Amino acids and peptides. XLIV. Synthesis of stereoisomeric pentapeptides of thiol proteinase inhibitor.

abstract：:Four new cycloart-7-ene triterpenol arabinosides, bugbanosides C-F, were isolated from the underground parts of Cimicifuga simplex Wormsk. (Ranunculaceae). The structures were elucidated as 12beta-acetoxy-3beta,15alpha,-24R,25-tetrahydroxy-16,23-dione-cycloart-7-ene 3-O-alpha-arabinopyranoside, 12beta-acetoxy-24R,25-e...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusano A,Shibano M,Tsukamoto D,Kusano G

更新日期：2001-04-01 00:00:00

abstract：:An aniline derivative which corresponds to UV-5 in the preceding paper was isolated from the case L-tryptophan sample associated with eosinophilia-myalgia syndrome (EMS). By spectroscopic analyses, the structure was identified as 3-anilinoalanine. The compound was optically active, and the stereochemistry of alanine m...

journal_title：Chemical & pharmaceutical bulletin

authors： Goda Y,Suzuki J,Maitani T,Yoshihira K,Takeda M,Uchiyama M

更新日期：1992-08-01 00:00:00

abstract：:The abnormal aggregation of amyloid β-peptide (Aβ) is central to the pathogenesis of Alzheimer's disease, the major form of dementia. Aromatic π-π interactions have been suggested to play a crucial role in the aggregation of not only Aβ, but also other amyloidogenic proteins. In this study, each or all phenylalanine (...

journal_title：Chemical & pharmaceutical bulletin

authors： Genji M,Yano Y,Hoshino M,Matsuzaki K

更新日期：2017-01-01 00:00:00

abstract：:ZnAB has the combined structure of N,N-bis(2-pyridylmethyl)ethylenediamine as a specific chelater for Zn(2+) and 1,3,5,7-tetramethyl-8-phenyl-boron dipyrromethene as a fluorophore. Complexation of ZnAB with Zn(2+) produces a remarkable enhancement of fluorescence intensity. ZnAB has the advantages of less sensitivity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koutaka H,Kosuge J,Fukasaku N,Hirano T,Kikuchi K,Urano Y,Kojima H,Nagano T

更新日期：2004-06-01 00:00:00

abstract：:We designed a single unit type controlled release tablet containing nateglinide to decrease both postprandial blood glucose level (PBG) and fasting blood glucose level (FBG) in normal beagle dogs. The tablet contains 60 mg of nateglinide in an immediate release portion, and 90 mg of nateglinide in a controlled release...

journal_title：Chemical & pharmaceutical bulletin

authors： Makino C,Sakai H,Yabuki A

更新日期：2010-09-01 00:00:00

abstract：:The alkylation of 2-phenyl-4-quinolones was investigated and showed that the N-alkylation versus O-alkylation is highly dependent on whether C-5 is hydroxylated or not. N-Alkylation is favoured by the presence of a 5-hydroxyl group. The synthetic and the NMR structural studies are reported. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hadjeri M,Mariotte AM,Boumendjel A

更新日期：2001-10-01 00:00:00

abstract：:Lipid peroxidation of erythrocyte membrane was caused by phorbol myristate acetate (PMA)-stimulated polymorphonuclear leukocytes (PMN) in the presence of ferritin. PMN themselves were not peroxidized. A lag period was observed before the start of the peroxidation reaction. In contrast, ferritin iron was continuously r...

journal_title：Chemical & pharmaceutical bulletin

authors： Miura T,Ogiso T

更新日期：1991-06-01 00:00:00

abstract：:Improved synthesis of the trans-3,5-disubstituted pyrrolidin-3-ylthio side-chain of the novel carbapenem 1 was achieved via stereoselective reduction of the 1-aryl-1-butanone derivative 5 and successive intramolecular cyclization of the resulting chiral alcohol 6. The 1-aryl-1-butanone derivative 5 was obtained by a c...

journal_title：Chemical & pharmaceutical bulletin

authors： Hashihayata T,Sakoh H,Goto Y,Hirose M,Sakuraba S,Imamura H,Sugimoto Y,Yamada K,Morishima H

更新日期：2001-11-01 00:00:00

abstract：:To expand the sequence of double-stranded DNA (dsDNA) targets in a triplex formation, 2',4'-BNAs (2'-O,4'-C-methylene bridged nucleic acids) having imidazoles as a nucleobase were synthesized and incorporated into oligonucleotides. Triplex-forming ability of the modified oligonucleotides was evaluated by using melting...

journal_title：Chemical & pharmaceutical bulletin

authors： Hari Y,Obika S,Inohara H,Ikejiri M,Une D,Imanishi T

更新日期：2005-07-01 00:00:00

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

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

更新日期：1990-11-01 00:00:00

abstract：:Two new pyrrole oligoglycosides, plancipyrrosides A and B (1 and 2), were isolated from methanol extract of the Vietnamese starfish Acanthaster planci using various chromatographic procedures. Their structures were elucidated by spectroscopic methods including one and two dimensional (1D- and 2D)-NMR and Fourier trans...

journal_title：Chemical & pharmaceutical bulletin

authors： Vien LT,Hanh TT,Huong PT,Dang NH,Thanh NV,Lyakhova E,Cuong NX,Nam NH,Kiem PV,Kicha A,Minh CV

更新日期：2016-11-01 00:00:00

abstract：:Two new synthetic methods were established for the efficient synthesis of optically active cyclohexene antisepsis agent, ethyl (6R)-6-[N-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate [(R)-1: TAK-242)]. The first method involved recrystallization from methanol of the diastereomeric mixture (6RS,1'R)-7...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada M,Ichikawa T,Yamano T,Kikumoto F,Nishikimi Y,Tamura N,Kitazaki T

更新日期：2006-01-01 00:00:00

abstract：:Anti-tauro 1 beta-hydroxycholic acid antisera were prepared by immunizing rabbits with N-(1 beta,3 alpha, 7 alpha, 12 alpha-tetrahydroxy-5 beta-cholan-24-oyl)-2- aminopropionic acid-bovine serum albumin (BSA) conjugate. The antisera raised had high affinity (1.25-1.46 x 10(9) M-1) and specificity for conjugated 1 beta...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikegawa S,Murai T,Yoshimura T,Tohma M

更新日期：1992-07-01 00:00:00

abstract：:Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lo...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

更新日期：2016-01-01 00:00:00

abstract：:The copper ions in the imidazole-clusters of histidine-oligopeptide, His(His)nGly (n = 18) and N-acetyl-His(His)nGly(n = 8 and 18), showed the d-d transition bands at 520 nm and 630 nm and oxidase-like activities. Those with the d-d bands at 480 nm and 550 nm did not have the activity. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda J,Hanaki A,Nakajima T

更新日期：1995-02-01 00:00:00

abstract：:Silicone has been utilized as a carrier material for sustained release system of lipophilic drugs. Extensive studies revealed that drug release rate is influenced by factors such as physicochemical properties of the drug and additives.(1-5)) When a lipophilic drug is highly potent at low concentrations, the drug relea...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajihara M,Sugie T,Sano A,Fujioka K,Urabe Y,Tanihara M,Imanishi Y

更新日期：2003-01-01 00:00:00

abstract：:4-(2-Pyridinylamino)-1,1,1-trifluoro-3-penten-2-ones 3, obtained from the reaction of commercially available 2-aminopyridine derivatives and 4-methoxy-1,1,1-trifluoro-3-penten-2-one 2, were converted to 6-(dimethylamino)-4-(2-pyridinylamino)-3,5-hexadien-2-ones 4 by treatment with dimethylformamide dimethyl acetal. Az...

journal_title：Chemical & pharmaceutical bulletin

authors： Cocco MT,Conglu C,Onnis V

更新日期：2001-06-01 00:00:00

abstract：:We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Hirono S

更新日期：2019-01-01 00:00:00

abstract：:The complexations of sulfasalazine (H3Suz) with some of transition metals have been investigated. Three types of complexes, [Mn(HSuz)-2(H2O)4] x 2H2O, [M(HSuz)-2(H2O)2] x xH2O (M=Hg(II), ZrO(II) and VO(II), x=4, 8 and 6, respectively) and [M(HSuz)-2(Cl)(H2O)3] x xH2O (M=Cr(III) and Y(III), x=5 and 6, respectively) wer...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Wahed MG,Refat MS,El-Megharbel SM

更新日期：2008-11-01 00:00:00

abstract：:Zanthoxylum schinifolium is an aromatic shrub, the pericarp and leaves of which are widely used in culinary applications in East Asian countries. In the present study, one new neolignan glycoside, zanthoxyloside A (1) together with 16 known glycosides (2-12) and alkaloids (13-17), were isolated from methanol extract o...

journal_title：Chemical & pharmaceutical bulletin

authors： Li W,Yang SY,Yan XT,Sun YN,Song SB,Kang HK,Kim YH

更新日期：2014-01-01 00:00:00

abstract：:Remote loading of insulin and bovine serum albumin (BSA) into neutral or positively-charged liposomes by incubation under a transmembrane pH gradient or non-pH gradient was investigated. Trapping efficiencies in several incubation conditions were compared with those of the conventional reverse-phase evaporation vesicl...

journal_title：Chemical & pharmaceutical bulletin

authors： Hwang SH,Maitani Y,Takayama K,Nagai T

更新日期：2000-03-01 00:00:00

abstract：:The 1-BuOH-soluble fraction of the methanol (MeOH) extract of Diospyros maritima was separated by chromatographic techniques to give three new oleanane-type and one new ursane-type triterpene glucoside, named ebenamariosides A-D (1-4); two megastigmanes were also isolated. The structures of triterpene glucosides was e...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawakami S,Miura E,Nobe A,Inagaki M,Nishimura M,Matsunami K,Otsuka H,Aramoto M

更新日期：2019-01-01 00:00:00

abstract：:The sequence Fourier analysis reported previously seems to be applicable to elucidating a simple and concerted interaction in Arabidopsis thaliana, similar to that in Homo sapiens. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Numao N,Miyama M,Hanagata N

更新日期：2004-08-01 00:00:00

abstract：:Thermodynamic studies were carried out to evaluate the binding of theophylline on adenosine deaminase (ADA) in 50 mM sodium phosphate buffer pH 7.5, at 300 K, using isothermal titration calorimetry (ITC). A simple method for determination of binding isotherm in the drug--ADA interaction was applied using ITC data. ADA...

journal_title：Chemical & pharmaceutical bulletin

authors： Saboury AA,Bagheri S,Ataie G,Amanlou M,Moosavi-Movahedi AA,Hakimelahi GH,Cristalli G,Namaki S

更新日期：2004-10-01 00:00:00

abstract：:The structures of the ternary palladium(II) complexes of the formulations [Pd(Gly)(bpy)](+)Cl(-).4H(2)O (Gly=glycine; bpy=2,2'-bipyridine) (1), [Pd(Gly)(phen)](+)Cl(-).4H(2)O (2) (phen=1,10-phenanthroline) and {[Pd(Gly)(bpa)](+)Cl(-)}(2).6H(2)O (3) (bpa=2,2'-bipyridylamine) were determined. All complexes are positivel...

journal_title：Chemical & pharmaceutical bulletin

authors： Yodoshi M,Okabe N

更新日期：2008-07-01 00:00:00

abstract：:From the bark of Cryptomeria japonica were isolated sugikurojins I (1) and J (2), and an abietane derivative (3) was obtained for the first time as a natural product. These structures were elucidated primarily through extensive NMR experiments. Sugikurojin I (1) has a unique skeleton incorporating an abietane diterpen...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa K,Suzuki K,Umeyama A,Arihara S

更新日期：2006-04-01 00:00:00

abstract：:Thirty-four extracts of crude drugs and medicinal plants have been screened for activity against Oncomelania nosophora, the intermediate host of the Japanese strain of Schistosoma japonicum. Strong molluscicidal activity was found in the MeOH extract of Anemarrhenae Rhizoma. Although timosaponin A-III, one of the main...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeda O,Tanaka S,Yamasaki K,Kohda H,Iwanaga Y,Tsuji M

更新日期：1989-04-01 00:00:00

abstract：:We describe here a Tf₂NH-catalyzed formal (3+3) cycloaddition of silyl enol ethers with acrylates as a new domino reaction. In the domino sequence, the catalyst activates Michael addition, deprotonation of the resulting silyloxonium cation and intramolecular Claisen condensation. It was found that reaction modes signi...

journal_title：Chemical & pharmaceutical bulletin

authors： Azuma T,Takemoto Y,Takasu K

更新日期：2011-01-01 00:00:00

abstract：:Enantioselective fluorinating agents, (R)- and (S)-,N-fluoro-3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (BNBT-F, 2) are readily prepared in 3 steps from racemic 3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (5) via optical resolution and fluorination. These agents m...

journal_title：Chemical & pharmaceutical bulletin

authors： Shibata N,Liu Z,Takeuchi Y

更新日期：2000-12-01 00:00:00

abstract：:When the beta-acyloxy esters (+/-)-10 and (+/-)-11 were exposed to the lipase OF-360 from Candida rugosa or immobilized lipase OF-360 in a water-saturated organic solvent, the hydrolyzed product (8aS)-6 was obtained in high chemical (40%) and optical (> 99% ee) yields. The absolute structure of (8aS)-6 was confirmed b...

journal_title：Chemical & pharmaceutical bulletin

authors： Akita H,Nozawa M,Futagami Y,Miyamoto M,Saotome C

更新日期：1997-05-01 00:00:00