tetrachloride-induced acute liver injury in mice.

    abstract::A new heptapeptide GAGPHGG (OC1) was isolated from Carapax trionycis which was a traditional Chinese medicine (TCM) used for treatment of hepatic diseases. The structure of OC1 was characterized by MS, NMR techniques, together with amino acid sequence analysis. The hepatoprotective activity of OC1 was evaluated in viv...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Wang P,Zhang Y,An Y,Xu K,Xu X,Fu C,Lin J,Xu S,Li Q,Lei H

    更新日期:2013-01-01 00:00:00

  • Characterization of crystalline L-carnosine Zn(II) complex (Z-103), a novel anti-gastric ulcer agent: tautomeric change of imidazole moiety upon complexation.

    abstract::A novel crystalline Zn(II) complex of L-carnosine was prepared and evaluated for inhibitory activity against gastric ulceration in rats. The complex was found to be much more active than various other Zn(II) compounds. It was characterized by means of infrared (IR) spectroscopy, solid-state carbon-13 (13C) and nitroge...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Matsukura T,Takahashi T,Nishimura Y,Ohtani T,Sawada M,Shibata K

    更新日期:1990-11-01 00:00:00

  • A novel analytical method for pharmaceutical polymorphs by terahertz spectroscopy and the optimization of crystal form at the discovery stage.

    abstract::A novel analytical method for the determination of pharmaceutical polymorphs was developed using terahertz spectroscopy. It was found out that each polymorph of a substance showed a specific terahertz absorption spectrum. In particular, analysis of the second derivative spectrum was enormously beneficial in the discri...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ikeda Y,Ishihara Y,Moriwaki T,Kato E,Terada K

    更新日期:2010-01-01 00:00:00

  • Structure-activity relationship of bis-galloyl derivatives related to (-)-epigallocatechin gallate.

    abstract::Green tea and (-)-epigallocatechin gallate (EGCG: one of main components of green tea) are well known to have preventive activities against human cancers. Previously, using a galloyl group as a core structure derived from EGCG, we developed alkyl gallate and gallamide derivatives, which showed strong antiproliferative...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Dodo K,Minato T,Hashimoto Y

    更新日期:2009-02-01 00:00:00

  • Effect of metal ions on transcription of the ada gene which encodes O6-methylguanine-DNA methyltransferase of Escherichia coli.

    abstract::The effect of metal ions on transcription of the ada gene of Escherichia coli which is promoted by Ada protein in the presence of methylated deoxyribonucleic acid (DNA) was examined in a reconstituted system. Their effect on the O6-methylguanine-DNA methyltransferase (MGTase) activity of Ada protein was also examined....

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Takahashi K,Suzuki M,Sekiguchi M,Kawazoe Y

    更新日期:1992-09-01 00:00:00

  • Structures of toxic steroidal saponins from Narthecium asiaticum MAXIM.

    abstract::The full structures of the two steroidal saponins from Narthecium asiaticum MAXIM. We previously identified as toxic substances by monitoring the toxicity in guinea pigs were phytochemically reinvestigation on the aerial parts of the plant. The desired toxic saponins (6,7) were isolated together with two known lignan ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Inoue T,Mimaki Y,Sashida Y,Kobayashi M

    更新日期:1995-07-01 00:00:00

  • Effect of pore size of FSM-16 on the entrapment of flurbiprofen in mesoporous structures.

    abstract::The interaction between FSM-16 and flurbiprofen (FBP) in the mesopores of FSM-16 was investigated by using three types of FSM-16 with different pore diameters, i.e., FSM-16(Oc), FSM-16(Do) and FSM-16(Doc) (pore diameters 16.0, 21.6, 45.0 A, respectively). Solid dispersions of 30% FBP-70% FSM-16 were prepared by solven...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tozuka Y,Wongmekiat A,Kimura K,Moribe K,Yamamura S,Yamamoto K

    更新日期:2005-08-01 00:00:00

  • Evaluation of Weight Variation in Mini-Tablets Manufactured by a Multiple-Tip Tool.

    abstract::Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kurashima H,Uchida S,Kashiwagura Y,Tanaka S,Namiki N

    更新日期:2020-01-01 00:00:00

  • Oplopanphesides A-C, three new phenolic glycosides from the root barks of Oplopanax horridus.

    abstract::Three new phenolic glycosides, named oplopanphesides A-C (1-3), have been isolated from the root barks of Oplopanax horridus. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR techniques. These phenolic glycosides possess a novel feature in their sugar moieties that ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Huang WH,Zhang QW,Meng LZ,Yuan CS,Wang CZ,Li SP

    更新日期:2011-01-01 00:00:00

  • Tannins and related polyphenols of euphorbiaceous plants. XI. Three new hydrolyzable tannins and a polyphenol glucoside from Euphorbia humifusa.

    abstract::Three new hydrolyzable tannins, euphormisins M1, M2, and M3, were isolated from Euphorbia humifusa WILLD., and respectively characterized as 1,3,6-tri-O-galloyl-4-O- brevifolincarboxyl-beta-D-glucose (19), an oxidative metabolite (23) of geraniin, and 1,3,6-tri-O-galloyl-alpha-D-glucose (18), by spectroscopic and chem...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yoshida T,Amakura Y,Liu YZ,Okuda T

    更新日期:1994-09-01 00:00:00