Preparations of anthraquinone and naphthoquinone derivatives and their cytotoxic effects.

abstract：:A series of bicyclic thiazoline derivatives (4a-s) was synthesized and evaluated for hepatoprotective activity against galactosamine-induced and monoclonal antibody-induced acute liver injuries in rats. The structure-activity relationships were investigated. Among the compounds synthesized, ethyl 3-(N-methylcarbamoyl)...

journal_title：Chemical & pharmaceutical bulletin

authors： Hasegawa M,Nakayama A,Hosokami T,Kurebayashi Y,Ikeda T,Shimoto Y,Ide S,Honda Y,Suzuki N

更新日期：1995-01-01 00:00:00

abstract：:To investigate the possible binding mode of E-64 (N-[N-(L-3-trans-carboxyoxirane-2-carbonyl)-L-leucyl]agmatine), a potent cysteine protease inhibitor, to papain active site, molecular dynamics simulations were applied to two complex forms: R- and S- configurational forms of E-64 C2 atom for the covalent bond formation...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto D,Ohishi H,Ishida T,Inoue M,Sumiya S,Kitamura K

更新日期：1990-09-01 00:00:00

abstract：:Cigarette smoke, a collection of many toxic chemicals, contributes to the pathogenesis of smoking-related diseases such as chronic obstructive pulmonary disease and cancer. Much work has been done on the chemical analysis of ingredients in cigarette smoke, but there are few reports on the active ingredients that can m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi Y,Horiyama S,Honda C,Suwa K,Nakamura K,Kunitomo M,Shimma S,Toyoda M,Sato H,Shizuma M,Takayama M

更新日期：2013-01-01 00:00:00

abstract：:The admixture of a steroid ointment and a moisturizing cream is frequently prescribed to patients suffering from atopic dermatitis. For the mixing operation, a revolution/rotation-type hybrid mixer is widely used in pharmacy. The purpose of this study was to monitor the mixed state of the admixtures during the mixing ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokokawa M,Setoyama H,Okada K,Hayashi Y,Machida Y,Onuki Y,Obata Y

更新日期：2018-01-01 00:00:00

abstract：:To expand the sequence of double-stranded DNA (dsDNA) targets in a triplex formation, 2',4'-BNAs (2'-O,4'-C-methylene bridged nucleic acids) having imidazoles as a nucleobase were synthesized and incorporated into oligonucleotides. Triplex-forming ability of the modified oligonucleotides was evaluated by using melting...

journal_title：Chemical & pharmaceutical bulletin

authors： Hari Y,Obika S,Inohara H,Ikejiri M,Une D,Imanishi T

更新日期：2005-07-01 00:00:00

abstract：:Design of compounds having good anti-tubercular activity is gaining much importance in the field of tuberculosis research due to reemergence of antibiotic resistance strains. In this paper quantitative structure activity relationships (QSAR) were developed on chalcones, chalcone-like compounds, flavones and flavanones...

journal_title：Chemical & pharmaceutical bulletin

authors： Sivakumar PM,Geetha Babu SK,Mukesh D

更新日期：2007-01-01 00:00:00

abstract：:To find candidates with high antimicrobial and low hemolytic activities, many gramicidin S (GS) analogs of various ring sizes have been designed and synthesized. However, syntheses of antimicrobially active analogues of GS having a disordered symmetry structure from C(2) have almost never been reported, because the st...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamaki M,Takanashi K,Harada T,Fujinuma K,Shindo M,Kimura M,Uchida Y

更新日期：2011-01-01 00:00:00

abstract：:Novel neutral glycosphingolipids isolated from the plerocercoids of a tapeworm, Spirometra erinacei, may be expected to be involved in host-parasite interactions. We have synthesized this glycosphingolipid analogue containing 2-branched fatty alkyl residue in place of ceramide. Glycosylation of nonreducing-end trisacc...

journal_title：Chemical & pharmaceutical bulletin

authors： Hada N,Kuroda M,Takeda T

更新日期：2000-08-01 00:00:00

abstract：:Two new pyrrole oligoglycosides, plancipyrrosides A and B (1 and 2), were isolated from methanol extract of the Vietnamese starfish Acanthaster planci using various chromatographic procedures. Their structures were elucidated by spectroscopic methods including one and two dimensional (1D- and 2D)-NMR and Fourier trans...

journal_title：Chemical & pharmaceutical bulletin

authors： Vien LT,Hanh TT,Huong PT,Dang NH,Thanh NV,Lyakhova E,Cuong NX,Nam NH,Kiem PV,Kicha A,Minh CV

更新日期：2016-11-01 00:00:00

abstract：:With the aim of improving of the efficacy and decreasing the side effects of oxybutynin (1), N-[(tetrahydro-3- or 4-pyridyl)methyl]-, N-(4-piperidyl)-, and N-(3- or 4-piperidylalkyl)-2-hydroxyacetamides (3a-n, 4a-g) and the related carboxamides (3o-r, 4h-k, 13', 17) were synthesized and evaluated for inhibitory activi...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi K,Tsubaki K,Mizuno H,Take K,Okumura K,Terai T,Shiokawa Y

更新日期：1994-01-01 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：:The bitter and sweet forms of a plant species differing with alkaloid contents may provide a model system for investigation of alkaloid biosynthesis at a molecular level. The pattern and concentration of quinolizidine alkaloids were determined by capillary GC-MS in bitter and sweet plants of Lupinus angustifolius. Bit...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirai MY,Suzuki H,Yamazaki M,Saito K

更新日期：2000-10-01 00:00:00

abstract：:Chiral building block syntheses of promising drugs were achieved using two types of catalytic stereoselective cyanosilylations of aldehydes promoted by Lewis acid-Lewis base bifunctional catalysts 1 and 2 as the key steps (diastereoselective cyanosilylation of amino aldehyde and enantioselective cyanosilylation). In t...

journal_title：Chemical & pharmaceutical bulletin

authors： Nogami H,Kanai M,Shibasaki M

更新日期：2003-06-01 00:00:00

abstract：:Four new ursane-type triterpenes, 3beta-acetoxy-11alpha-methoxy-12-ursene (1), 3beta-acetoxy-11alpha-ethoxy-12-ursene (2), 3beta-acetoxy-11alpha-hydroperoxy-12-ursene (3), 3beta-hydroxy-11alpha-hydroperoxy-12-ursene (4), and two new oleanane-type triterpenes, 3beta-acetoxy-11alpha-ethoxy-12-oleanene (5), 3beta-acetoxy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chiang YM

更新日期：2000-05-01 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：:Evaluating the acute toxic effects of drugs or toxins is based mainly on studies which require the use of light microscopy. Recently, the effects of such substances on biological membranes, such as the nasal membrane, has been studied using the traditional Ussing chambers, which make it possible to study the transepit...

journal_title：Chemical & pharmaceutical bulletin

authors： Gizurarson S,Tamura S,Kurata T

更新日期：1991-06-01 00:00:00

abstract：:Analogs related to 1 alpha,25-dihydroxy-2 beta-(3-hydroxypropoxy)vitamin D3 (ED-71) (4), oxa-type and carba-type analogs of vitamin D3 bearing substituents at the 2 beta-position of 1 alpha,25-dihydroxyvitamin D3 (1), were synthesized from the alpha-epoxides (6 and 13). Three analogs, ED-71 (4) and two carba-type anal...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono Y,Watanabe H,Shiraishi A,Takeda S,Higuchi Y,Sato K,Tsugawa N,Okano T,Kobayashi T,Kubodera N

更新日期：1997-10-01 00:00:00

abstract：:Asymmetric epoxidation reactions of chalcone derivatives catalyzed by chiral calcium complexes using hydrogen peroxide were developed. The epoxidation reactions proceeded smoothly to afford the desired products in good yields with good enantioselectivities. This is the first example of chiral calcium-catalyzed asymmet...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita Y,Macor JA,Fushimi S,Tsubogo T,Kobayashi S

更新日期：2018-01-01 00:00:00

abstract：:A method for scale-up of a lubricant mixing process in a V-type blender was proposed. Magnesium stearate was used for the lubricant, and the lubricant mixing experiment was conducted using three scales of V-type blenders (1.45, 21 and 130 L) under the same fill level and Froude (Fr) number. However, the properties of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Horibe M,Sonoda R,Watano S

更新日期：2018-01-01 00:00:00

abstract：:Six new dammarane-type triterpene diglycosides with a hydroperoxide group, floralginsenosides A, B, C, D, E, and F, were isolated from ginseng flower, the flower buds of Panax ginseng C. A. MEYER, together with seven known dammarane-type triterpene oligoglycosides. The structures of new floralginsenosides were elucida...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Sugimoto S,Nakamura S,Matsuda H

更新日期：2007-04-01 00:00:00

abstract：:Glycyrrhetinic acid (Ia) and eighteen related derivatives were examined for antiulcer activity using stress-induced gastric lesions (restraint plus water immersion at 25 degrees C) in mice and rats as screening tests. Among the compounds tested, dihemiphthalate derivatives of 18 alpha- or 18 beta-olean-12-ene-3 beta,3...

journal_title：Chemical & pharmaceutical bulletin

authors： Yano S,Harada M,Watanabe K,Nakamaru K,Hatakeyama Y,Shibata S,Takahashi K,Mori T,Hirabayashi K,Takeda M

更新日期：1989-09-01 00:00:00

abstract：:This paper introduces a new delivery system for rapid and controlled drug release. Mixture of hydrophilic, (poly vinyl alcohol, PVA, and randomly methylated beta-cyclodextrin, RM beta-CD), and hydrophobic (poly D,L-lactide, PLA, and poly D,L-lactide-co-glycoside, PLGA) polymers were electrospun to make a multi-layered...

journal_title：Chemical & pharmaceutical bulletin

authors： Fathi-Azarbayjani A,Chan SY

更新日期：2010-02-01 00:00:00

abstract：:Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurashima H,Uchida S,Kashiwagura Y,Tanaka S,Namiki N

更新日期：2020-01-01 00:00:00

abstract：:A mechanism for the relatively high permeability of vitamin C in relation to the change in the protein domain of the stratum corneum has been proposed. Firstly, the skin permeation characteristics of vitamin C (l-[1-14C]-ascorbic acid) using whole skin and stripped skin of the hairless mouse were investigated. By empl...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee AR,Tojo K

更新日期：1998-01-01 00:00:00

abstract：:Amodiaquine (AQ) is an antimalarial which is effective against chloroquino-resistant strains of Plasmodium falciparum but whose clinical use is severely restricted because of associated hepatotoxicity and agranulocytosis. "One-pot" synthesis of formamidines likely to be transformed into AQ derivatives is reported. Com...

journal_title：Chemical & pharmaceutical bulletin

authors： Delarue S,Girault S,Dali Ali F,Maes L,Grellier P,Sergheraert C

更新日期：2001-08-01 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：:Xanthones and acridones were synthesized from 3,4-difluoronitrobenzene and 2-fluorobenzaldehydes in two or three steps. The key step was nucleophilic aroylation catalyzed by imidazolidenyl carbene. The nucleophilic aroylation of 3,4-difluoronitrobenzene afforded 2,2'-difluoro-4-nitrobenzophenones. The cyclization of t...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki Y,Toyota T,Miyashita A,Sato M

更新日期：2006-12-01 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：:The percutaneous (p.c.) absorption of clonazepam (CZP), an antiepileptic drug, was investigated in rabbits. CZP was efficiently absorbed from a gel ointment (0.5% CZP, 1g, 9 cm2) with Azone and therapeutic plasma concentrations were maintained for 27 h. The bioavailability of CZP from the gel ointment was 47.2 +/- 3.1...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogiso T,Ito Y,Iwaki M,Yamamoto Y

更新日期：1989-02-01 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