Synthesis of macromolecular prodrugs of procaine, histamine and isoniazid.

abstract：:Novel hybrid L-ascorbic acid (vitamin C) derivatives with other biologically active substances, 5-hydroxy-2-hydroxymethyl-beta-pyrone (kojic acid) and alpha-tocopherol (vitamin E), linked at the C-2 or C-3 hydroxyl group were synthesized, and their thermal stability and inhibitory effects on tyrosinase activity, activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morisaki K,Ozaki S

更新日期：1996-09-01 00:00:00

abstract：:A series of novel N6,N6-dialkyl adenosine 3',5'-cyclic phosphates N6,N6-dialkyl cAMPs) was synthesized from 2'-O-p-toluenesulfonyl cAMP (2'-O-tosyl cAMP, 2) and tested for inotropic and chronotropic activities in vitro. Treatment of 2 with excess alkyl halides and sodium hydride followed by detosylation with aqueous N...

journal_title：Chemical & pharmaceutical bulletin

authors： Kataoka S,Yamaji N,Kato M,Kawada T,Imai S

更新日期：1990-11-01 00:00:00

abstract：:Six new furostanol saponins called trigoneosides Ia, Ib, IIa, IIb, IIIa, and IIIb were isolated from a medicinal foodstuff, fenugreek seed, the seed of Trigonella foenum-graecum L. (Leguminosae) originating from India, together with two known saponins, glycoside D and trigofoenoside A. The structures of trigoneosides ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Murakami T,Komatsu H,Murakami N,Yamahara J,Matsuda H

更新日期：1997-01-01 00:00:00

abstract：:Chitosan-alginate polyelectrolyte complex (PEC) have been prepared in situ in beads and microspheres. This study examines the preparation of suitable chitosan-alginate coacervates for casting into homogeneous PEC films for potential applications in packaging, controlled release systems and wound dressings. Coacervatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yan X,Khor E,Lim LY

更新日期：2000-07-01 00:00:00

abstract：:Two efficient and practical methods of synthesis of the C-10 substituent of DV-7751 (1), a novel quinolone carboxylic acid, were established. The first method utilizes an optical resolution of racemic 8-amino-6-benzyl-6-azaspiro[3.4]octane (13), while the second employs an enantioselective microbial reduction of 6-ben...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyadera A,Satoh K,Imura A

更新日期：2000-04-01 00:00:00

abstract：:The miscibility of a drug with excipients in solid dispersions is considered to be one of the most important factors for preparation of stable amorphous solid dispersions. The purpose of the present study was to elucidate the feasibility of (1)H-NMR spin-lattice relaxation measurements to assess the miscibility of a d...

journal_title：Chemical & pharmaceutical bulletin

authors： Aso Y,Yoshioka S,Miyazaki T,Kawanishi T,Tanaka K,Kitamura S,Takakura A,Hayashi T,Muranushi N

更新日期：2007-08-01 00:00:00

abstract：:Absorption spectra of polycrystalline L-, D-, and DL-tartaric acid have been measured by terahertz time domain spectroscopy (THz-TDS). Different absorption bands are observed for DL-tartaric acid and its enantiomers (L- and D-tartaric acid). This result shows that the THz-TDS can be used for distinguishing between DL-...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishikiori R,Yamaguchi M,Takano K,Enatsu T,Tani M,de Silva UC,Kawashita N,Takagi T,Morimoto S,Hangyo M,Kawase M

更新日期：2008-03-01 00:00:00

abstract：:Monoterpene glucosides, perillosides A and C, obtained from the leaves of Perilla frutescens, were found to be inhibitors of aldose reductase (EC 1.1.1.21) which is considered to be a key enzyme in diabetic complications such as cataract. The apparent type of inhibition of rat lens aldose reductase by perillosides A a...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujita T,Ohira K,Miyatake K,Nakano Y,Nakayama M

更新日期：1995-06-01 00:00:00

abstract：:The gamma subunit of enolase (gamma-enolase) was purified from the brain tissues of cow, dog, goat, pig, rabbit, and rat. The purification was achieved in only three steps: ammonium sulfate-precipitation, DE 53 cellulose ion-exchange chromatography, and polyacrylamide gel electrophoresis (PAGE) in a preparative mode. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoki T,Tanaka T,Watabe H

更新日期：1992-05-01 00:00:00

abstract：:The combination of electrolysis and the Fe(III)(PA)3/O2/CH3CN system was investigated for allylic hydroxylation of octahydronaphthalene derivatives. Substrates with a bridgehead double bond gave the allylic alcohol with alpha-preference, while non-bridgehead olefin did not react smoothly. This system is a useful tool ...

journal_title：Chemical & pharmaceutical bulletin

authors： Okamoto I,Funaki W,Nobuchika S,Sawamura M,Kotani E,Takeya T

更新日期：2005-02-01 00:00:00

abstract：:An effective procedure for decontamination of beta-lactam antibiotic residues or contaminants in the pharmaceutical manufacturing environment was investigated. Decontamination with solutions of hydrochloric acid, sodium hydroxide, hydrogen peroxide and hydroxylamine as agents for degradation was assessed. According to...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukutsu N,Kawasaki T,Saito K,Nakazawa H

更新日期：2006-09-01 00:00:00

abstract：:Six new cyclic peptides, gypsophin A-F (1-6), were isolated from Gypsophila oldhamiana. Their structures were elucidated by extensive NMR and chemical degradation. Compound 3 exhibited moderate activity of antiplatelet aggregation in vitro. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang G,Luo JG,Yang MH,Wang XB,Kong LY

更新日期：2013-01-01 00:00:00

abstract：:Allylamine (ALAM) film was plasma-polymerized on a flat glass (referred to as ALAM(GLA): GLA refers to a flat glass plate) for use as a solid phase in two-site immunoradiometric assay (two-site IRMA). Adsorption of F(ab')2 anti-human immunoglobulin G [formula: see text] to ALAM(GLA) was larger than adsorption on a pol...

journal_title：Chemical & pharmaceutical bulletin

authors： Muratsugu M,Kurosawa S,Mori Y,Kamo N

更新日期：1992-02-01 00:00:00

abstract：:An automated synthesis system using a solid-phase extraction (SPE) system and column packed with octadecylsilica (ODS), which was coated with phospholipid and loaded with dog liver microsomes, was developed for synthesis of glucuronides. Preparation of the microsome-immobilized SPE column, glucuronidation of drugs to ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kashima Y,Kitade T,Kashima Y,Okabayashi Y

更新日期：2010-03-01 00:00:00

abstract：:Diphenhydramine, a sedating antihistamine, is an agonist of human bitter taste receptor 14 (hTAS2R14). Diphenhydramine hydrochloride (DPH) was used as a model bitter medicine to evaluate whether the umami dipeptides (Glu-Glu and Asp-Asp) and their constituent amino acids (Glu, Asp) could suppress its bitterness intens...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuno T,Morimoto S,Nishikawa H,Haraguchi T,Kojima H,Tsujino H,Arisawa M,Yamashita T,Nishikawa J,Yoshida M,Habara M,Ikezaki H,Uchida T

更新日期：2020-01-01 00:00:00

abstract：:Two new naphthopyrones, cassiasides B2 (1) and C2 (2), were isolated from the seeds (Cassiae Semen) of Cassia obtusifolia L. The structures of the two new compounds 1 and 2 were established as rubrofusarin 6-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-glucopyranosyl-(1-->3)-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-gluc...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitanaka S,Nakayama T,Shibano T,Ohkoshi E,Takido M

更新日期：1998-10-01 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：:Bioassay-directed fractionation of the extract of the cyanobacterium P. tenue led to the isolation of the three classes of glycolipids, viz., monogalactosyl diacylglycerol (MGDG), digalactosyl diacylglycerol (DGDG), and sulfoquinovosyl diacylglycerol (SQDG) as anti-tumor-promoters. In comparing the anti-tumor-promotin...

journal_title：Chemical & pharmaceutical bulletin

authors： Shirahashi H,Murakami N,Watanabe M,Nagatsu A,Sakakibara J,Tokuda H,Nishino H,Iwashima A

更新日期：1993-09-01 00:00:00

abstract：:A highly polar saponin mixture from pods of Acacia concinna (Leguminosae) was hydrolyzed with alkali to yield five new triterpenoidal prosapogenols named concinnosides A (6), B (3), C (7), D (4), and E (8), together with four known glycosides, acaciaside, (2), julibroside A1 (10) julibroside A3 (9), albiziasaponin C (...

journal_title：Chemical & pharmaceutical bulletin

authors： Abul Gafur M,Obata T,Kiuchi F,Tsuda Y

更新日期：1997-04-01 00:00:00

abstract：:The oxidative behaviour of, a hypnotic drug, zolpidem was studied at glassy carbon electrode in Britton-Robinson buffer over the pH range 2.0-11.0 using cyclic, linear sweep and differential pulse voltammetry. Oxidation of the drug was effected in a single irreversible, diffusion-controlled step. Using differential pu...

journal_title：Chemical & pharmaceutical bulletin

authors： Radi AE,Bekhiet G,Wahdan T

更新日期：2004-09-01 00:00:00

abstract：:Scale-up of wet granulation in a vertical high shear mixer was conducted. Pharmaceutical excipient powders composed of lactose, cornstarch and micro-crystallinecellulose, and hydroxypropylcellulose as a binder were mixed together and then granulated with purified water under various operating conditions and vessel sca...

journal_title：Chemical & pharmaceutical bulletin

authors： Watano S,Okamoto T,Sato Y,Osako Y

更新日期：2005-04-01 00:00:00

abstract：:The phosphorylation of several D-glucose derivatives has been achieved using inorganic sodium cyclo-triphosphate hexahydrate (P3m), Na3P3O9 x 6H2O, in aqueous solution. In the phosphorylation of D-glucuronic acid, 6-phosphoryl-D-glucose and D-xylose, beta-D-glucuronic acid 1-triphosphate, 6-phosphoryl-beta-D-glucose 1...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue H,Watanabe M,Nakayama H,Tsuhako M

更新日期：2000-06-01 00:00:00

abstract：:The synthesis of acetomycin and related analogs was investigated. Acetomycin was synthesized from diethyl allyl(methyl)malonate in 6.5% yield over 18 steps. The total number of steps was improved compared to our previous synthesis; i.e., four steps shorter, and the total yield was 4.5% greater than the previous synthe...

journal_title：Chemical & pharmaceutical bulletin

authors： Uenishi J,Kobayashi N,Komine S,Okadai T,Yonemitsu O,Sasaki T,Yamada Y

更新日期：1999-04-01 00:00:00

abstract：:We have improved sample pre-treatment for the effective removal of polyphenols and simple analysis of caffeine in tea using a cartridge filled with polyvinylpolypyrroridone (PVPP). Nearly 100% of catechins were removed from the green tea sample and caffeine was completely recovered in the range of 98.2-101.3% by sampl...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamauchi Y,Nakamura A,Kitai M,Hatanaka K,Kohno I,Tanimoto T

更新日期：2007-09-01 00:00:00

abstract：:Alkylidenemalonates were readily dimerized in the presence of SmI2 to give 2,3-disubstituted 1,1,4,4-butanetetracarboxylates as mixtures of meso and racemic isomers in moderate to good yields. The structure of the less polar isomer of tetraethyl 2,3-diphenyl-1,1,4,4-butanetetracarboxylate was determined by X-ray cryst...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita M,Okuyama K,Kawasaki I,Nakamura S,Nagamine R,Tsujita T,Ohta S

更新日期：2000-11-01 00:00:00

abstract：:The regioselective intramolecular 1,3-dipolar cycloaddition of the phenylsulfonylallene-nitrone derivatives has been developed. This reaction showed that the distal double bond of the allene exclusively reacted with the nitrone group to produce the bicyclic isoxazolidine derivatives regardless of the substitution patt...

journal_title：Chemical & pharmaceutical bulletin

authors： Inagaki F,Kobayashi H,Mukai C

更新日期：2012-01-01 00:00:00

abstract：:Phytochemical investigation of the leaves of Umbilicus pendulinus afforded in addition to 2-O-caffeoyl malate, isoquercitrin and Z-venusol, the new isomer E-venusol. Special NMR experiments were carried out to elucidate the configuration of the two latter compounds. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Viornery L,Saliba C,Daskiewicz JB,Bayet C,Comte G,Fenet B,Gutierrez G,Barron D

更新日期：2000-11-01 00:00:00

abstract：:The reaction of the N-furfuryloxamic acid sodium salt (12) with 1,1'-oxalyldiimidazole (ODI) yielded the imidazolide (13) as an intermediate, and this directly reacted with 2-aminothiazole derivatives (14) or 2-aminobenzothiazole derivatives (15) under essentially neutral conditions to afford the N'-12-(substituted th...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa T,Tsutsui C

更新日期：2000-09-01 00:00:00

abstract：:We discuss here the effect of water-insoluble pharmaceutical aids on the nature of drug release from composite polymeric prodrugs synthesized by mechanochemical solid-state polymerization. Magnesium stearate (Mgst) and hydrogen castor oil (HCO) were used as water-insoluble pharmaceutical aids. Composite polymeric prod...

journal_title：Chemical & pharmaceutical bulletin

authors： Kondo S,Hosaka S,Sasai Y,Kuzuya M

更新日期：2004-11-01 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