Mechanochemical solid-state polymerization (XI): effect of water-insoluble pharmaceutical aids on drug release from mechanically synthesized polymeric prodrugs.

abstract：:The differences in biological activities among polychlorinated dibenzo-p-dioxins (dioxins) are strongly dependent on the substitution pattern of chlorine at various positions on the parent dibenzo-p-dioxin molecule. The absolute hardness, eta, of dioxins shows a good correlation with the potency of biological activity...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi S,Sameshima K,Ishii Y,Tanaka A

更新日期：1995-10-01 00:00:00

abstract：:The involvement of prostanoids in the improvement of adenine-induced renal failure in rats by magnesium lithospermate B was studied. After intraperitoneal administration of magnesium lithospermate B to renal failure rats, the levels of glomerular filtration rate, renal plasma flow and renal blood flow were increased. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokozawa T,Chung HY,Lee TW,Oura H,Tanaka T,Nonaka G,Nishioka I,Hirai A

更新日期：1989-06-01 00:00:00

abstract：:Analysis of the structural requirements of compound 1 (SR48968), a potent NK2 receptor antagonist, revealed that the 4-phenyl group of the piperidine is essential for binding with the NK2 receptor and occupies an equatorial position. Energy calculation of a variety of substituted 4-phenyl piperidines revealed that spi...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Fujii M,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The "in vitro" antibacterial activity of these compounds and their corresponding alpha-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobi...

journal_title：Chemical & pharmaceutical bulletin

authors： Rival Y,Grassy G,Michel G

更新日期：1992-05-01 00:00:00

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

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

更新日期：2010-01-01 00:00:00

abstract：:In addition to 19-dydroxybaccatin III, 1beta-hydroxy-5 alpha-deacetylbaccatin I, taxayuntin G and 13-O-deacetyltaxumairol Z (4), three new taxane diterpenoids, taxumairols X (1), Y (2), Z (3) have been isolated from extracts of the Formosan Taxus mairei (LEMEE & LEVL.) S. Y. HU. Compounds 1-2 belong to the 11(15-->1)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Shen YC,Chang YT,Wang SS,Lin YC,Chen CY

更新日期：2002-12-01 00:00:00

abstract：:We have developed a novel organometallic catalysis and applied it to drug discovery. Two new catalysts were found, ruthenium hydride with a nitrogen-containing heterocyclic carbene (A) and an organopalladium catalyst supported on a sulfur-terminated semiconductor, gallium arsenide (001) (B). Both catalysts are environ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arisawa M

更新日期：2007-08-01 00:00:00

abstract：:New triazine-type dehydrocondensing reagents, such as ROMP-Trz-Cl and ROMP(OH)-Trz-Cl, were synthesized by a ring opening metathesis polymerization (ROMP) method, and these showed higher loading than conventional polymer-supported condensing reagents. These polymers effect the formation of amides in good yields by add...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Kameyama S,Tani S,Kunishima M

更新日期：2007-05-01 00:00:00

abstract：:Peptides mimicking chemokine receptor CCR5 were synthesized and their anti-HIV-1 activities evaluated. Prepared compounds, especially a sulfated derivatives, showed significant anti-HIV-1 activities. Furthermore, a hybrid molecule linked to an N-carbomethoxycarbonyl-prolyl-phenylalanine (CPF) moiety had a greater effe...

journal_title：Chemical & pharmaceutical bulletin

authors： Konishi K,Ikeda K,Achiwa K,Hoshino H,Tanaka K

更新日期：2000-02-01 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：:A series of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6,7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishikawa H,Tabusa F,Miyamoto H,Kano M,Ueda H,Tamaoka H,Nakagawa K

更新日期：1989-08-01 00:00:00

abstract：:We recently proposed a new hydrogen-accepting parameter, S(HA), for monosubstituted (di)azines on the basis of the heat of formation calculated by the conductor-like screening model (COSMO) method. In this work, S(HA) values for monosubstituted thiophenes and furans were calculated and the results were applied to the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamagami C,Tachikawa H

更新日期：2003-10-01 00:00:00

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

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

abstract：:Five new components, named multiforisins A, B, C, D, and E, with immunosuppressive activity were isolated from an Ascomycete, Gelasinospora multiforis. Multiforisin A, the main immunosuppressive principle of this fungus, was deduced to be 5-formyl-3-(hydroxymethyl)-4-methoxy-6-(1E-propenyl)-alpha-pyrone. Multiforisins...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujimoto H,Satoh Y,Nakayama M,Takayama T,Yamazaki M

更新日期：1995-04-01 00:00:00

abstract：:A new phenolic glycoside, 3,4,5-trimethoxyphenol-1-(6-xylopyranosyl)glucopyranoside, was isolated together with twenty known compounds identified as koaburaside, 3,4,5-trimethoxyphenol, 5,7-dihydroxychromone-7-neohesperidoside, naringin, neoeriocitrin, p-coumaric acid, vanillin, vanillic acid, coniferyl aldehyde, feru...

journal_title：Chemical & pharmaceutical bulletin

authors： Kosuge K,Mitsunaga K,Koike K,Ohmoto T

更新日期：1994-08-01 00:00:00

abstract：:CX-659S (1) [(S)-6-amino-5-(6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxamido)-3-methyl-1-phenyl-2,4-(1H,3H)-pyrimidinedione], has been developed as a new type anti-inflammatory agent for the treatment of dermatitis. The structure of a major metabolite of CX-659S was determined as (S)-6-amino-5-[2-hydroxy-2-methyl-4-...

journal_title：Chemical & pharmaceutical bulletin

authors： Isobe Y,Tobe M,Takahashi O,Goto Y,Inoue Y,Obara F,Tsuchiya M,Hayashi H

更新日期：2002-10-01 00:00:00

abstract：:The hypoglycemic component, elatoside E, was isolated from the root cortex of Aralia elata SEEM. (Araliaceae) together with elatoside F and eight known oleanolic acid glycosides, elatosides A and C, oleanolic acid 3-O-[alpha-L-arabinofuranosyl (1-->4)]-beta-D-glucopyranosiduronic acid, oleanolic acid 3-O-beta-D-glucop...

journal_title：Chemical & pharmaceutical bulletin

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

更新日期：1996-10-01 00:00:00

abstract：:Tryptanthrin is an ancient medicine which recently was also found to have a function of downregulating multidrug resistance (MDR). However, tryptanthrin is insoluble in water, which limits its availability for delivery into cancer cells. There is a need to improve delivery systems to increase the inhibition of MDR. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Fang YP,Lin YK,Su YH,Fang JY

更新日期：2011-01-01 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：: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

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

更新日期：1997-12-01 00:00:00

abstract：:Prolyl endopeptidase (PEP, EC 3.4.21.26) is an enzyme playing a role in the metabolism of proline-containing neuropeptides which have been suggested to be involved in learning and memory processes. In screening for PEP inhibitors from fourteen traditional Kampo formulas, we found that Tokaku-joki-to shows a significan...

journal_title：Chemical & pharmaceutical bulletin

authors： Fan W,Tezuka Y,Kadota S

更新日期：2000-07-01 00:00:00

abstract：:The pharmacokinetic profiles of the hypoglycemic agent, acetohexamide (AH) and its major active metabolite, hydroxyhexamide (HH) were studied in three species of laboratory animals after intraperitoneal (ipl) administration in comparison with those after intravenous (iv) administration of AH and of the preformed metab...

journal_title：Chemical & pharmaceutical bulletin

authors： Asada S,Nagamine S,Nakae H

更新日期：1989-03-01 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：:The adsorption properties of As(III) and Cr(VI) by gibbsite (GB) calcined at 200 to 1150 degrees C was investigated on basis of their specific surface area, number of hydroxyl groups, surface pH and adsorption isotherms. The amount of As(III) and Cr(VI) adsorbed on the calcined GB at 300 or 400 degrees C was the highe...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogata F,Kawasaki N,Kabayama M,Kakehi K

更新日期：2009-02-01 00:00:00

abstract：:Rhodiola rosea L. (Golden Root) has been used for a long time as an adaptogen in Chinese traditional medicine and is reported to have many pharmacological properties. Along its known secondary metabolites tyrosol (1), salidroside (rhodioloside) (2), rosin (3), rosarin (4), rosavin (5), sachaliside 1 (6) and 4-methoxy-...

journal_title：Chemical & pharmaceutical bulletin

authors： Tolonen A,Pakonen M,Hohtola A,Jalonen J

更新日期：2003-04-01 00:00:00

abstract：:Five glycyrrhetinic acid (Ib) derivatives have been synthesized to try to improve the antioxidant activity. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA pr...

journal_title：Chemical & pharmaceutical bulletin

authors： Ablise M,Leininger-Muller B,Wong CD,Siest G,Loppinet V,Visvikis S

更新日期：2004-12-01 00:00:00

abstract：:Pyrrole-2,5-dicarboxylates were rapidly and selectively reduced to the corresponding mono-alcohol using 3 eq of diisobutylaluminum hydride at 0°C. Pyrrole-2,4-dicarboxylate showed the same reactivity; however, the selectivity decreased with pyrrole-3,4-dicarboxylate. When the nitrogen atom of the pyrrole-2,5-dicarboxy...

journal_title：Chemical & pharmaceutical bulletin

authors： Yasui E,Tsuda J,Ohnuki S,Nagumo S

更新日期：2016-01-01 00:00:00

abstract：:Biodegradable pasty-type copolyesters with a relatively low molecular weight of 4500 were synthesized by direct copolycondensation of epsilon-caprolactone (CL) and delta-valerolactone (VL) in the absence of catalysts to evaluate in vivo capabilities of the polymer for implantable controlled release devices in drug del...

journal_title：Chemical & pharmaceutical bulletin

authors： Imasaka K,Yoshida M,Fukuzaki H,Asano M,Kumakura M,Mashimo T,Yamanaka H,Nagai T

更新日期：1991-08-01 00:00:00

abstract：:Dryocrassyl formate, sitostanyl formate, and 12alpha-hydroxyfern-9(11)-ene were isolated from the fresh fronds of Cyathea podophylla. Their structures were elucidated by spectroscopic techniques and synthesis. Ten known triterpenoids, three derivatives of phytol, a stanol, and beta-tocopherol were also identified from...

journal_title：Chemical & pharmaceutical bulletin

authors： Arai Y,Hattori T,Hamaguchi N,Masuda K,Takano A,Shiojima K

更新日期：2003-11-01 00:00:00

abstract：:Hot aqueous extracts of 134 Chinese crude drugs were subjected to screening for inhibitory activity on K+ contracture of guinea pig taenia coli, and significant activity was observed in 17 crude drugs. Chemical investigations of two crude drugs, Kakko and Ubai, which originate from Pogostemon cablin and Prunus mume, r...

journal_title：Chemical & pharmaceutical bulletin

authors： Ichikawa K,Kinoshita T,Sankawa U

更新日期：1989-02-01 00:00:00