Increase in aminobutyrate aminotransferase and cholineacetyltransferase in cerebrum of aged rats.

abstract：:To develop non-prodrugs of taxoids with satisfactory stability in vivo, high water-solubility, and potent antitumor activity, we prepared several 10-O-sec-aminoethyl docetaxel analogs (3) and evaluated their cytotoxicity against mouse leukemia and human tumor cell lines, microtubule disassembly-inhibitory activity, an...

journal_title：Chemical & pharmaceutical bulletin

authors： Uoto K,Takenoshita H,Yoshino T,Hirota Y,Ando S,Mitsui I,Terasawa H,Soga T

更新日期：1998-05-01 00:00:00

abstract：:A new series of 11-substituted 6,11-dihydrodibenz[b,e]oxepin derivatives was synthesized and evaluated for antiallergic activity. Convenient methods for the preparation of sulfides from alcohols were developed. Structure-activity relationships are described. Compound 7, 11-[2-(dimethylamin)ethyl]thio-6,11-dihydrodiben...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohshima E,Kumazawa T,Takizawa H,Harakawa H,Sato H,Obase H,Oiji Y,Ishii A,Ishii H,Ohmori K

更新日期：1991-10-01 00:00:00

abstract：:An efficient synthesis of the antiviral and antioxidative chromene (1) was achieved. A small amount of chromene 1 could be derived from plastoquinones 2 and 3, the major constituents of the brown alga, Sargassum micracanthum. By the following synthetic scheme involving its application, many kinds of analogs can be syn...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori J,Iwashima M,Takeuchi M,Saito H

更新日期：2006-03-01 00:00:00

abstract：:Electron spin resonance studies showed that addition of rat liver microsomes to the reaction system of alloxan with reduced nicotinamide adenine dinucleotide phosphate (NADPH) resulted in a marked increase in the generation of alloxan radicals (AH.), whereas heat-denatured microsomes were without such effect. Oxidatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai K,Haga K,Ogiso T

更新日期：1992-02-01 00:00:00

abstract：:Poorly water-soluble drugs N-5159, griseofulvin (GFV), glibenclamide (GBM) and nifedipine (NFP) were ground in a dry process with polyvinylpyrrolidone (PVP) and sodium dodecyl sulfate (SDS). Different crystallinity behavior of each drug during grinding was shown in the ternary Drug/PVP/SDS system. However, when each t...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh K,Pongpeerapat A,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2003-02-01 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：: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

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

更新日期：1995-11-01 00:00:00

abstract：:In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) value...

journal_title：Chemical & pharmaceutical bulletin

authors： Pinna GA,Loriga G,Murineddu G,Grella G,Mura M,Vargiu L,Murgioni C,La Colla P

更新日期：2001-11-01 00:00:00

abstract：:To understand more fully the effect of polyunsaturated fatty acids (PUFAs) on lipid bilayers, we investigated the effects of treatment with fatty acids on the properties of a model membrane. Three kinds of liposomes comprising dipalmitoylphosphatidylcholine (DPPC), dioleylphosphatidylcholine (DOPC), and cholesterol (C...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Hagiwara C,Sugibayashi K,Takayama K

更新日期：2008-08-01 00:00:00

abstract：:A catalytic amount of tin(IV) chloride catalyzed formal [4+2] cycloaddition reaction of di-tert-butyl 2-ethoxycyclobutane-1,1-carboxylate with ketones or aldehydes to give diethyl 6-ethoxydihydro-2H-pyran-3,3(4H)-dicarboxylates, whereas two equivalents of trimethylsilyl triflate promoted tandem [4+2] cycloaddition and...

journal_title：Chemical & pharmaceutical bulletin

authors： Okado R,Nowaki A,Matsuo J,Ishibashi H

更新日期：2012-01-01 00:00:00

abstract：:The oxalate salts and free bases of fentanyl and N-[1-(2-phenylethyl)-4-piperidyl]-N-(1-phenyl-4-pyrazolyl)propanamide, a new lead compound for long-acting analgesia, have been characterized by (1)H- and (13)C-NMR spectroscopy. The crystal structure of the hydrochloride of N-[1-(2-phenylethyl)-4-piperidyl]-N-(1-phenyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Jimeno ML,Alkorta I,Cano C,Jagerovic N,Goya P,Elguero J,Foces-Foces C

更新日期：2003-08-01 00:00:00

abstract：:We investigated the distribution and stability of pirarubicin in human blood obtained from 12 healthy volunteers. The distribution of pirarubicin into blood cells showed marked temperature- and concentration-dependencies and the Arrhenius plot for pirarubicin uptake in blood was biphasic. Therefore, pirarubicin appear...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagasawa K,Kitada N,Tsuji C,Ogawa M,Yokoyama T,Ohnishi N,Iwakawa S,Okumura K

更新日期：1992-10-01 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：:Four new bromotyrosine alkaloids, tyrokeradines C-F (1-4), have been isolated from Okinawan marine sponges of the order Verongidae. The structures of 1-4 were elucidated on the basis of spectroscopic data. Tyrokeradines C (1) and D (2) are new bromotyrosine alkaloids possesing an imidazole ring, while tyrokeradines E ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota T,Watase S,Mukai H,Fromont J,Kobayashi J

更新日期：2012-01-01 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：:Enantiomerically pure (1S,3S)- and (1S,3R)-1-amino-3-(hydroxymethyl)cyclopentanes have been efficiently synthesized from L-aspartic acid. The title compounds are isosteres of ribose and may be used to construct nucleoside analogs with important antiviral and antineoplastic activities as demonstrated by a concise total...

journal_title：Chemical & pharmaceutical bulletin

authors： Rapoport H,Chen Y,Mohareb RM,Ahn JH,Sim TB,Ho JZ

更新日期：2003-10-01 00:00:00

abstract：:A series of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5HT3) receptor antagonistic activities by means of assays of 5-HT3 receptor binding and the ability to antagonize the von Bezold-Jarisch reflex in rats. Replacement of the 1,4-benzoxazine ring with a 1,4...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroita T,Marubayashi N,Sano M,Kanzaki K,Inaba K,Kawakita T

更新日期：1996-11-01 00:00:00

abstract：:Three new quinovic acid glycosides, named gongganosides A (1), B (2), and C (3), were isolated from the bark of Bhesa paniculata (Celastraceae), an Indonesian medicinal plant collected in Sumatra Island. The chemical structures have been elucidated on the basis of chemical and physicochemical evidence as quinovic acid...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohashi K,Kojima H,Tanikawa T,Okumura Y,Kawazoe K,Tatara N,Shibuya H,Kitagawa I

更新日期：1994-08-01 00:00:00

abstract：:Toxicarioside D (1), a new cardenolide, along with 10 other known ones, was isolated from the stem of Antiaris toxicaria LESCH. by bioassay-guided fractionation. Their structures were determined on the basis of spectroscopic analysis. All the reported compounds effectively inhibited the growth of various cancer cell l...

journal_title：Chemical & pharmaceutical bulletin

authors： Jiang MM,Dai Y,Gao H,Zhang X,Wang GH,He JY,Hu QY,Zeng JZ,Zhang XK,Yao XS

更新日期：2008-07-01 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：:Various novel methotrexate (MTX) derivatives bearing an indoline moiety were synthesized and tested for biological activities using human peripheral blood mononuclear cell (hPBMC) and human synovial cells (hSC) derived from patients with rheumatoid arthritis (RA). Compounds having potent activity in vitro were further...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuoka H,Kato N,Tsuji K,Maruyama N,Suzuki H,Mihara M,Takeda Y,Yano K

更新日期：1996-07-01 00:00:00

abstract：:In this study, the interactions of different groups substituted isoeuxanthone derivatives with calf thymus DNA (ct DNA) were investigated by spectrophotometric methods and viscosity measurements. Results indicated that the xanthone derivatives could intercalate into the DNA base pairs by the plane of xanthone ring and...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang HF,Yan H,Gao X,Niu B,Guo R,Wei L,Xu B,Tang N

更新日期：2014-01-01 00:00:00

abstract：:The binding of carprofen (CP) to human serum albumin (HSA) and bovine serum albumin (BSA) was compared using equilibrium dialysis method. The affinity of CP for the primary binding site was BSA > HSA. However, the number of primary binding sites (n1) was 1.94 on HSA, considerably greater than that on BSA (0.79). The d...

journal_title：Chemical & pharmaceutical bulletin

authors： Kohita H,Matsushita Y,Moriguchi I

更新日期：1994-04-01 00:00:00

abstract：:A 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-16alpha-hydroxytrametenolic acid (3), polyporenic acid C (4), 3-epi-dehydropachymic acid (5), 3-epi-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou L,Zhang Y,Gapter LA,Ling H,Agarwal R,Ng KY

更新日期：2008-10-01 00:00:00

abstract：:A series of dibenzofurans were efficiently and conveniently synthesized via one-pot consecutive C(sp(2))-O bond formation reaction (SNAr) in the presence of anhydrous K(2)CO(3), followed by C(sp(2))-C(sp(2)) bond formation reaction (intramolecular palladium-catalyzed aryl-aryl coupling reaction) between aryl halides a...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu H,Fan LL

更新日期：2008-10-01 00:00:00

abstract：:Biological activity of thioaurones was not tested so far and the group constitute completely unexplored source of new molecules of pharmacological interest. We report synthesis and evaluation of cytotoxic activity of thioaurone derivatives bearing p-hydroquinone system in ring A. Their activity was found to depend str...

journal_title：Chemical & pharmaceutical bulletin

authors： Konieczny MT,Konieczny W,Okabe S,Tsujimoto H,Suda Y,Wierzba K

更新日期：2006-03-01 00:00:00

abstract：:ZCVI₄-2 is a newly developed furoxan-based nitric oxide-releasing derivative of oleanolic acid. It exhibited strong cytotoxicity against human hepatocellular carcinoma (HCC) in vitro and significantly inhibited the growth of HCC tumors in vivo. However, its low aqueous solubility and toxicity due to the fast release o...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang J,Gao Y,Su F,Gong Z,Zhang Y

更新日期：2011-01-01 00:00:00

abstract：:N-1 and N-2 substituted pyrazolo[4,5-g]pyrido[1,2-a]benzimidazoles were prepared regioselectively, and cytotoxicities evaluated in vitro against K562 and HL60 cells. All compounds displayed weaker activity than doxorubicin against sensitive lines, but showed the same activity against resistant cell lines (multidrug re...

journal_title：Chemical & pharmaceutical bulletin

authors： Dupuy M,Pinguet F,Blache Y,Chavignon O,Teulade JC,Chapat JP

更新日期：1998-11-01 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：:Different green synthesis of alkyl esters of acyclovir (acyclovir prodrugs) is described. Hexanoic, decanoic, dodecanoic and tetradecanoic acyclovir esters were synthesized reacting acyclovir and the respective acid anhydride in dimethyl sulfoxide (DMSO), in solvents from renewable sources and without solvent (T=30 °C...

journal_title：Chemical & pharmaceutical bulletin

authors： de Regil-Hernández R,Martínez-Lagos F,Rodríguez-Bayón A,Sinisterra JV

更新日期：2011-01-01 00:00:00