Percutaneous absorption of clonazepam in rabbit.

abstract：:Fourteen flavonol glycosides including two new compounds were isolated from the leaves of two Diospyros plants (D. cathayensis and D. rhombifolia). The structures of isolated compounds were determined by spectroscopic analysis. The scavenging activity of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical of the isolated com...

journal_title：Chemical & pharmaceutical bulletin

authors： Furusawa M,Tanaka T,Ito T,Nakaya K,Iliya I,Ohyama M,Iinuma M,Murata H,Inatomi Y,Inada A,Nakanishi T,Matsushita S,Kubota Y,Sawa R,Takahashi Y

更新日期：2005-05-01 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：:Epidermal cells from newborn rat skin were cultured on type IV collagen-coated Millipore filter, and the transport of low density lipoprotein (LDL) labeled with Rhodamine B isothiocyanate (RB-LDL) through the cultured cell layer was examined. The transport of RB-LDL was dependent on temperature and biological energy. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohkura K,Terada H

更新日期：1991-02-01 00:00:00

abstract：:Chemical reactivity descriptors and lipophilicyty (log P) were evaluated via semi-empirical method for the quantum calculation of molecular electronic structure (PM3) in order to clarify the structure-cytotoxic activity relationships of disubstutited thioureas. Analysed compounds were obtained by the linkage of 2-amin...

journal_title：Chemical & pharmaceutical bulletin

authors： Filipowska A,Filipowski W,Tkacz E,Nowicka G,Struga M

更新日期：2016-01-01 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：:Structural optimization of 2-aminonicotinamide derivatives as ghrelin receptor inverse agonists is reported. So as to avoid mechanism-based inactivation (MBI) of CYP3A4, 1,3-benzodioxol ring of the lead compound was modified. Improvement of the main activity and lipophilicity was achieved simultaneously, leading to co...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi B,Funami H,Shibata M,Maruoka H,Koyama M,Kanki S,Muto T

更新日期：2015-01-01 00:00:00

abstract：:From the Fresh leaves of Hovenia dulcis Thunb. var. tomentella Makino, five five new dammarane glycosides named hodulosides VI-X (1-5) were isolated. Their structures were determined on the basis of chemical and spectral evidence. Hodulosides VII-X showed antisweet activities. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa K,Nagai Y,Yoshida M,Arihara S

更新日期：1993-10-01 00:00:00

abstract：:To experimentally clarify a possible stereostructure-activity relationship proposed for H2-receptor antagonists, three 5-aminophenylimidazoles (1, 2 and 3), in which respective amino groups are located on the ortho, meta and para positions of the benzene ring, were synthesized and examined for their conformational cha...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida T,In Y,Inoue M,Kurihara T,Moriomoto K,Morisaka K,Shibata K

更新日期：1990-07-01 00:00:00

abstract：:Three new cardiac glycosides named cheiranthoside VIII (1), cheiranthoside IX (2) and cheiranthoside X (3) were isolated from the seeds of Erysimum cheiranthoides. Based on spectroscopic data, the structures of 1-3 were characterized as strophanthidin 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-antiaropyranoside, cheiran...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei ZH,Nakayama H,Kuniyasu A,Tai BS,Nohara T

更新日期：2002-06-01 00:00:00

abstract：:We have developed a new method to modify the C-4 position of 10-deacetylbaccatin III (5) using the C-4 acetoxy anion of the 13-keto derivative (7) and various alkyl halides. The method developed herein should be very useful for the preparation of C-4 modified taxoid analogs. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Uoto K,Takenoshita H,Ishiyama T,Terasawa H,Soga T

更新日期：1997-12-01 00:00:00

abstract：:A moisturizing cream mixed with a steroid ointment is frequently prescribed to patients suffering from atopic dermatitis. However, there is a concern that the mixing operation causes destabilization. The present study was performed to investigate the stability of such preparations closely using magnetic resonance imag...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Funatani C,Yamamoto Y,Fukami T,Koide T,Hayashi Y,Takayama K

更新日期：2017-01-01 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：:A series of 4-aza-5 alpha-androstane compounds with one or two aromatic moieties in the carbamoyl group at the C-17 position were synthesized and their inhibitory activities for rat and human prostatic testosterone 5 alpha-reductase were tested in vitro. Compounds with one aromatic moiety in the carbamoyl group showed...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurata H,Ishibashi K,Saito S,Hamada T,Horikoshi H,Furukawa Y,Kojima K

更新日期：1996-01-01 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：:A series of optically active substituted 1,2-dihydro-6-oxo-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids was prepared via optically active 2-methyl-4,5-difluoroindoline (10) and tested for antibacterial activities. Among them, (2S)-9-[(3R,1'S)-3-(1'-amino)ethyl-1-pyrrolidinyl]-8-fluoro-1,2-dihydro- 2- methyl-6-oxo-6H-...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsuji K,Tsubouchi H,Ishikawa H

更新日期：1995-10-01 00:00:00

abstract：:Conjugates of 2-aminooxyethyliminodiacetic acid with estrone, testosterone, epiandrosterone, 17-alpha-hydroxy-progesterone and progesterone were synthesized and their complexes with Tc-99m were successfully prepared in good yields, which indicated the agent to be promising for metal-labeling of biomolecules and relate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoda R,Karube Y,Takata J,Nagata Y,Matsushima Y

更新日期：1999-03-01 00:00:00

abstract：:Two novel pentanorcucurbitane triterpenes, 22-hydroxy-23,24,25,26,27-pentanorcucurbit-5-en-3-one (1) and 3,7-dioxo-23,24,25,26,27-pentanorcucurbit-5-en-22-oic acid (2) together with a new trinorcucurbitane triterpene, 25,26,27-trinorcucurbit-5-ene-3,7,23-trione (3) were isolated from the methyl alcohol extract of the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen CR,Liao YW,Wang L,Kuo YH,Liu HJ,Shih WL,Cheng HL,Chang CI

更新日期：2010-12-01 00:00:00

abstract：:Particles of poorly water-soluble drugs were prepared to develop a dry powder inhaler (DPI). Spray freeze-drying (SFD) technique using a four-fluid nozzle (4N), which has been developed by authors, was applied in this research. Ciclosporin and mannitol were used as a poorly water-soluble model drug and a dissolution-e...

journal_title：Chemical & pharmaceutical bulletin

authors： Niwa T,Mizutani D,Danjo K

更新日期：2012-01-01 00:00:00

abstract：:We have already reported unique compounds containing a N,O-spiro acetal structure as an orally active factor Xa (FXa) inhibitor. This time, we described a N,N-spiro acetal structure as an analogue of the N,O-spiro acetal structure for an orally active FXa inhibitor. The synthesis of these analogues could be achieved i...

journal_title：Chemical & pharmaceutical bulletin

authors： Saitoh F,Mukaihira T,Nishida H,Satoh T,Okano A,Yumiya Y,Ohkouchi M,Johka R,Matsusue T,Shiromizu I,Hosaka Y,Matsumoto M,Ohnishi S

更新日期：2006-11-01 00:00:00

abstract：:Using a microcalorimetric method, we have measured the heat production in states 3 and 4 respiration of a mitochondrial preparation from rat heart ventricle. Adenosine triphosphate production in state 3 respiration was also determined for the same preparation after heat production was measured. In Tris-buffered soluti...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamura K,Hayatsu H,Watanabe I,Nakano T,Sugawara Y,Nishii Y

更新日期：1989-11-01 00:00:00

abstract：:Italian canned tomatoes contain the tomato glycosides esculeosides B-1 (1, 0.0052%) and B-2 (2, 0.0068%) without esculeoside A. Herein, the structure of esculeoside B-1 (1) is characterized to be 3-O-β-lycotetraosyl (5S,22R,23S,25S)-22,26-epimino-16β,23-epoxy-3β,23,27-trihydroxycholestane 27-O-β-D-glucopyranoside. We ...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Fujiwara Y,Ikeda T,Ono M,Murakami K,Zhou JR,Yokomizo K,Nohara T

更新日期：2013-01-01 00:00:00

abstract：:The in vitro percutaneous transport of sodium diclofenac from various oil vehicles was examined using rat abdominal skin as a model skin membrane. The overall transport of diclofenac through the skin from the oleaginous vehicles was very poor because of a poor solubility of sodium diclofenac in nonpolar oils. To incre...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi K,Tamagawa S,Katagi T,Yoshitomi H,Kamada A,Rytting JH,Nishihata T,Mizuno N

更新日期：1991-01-01 00:00:00

abstract：:The influence of various phenolic compounds on the lactoperoxidase (LPO)/hydrogen peroxide (H2O2)-catalyzed oxidation of biochemical reductants such as reduced beta-nicotinamide adenine dinucleotide (NADH), reduced beta-nicotinamide adenine dinucleotide phosphate (NADPH) or reduced glutathione (GSH) was investigated b...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda J,Tsuchiya Y,Ozawa T

更新日期：2001-03-01 00:00:00

abstract：:The mechanism of the deprotonation of 2-butanone (1) with methoxide anion (2) was studied by ab initio molecular orbital (MO) methods. Calculations of the thermodynamic stabilities of each complex and the regioselectivity of the reaction were performed using a static isodensity surface polarized continuum model (IPCM)...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda H,Yukawa M,Niiya T

更新日期：2006-05-01 00:00:00

abstract：:A series of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones were designed, synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of target compounds had remarkable inhibitory activities on mushroom tyrosinase. Interestingly, compound 2h was found to be the mo...

journal_title：Chemical & pharmaceutical bulletin

authors： Yi W,Cao RH,Chen ZY,Yu L,Ma L,Song HC

更新日期：2009-11-01 00:00:00

abstract：:The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Sev...

journal_title：Chemical & pharmaceutical bulletin

authors： Ha ES,Baek IH,Cho W,Hwang SJ,Kim MS

更新日期：2014-01-01 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：:This paper describes practical and selective hydrogenation methodologies using heterogeneous palladium catalysts. Chemoselectivity develops dependent on the catalyst activity based on the characteristic of the supports, derived from structural components, functional groups, and/or morphologies. We especially focus on ...

journal_title：Chemical & pharmaceutical bulletin

authors： Monguchi Y,Ichikawa T,Sajiki H

更新日期：2017-01-01 00:00:00

abstract：:The purpose of this research is to investigate the applicability of terahertz (THz) reflectance spectroscopy for quantification of drug substance in tablets, so as to demonstrate the feasibility for applying this technique to tableting process monitoring. In order to acquire a suitable absorbance spectrum for this pur...

journal_title：Chemical & pharmaceutical bulletin

authors： Hisazumi J,Watanabe T,Suzuki T,Wakiyama N,Terada K

更新日期：2012-01-01 00:00:00

abstract：:Six new compounds, diospyrolide (1), diospyrolidone (2), diethyl (2R)-malate (3), 3-(E)-coumaroylbetulin-28-yl ethyl nonanedioate (4), 3-(E)-coumaroylbetulin-28-yl ethyl succinate (5), and 3-(E)-coumaroylbetulin-28-yl ethyl (2R)-2-hydroxysuccinate (6), have been isolated from the heartwood of Diospyros maritima. Compo...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chang CI

更新日期：2000-08-01 00:00:00