Synthesis of all-methylated isorugosin B.

abstract：:Regioselectivity in N-acetylation of nitro-0-phenylenediamine, a widely used hair dye component, by rat liver cytosolic N-acetyltransferases was studied in relation to its substituent effects on enzymatic N-acetylation of mono-substituted anilines. Nitro-p-phenylenediamine was acetylated specifically at the N4-positio...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakao M,Goto Y,Matsuki Y,Hiratsuka A,Watabe T

更新日期：1990-09-01 00:00:00

abstract：:This study demonstrates the structure-activity relationship of Col-003, a potent collagen-heat-shock protein 47 (Hsp47) interaction inhibitor. Col-003 analogues were successfully synthesized by Pd(0)-catalyzed cross-coupling reactions of 5-bromosalicylaldehyde derivatives with alkyl-metal species, and the inhibitory a...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Saito M,Ito S,Ogawa K,Goshima N,Nagata K,Doi T

更新日期：2020-03-01 00:00:00

abstract：:Jellies for oral administration are dosage forms that contain water, as stipulated in the Japanese Pharmacopeia, and heat is generally applied to the jellies during the manufacturing process. Therefore, it is difficult to formulate drugs that may be affected adversely by water and/or heat. To solve this problem, we tr...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakino Y,Hishikawa Y,Onodera R,Tahara K,Takeuchi H

更新日期：2017-01-01 00:00:00

abstract：:Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we ...

journal_title：Chemical & pharmaceutical bulletin

authors： Dohi M,Momose W,Yamashita K,Hakomori T,Sato S,Noguchi S,Terada K

更新日期：2017-02-01 00:00:00

abstract：:N-Terminal tripeptide analogs of fibrin alpha-chain were synthesized and their inhibitory effect on fibrinogen/thrombin clotting was examined. A new water-soluble active ester, 3-pyridinium ester, was used for the synthesis. Among the synthetic peptides, H-Gly-Pro-Arg-hexamethyleneimine exhibited the highest inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawasaki K,Tsuji T,Hirase K,Miyano M,Imoto Y,Iwamoto M

更新日期：1991-03-01 00:00:00

abstract：:As part of our search for a dual inhibitor possessing both thromboxane A2 (TXA2) receptor antagonistic and TXA2 synthase inhibitory activities, some [[(benzenesulfonamido)alkyl]phenyl]alkanoic acid derivatives possessing a pyridyl or imidazolyl group were synthesized. Their TXA2 receptor antagonistic and TXA2 synthase...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai S,Ogawa N,Suzuki T,Kato K,Ohashi T,Yasuda S,Kato H

更新日期：1996-08-01 00:00:00

abstract：:The superoxide O2(·-) scavenging reaction of (+)-catechin (Cat), quercetin (Que), rutin, and α-tocopherol (α-TOH) as natural phenolic compounds is investigated on the basis of electrochemical and ESR spectral measurements with the aid of density functional theory (DFT) calculations. Reversibility of the O2/O2(·-) redo...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakayama T,Uno B

更新日期：2015-01-01 00:00:00

abstract：:Three new 15,16-seco-cycloartane glycosides, which were constructed by a C-C bond cleavage in the D ring, have been isolated from Cimicifuga Rhizome for the first time. Their structures were determined by the use of 2D NMR techniques and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshimitsu H,Nishida M,Nohara T

更新日期：2007-05-01 00:00:00

abstract：:Six novel acyclic sulfides, named garlicnins L-1-L-4 (1-4), E (5), and F (6), were isolated from the acetone extracts, with the ability to suppress M2 macrophage activation, of the bulbs of garlic (Allium sativum L.), and their chemical structures were characterized. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nohara T,Fujiwara Y,Ikeda T,Yamaguchi K,Manabe H,Murakami K,Ono M,Nakano D,Kinjo J

更新日期：2014-01-01 00:00:00

abstract：:A series of carbamates of the phenolic compound 1 were prepared and evaluated in vivo as its prodrug. Each carbamate was orally administered to rats, and plasma concentrations of the parent compound 1 were measured with the passage of time. We judged which carbamate was suitable for the prodrug of 1 from both the AUC ...

journal_title：Chemical & pharmaceutical bulletin

authors： Igarashi Y,Yanagisawa E,Ohshima T,Takeda S,Aburada M,Miyamoto K

更新日期：2007-02-01 00:00:00

abstract：:A highly sensitive high-performance liquid chromatography with fluorescence detection for the determination of arachidonic acid metabolites is described. The metabolites are converted into corresponding fluorescent derivatives by reaction with 3-bromomethyl-6,7-methylenedioxy-1-methyl-2(1H)-quinoxalinone in the presen...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Takehiro O,Ishida J,Nakamura M

更新日期：1989-10-01 00:00:00

abstract：:The asymmetric platinum complexes cis-Pt(LL')Cl2 (L = NH3, L' = CH3NH2, (CH3)2NH, C2H5NH2 and (C2H5)2NH and LL' = N,N-dimethylethylenediamine),--one of the NH3 groups of cis-Pt(NH3)2Cl2 was substituted by alkylamine--, were synthesized and their cytotoxic effects have been measured using L-1210 cells. The IC50 values ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirano T,Inagaki K,Fukai T,Alink M,Nakahara H,Kidani Y

更新日期：1990-10-01 00:00:00

abstract：:A series of novel disulfides containing 1,3,4-thiadiazole moiety were designed, synthesized, and the structures of all products were identified by spectral data (IR, NMR, and high resolution (HR)-MS). Their in vitro antiproliferative activities were evaluated using 2-(2-methoxy-4-nitro-phenyl)-3-(4-nitro-phenyl)-5-(2,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang S,Liu XJ,Tang R,Wang HX,Liu HY,Liu YM,Chen BQ

更新日期：2017-01-01 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 compound tentatively named TL-1 was isolated from Talaromyces luteus as a metabolite having monoamine oxidase (MAO) inhibitory potency. TL-1 showed mixed-type inhibition of MAO in mouse liver when kynuramine was used as a substrate, and the IC50 was 6.6 microM. The inhibition constants (Ki) for MAO-A and -B in mou...

journal_title：Chemical & pharmaceutical bulletin

authors： Satoh Y,Yamazaki M

更新日期：1989-01-01 00:00:00

abstract：:We investigated the distribution and fate of liposomes after their intravenous injection into a mouse. Liposomes were composed of dimyristoylphosphatidylcholine, cholesterol and dicetylphosphate (7:2:1, molar ratio) with or without lactosylceramide. They were characterized as small unilamellar vesicles, approximately ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshioka S,Banno Y,Okano Y,Ohki K,Mizukami Y

更新日期：1992-04-01 00:00:00

abstract：:Asymmetric total synthesis of benzene analogues of galbonolide, a 14-membered antifungal macrolide, possessing a benzene ring instead of a conjugated diene structure, was achieved starting from chiral 1-aryl-1-propanol obtained by enzyme-catalyzed kinetic resolution with high enantioselectivity. Representatively, a me...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakoh H,Sakuraba S,Sugimoto Y,Imamura H,Jona H,Yamada K,Bamba-Nagano R,Hashizume T,Morishima H

更新日期：2004-01-01 00:00:00

abstract：:A new method has been developed for the umpolung α-heteroarylation of ketones via an N-alkoxyenamine. The treatment of ketones with tris(heteroaryl)aluminum reagents in the presence of isoxazolidine gave the corresponding α-heteroarylated ketones in moderate to good yields. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyoshi T,Takeda N,Fukami M,Sato S,Ueda M,Miyata O

更新日期：2014-01-01 00:00:00

abstract：:To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng XW,Huang N,Xu H,Yang WB,Yang LM,Qu H,Zheng YT

更新日期：2010-07-01 00:00:00

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

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

更新日期：1992-09-01 00:00:00

abstract：:Characteristics of the secondary structure of neocarzinostatin apoprotein (apo-NCS) were examined by various means. Gaussian analysis of the Fourier-transform infrared (FT-IR) curve and curve-fitting of the circular dichroism (CD) spectrum for apo-NCS revealed that this peptide was abundant in beta-structures. In the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Saito K,Sato Y,Edo K,Akiyama-Murai Y,Koide Y,Ishida N,Mizugaki M

更新日期：1989-11-01 00:00:00

abstract：:Gadolinium-diethylenetriaminepentaacetic acid (Gd-DTPA), a paramagnetic contrast agent for use in magnetic resonance imaging (MRI) was bound to stearylamine and incorporated into the liposomal membranes (Gd-DTPA liposomes). In addition, the Gd-DTPA liposomes were coated with mannan (cholesterol-aminoethylcarbamylmethy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kunimasa J,Inui K,Hori R,Kawamura Y,Endo K

更新日期：1992-09-01 00:00:00

abstract：:The intercalation reaction of diclofenac sodium (DFS) with layered inorganic compounds, gamma-titanium phosphate (gamma-TiP), proton type titanium oxide (H-TiO2) and sodium type synthetic mica (Na-TSM), was examined on. The direct reaction of DFS in ethanol-water mixed solvent resulted in the large amount accommodatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Tajima T,Suzuki N,Watanabe Y,Kanzaki Y

更新日期：2005-11-01 00:00:00

abstract：:The purpose of the present study was to quantify the degree of suppression of the bitterness of two amino acids (L-isoleucine (L-Ile), and L-phenylalanine (L-Phe)) which could be achieved by the addition of various test chemicals, and to examine the mechanism of this bitterness suppression. The test chemicals used wer...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawa T,Nakamura T,Tsuji E,Miyanaga Y,Nakagawa H,Hirabayashi H,Uchida T

更新日期：2004-02-01 00:00:00

abstract：:Further isolation work on the water-soluble fraction of a MeOH extract of Tricalysia dubia afforded one new megastigmane gentiobioside, named tricalysionoside A (1), and three sulfates, named sulfatricalysines A-C (2-4). Extensive isolation work on the 1-BuOH-soluble fraction of a MeOH extract of T. dubia yielded sulf...

journal_title：Chemical & pharmaceutical bulletin

authors： Shitamoto J,Sugimoto S,Matsunami K,Otsuka H,Shinzato T,Takeda Y

更新日期：2011-01-01 00:00:00

abstract：:The alpha,alpha-gem-difluorination of 2',4'-difluoro-alpha-(methylthio)acetophenone (1a) with N-fluoropyridinium salts gave 2',4',alpha,alpha-tetrafluoro-alpha-(methylthio)acetophenone (3a). This reaction was accelerated by the addition of zinc chloride, zinc bromide or anhydrous iron(III) chloride, and higher yields ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeda S,Kaneko Y,Eto H,Tokizawa M,Sato S,Yoshida K,Namiki S,Ogawa M

更新日期：2000-07-01 00:00:00

abstract：:The metabolites of clentiazem in the urine or bile of rats and dogs were investigated. Fifteen basic, 6 acidic, 2 neutral and 4 conjugated metabolites were isolated. In the present paper, fourteen reference compounds as shown in Charts 1, 2 and 3 were synthesized to identify the structures of the metabolites in proced...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue H,Nakamura S,Otsuka H,Gaino M,Harada T,Matsuki K,Takeda M

更新日期：1994-01-01 00:00:00

abstract：:Two new acylated flavonol glycosides, named amurenosides A and B, together with quercetin 3-(2,6-di-O-alpha-rhamnopyranosyl-beta-galactopyranoside), have been isolated from the whole plant of Vicia amurensis. Their structures were elucidated as quercetin 3-O-alpha-L-(3-feruloylrhamnopyranosyl)(1-->6)-[alpha-L-rhamnopy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kang SS,Chang YS,Kim JS

更新日期：2000-08-01 00:00:00

abstract：:Heparan sulfate proteoglycan was extracted from bovine lens capsules by 0.45 M NaCl/2 M urea and purified using ion-exchange chromatography and gel filtration. The proteoglycan was found to consist of protein and carbohydrate in a ratio of 75 to 25. The estimated average molecular weight of the heparan sulfate proteog...

journal_title：Chemical & pharmaceutical bulletin

authors： Onodera S

更新日期：1991-04-01 00:00:00

abstract：:In the course of our chemotaxonomic study of the liverworts growing in Madagascar, mastigophoric acid methyl ester, along with eleven known compounds were isolated from Mastigophora diclados. Isolated metabolites showed that the Malagasy Mastigophora is more related to the samples from Borneo and Japan than to the Tai...

journal_title：Chemical & pharmaceutical bulletin

authors： Harinantenaina L,Asakawa Y

更新日期：2004-11-01 00:00:00