Synthesis and azannulation of pyridinylaminohexadienones.

abstract：:The purpose of this study was to determine which foods and/or drinks are capable of reducing the bitterness of topiramate when consumed together with the medicine. The inhibitory effects of foods/drinks (yoghurt and nine other foods/drinks) on the bitterness of topiramate (5 mg/mL) were evaluated with a taste sensor u...

journal_title：Chemical & pharmaceutical bulletin

authors： Haraguchi T,Uchida T,Hazekawa M,Yoshida M,Nakashima M,Sanda H,Hase T,Tomoda Y

更新日期：2016-01-01 00:00:00

abstract：:Using the unique character of the chiral Pd complexes 1 and 2, highly efficient catalytic asymmetric reactions have been developed. In contrast to conventional Pd(0)-catalyzed reactions, these complexes function as an acid-base catalyst. Thus active methine and methylene compounds were activated to form chiral palladi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hamashima Y

更新日期：2006-10-01 00:00:00

abstract：:Thermodynamic studies were carried out to evaluate the binding of theophylline on adenosine deaminase (ADA) in 50 mM sodium phosphate buffer pH 7.5, at 300 K, using isothermal titration calorimetry (ITC). A simple method for determination of binding isotherm in the drug--ADA interaction was applied using ITC data. ADA...

journal_title：Chemical & pharmaceutical bulletin

authors： Saboury AA,Bagheri S,Ataie G,Amanlou M,Moosavi-Movahedi AA,Hakimelahi GH,Cristalli G,Namaki S

更新日期：2004-10-01 00:00:00

abstract：:Three aromatic compounds (2-4) possessing a carbomethoxyl group or a dimethoxyphthaloyl group, prepared by the Diels-Alder reaction of the cardiac glycoside, proscillaridin (1), with dimethyl acetylenedicarboxylate and methyl propiolate, were transformed into alcohols, carboxylic acids and amides. The biological activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanase T,Murakami N,Nagai S,Ueda T,Sakakibara J,Ando H,Hotta Y,Takeya K

更新日期：1992-02-01 00:00:00

abstract：:Nitroxyl (HNO), a one-electron-reduced form of nitric oxide, has various biological activities, including a cardioprotective effect. Here, we first synthesized another, more hydrophilic photocontrollable HNO donor (3), which can release HNO in a spatially and temporally controlled manner, and then examined the propert...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuo K,Nakagawa H,Adachi Y,Kameda E,Aizawa K,Tsumoto H,Suzuki T,Miyata N

更新日期：2012-01-01 00:00:00

abstract：:Two novel triterpenoid saponins, ardisicrenoside C (1) [3 beta-O-(alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->4)- [beta-D-glucopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)-16 alpha, 28-dihydroxy-olean-12-en-30-oic acid 30-O-beta-D-glucopyranosyl ester] and ardisicrenoside D (2) [3 beta-O-(beta-D-xylopyr...

journal_title：Chemical & pharmaceutical bulletin

authors： Jia Z,Koike K,Nikaido T,Ohmoto T,Ni M

更新日期：1994-11-01 00:00:00

abstract：:A new route to (+)-estrone has been developed starting from the chiral building block having a bicyclo[3.2.1]octane framework based on the inherent stereochemical chemical nature of the chiral building block. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hanada K,Miyazawa N,Ogasawara K

更新日期：2003-01-01 00:00:00

abstract：:From the MeOH extract of the aerial part of Vietnamese Orthosiphon stamineus, five new isopimarane-type diterpenes [orthosiphols F-J (1-5)] and two new diterpenes [staminols A (6) and B (7)] with a novel carbon-framework, to which we proposed the name "staminane", and three new highly-oxygenated staminane-type diterpe...

journal_title：Chemical & pharmaceutical bulletin

authors： Tezuka Y,Stampoulis P,Banskota AH,Awale S,Tran KQ,Saiki I,Kadota S

更新日期：2000-11-01 00:00:00

abstract：:Two major and two minor forms of dihydrodiol dehydrogenase with similar molecular weights of around 36000 were purified from monkey liver cytosol. All the forms oxidized trans-dihydrodiols of benzene and naphthalene and reduced aromatic aldehydes, but showed differences in charge, specificity for other substrates and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakagawa M,Harada T,Hara A,Nakayama T,Sawada H

更新日期：1989-10-01 00:00:00

abstract：:Novel C(7)-derivatives of 1-cyclopropyl-6-fluoro-4-quinolone carboxylic acid (3a-o) have been synthesized and evaluated for in vitro antibacterial activity. Compounds 3e (3-aminocyclobutyl), 3g (1-aminocyclopropyl), 3m ((2-aminomethyl)vinyl), and 3o ((1-aminomethyl)vinyl) showed significant inhibitory activity, compar...

journal_title：Chemical & pharmaceutical bulletin

authors： Todo Y,Nitta J,Miyajima M,Fukuoka Y,Ikeda Y,Yamashiro Y,Saikawa I,Narita H

更新日期：1994-10-01 00:00:00

abstract：:A novel C-methylated biflavone, taiwanhomoflavone-B (1), together with known compounds, 7,4',7"-tri-O-methylamentoflavone, 6-C-methylnaringenin and apigenin-7-O-beta-glucoside were isolated from an ethanolic extract of Cephalotaxus wilsoniana. The structure of 1 was elucidated on the basis of spectroscopic analysis. T...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Hwang SY,Yang Kuo LM,Lee YL,Li SY,Shen YC

更新日期：2002-12-01 00:00:00

abstract：:Corollosporine isolated from the marine fungus Corollospora maritima and N-analogous corollosporines are antimicrobial substances. Owing to the basic structure of the N-analogous corollosporines, they have become an attractive target for laccase-catalyzed derivatisation. In this regard we report on the straightforward...

journal_title：Chemical & pharmaceutical bulletin

authors： Mikolasch A,Hessel S,Salazar MG,Neumann H,Manda K,Gōrdes D,Schmidt E,Thurow K,Hammer E,Lindequist U,Beller M,Schauer F

更新日期：2008-06-01 00:00:00

abstract：:The amount of adsorption of bovine serum albumin (BSA) by hydroxyapatite (HAP) increased with a concentration of CaCl2 due to the bridging effect of Ca2+ between adsorbate BSA and adsorbent HAP. On the other hand, it decreased remarkably with a concentration of K2HPO4. This was explained in terms of the effects of ion...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimabayashi S,Tanizawa Y,Ishida K

更新日期：1991-09-01 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：: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：:Tranilast, a lipophilic drug with various ophthalmic applications, was used as a model drug to establish the possibility of delivering lipophilic drugs through the eyelid skin. Pharmacokinetics and tissue distribution studies were conducted employing three application methods (topical application onto eyelid skin, eye...

journal_title：Chemical & pharmaceutical bulletin

authors： See GL,Arce F Jr,Itakura S,Todo H,Sugibayashi K

更新日期：2020-01-01 00:00:00

abstract：:A new toxic neoanisatin-derivative (1) was isolated from the pericarps of Illicium majus. The structure of this compound was elucidated by spectroscopic data, including the 2D COSY NMR technique. The toxicity of compound 1 is also described. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang CS,Hashimoto M,Baba N,Takahashi M,Kaneto H,Kawano N,Kouno I

更新日期：1990-01-01 00:00:00

abstract：:In the present study, a novel series of 2-(2-(3-aryl-5-substituted-1,3,4-thiadiazol-2(3H)-ylidene)hydrazinyl)-4,4-diphenyl-1H-imidazol-5(4H)-one derivatives were designed and prepared via the reaction of the most versatile, hitherto unreported 2-(5-oxo-4,4-diphenyl-4,5-dihydro-1H-imidazol-2-yl)-N-phenylhydrazinecarbot...

journal_title：Chemical & pharmaceutical bulletin

authors： Gomha SM,Abdel-Aziz HM,Khalil KD

更新日期：2016-01-01 00:00:00

abstract：:The structural conversion of the prion protein (PrP) from the normal cellular isoform (PrP(C)) to the posttranslationally modified form (PrP(Sc)) is thought to relate to Cu²⁺ binding to histidine (H) residues. Traditionally, the binding of metals to PrP has been investigated by monitoring the conformational conversion...

journal_title：Chemical & pharmaceutical bulletin

authors： Kojima A,Mabuchi Y,Konishi M,Okihara R,Nagano M,Akizawa T

更新日期：2011-01-01 00:00:00

abstract：:The n-BuOH extract of Swertia japonica showed a significant hepatoprotective effect on D-galactosamine (D-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice. The activity-guided fractionation led to the isolation of a new tetrahydroxanthone derivative, tetrahydroswertianolin (1), as well as two known iridoids...

journal_title：Chemical & pharmaceutical bulletin

authors： Hase K,Li J,Basnet P,Xiong Q,Takamura S,Namba T,Kadota S

更新日期：1997-11-01 00:00:00

abstract：:A new pregnane glycoside, a dibenzylbutyrolactone lignan, 5-hydroxymatairesinol dimethyl ether, and three new flavonoids, including one 8-methylflavan-3-ol, and two 8-methylflavones, together with five known flavonoids and two known alkaloids were isolated from the rhizomes of Tupistra chinensis. The structures of all...

journal_title：Chemical & pharmaceutical bulletin

authors： Pan WB,Wei LM,Wei LL,Wu YC

更新日期：2006-07-01 00:00:00

abstract：:A chemical investigation on a South China Sea gorgonian, Menella sp. resulted in the isolation and elucidation of menellin A (1), a highly oxygenated racemate with C(8) skeleton, and a polyhydroxylated steroid, menellsteroid C (2), along with eight known compounds (3-10). The structures of the new compounds were eluci...

journal_title：Chemical & pharmaceutical bulletin

authors： Chai XY,Sun JF,Tang LY,Yang XW,Li YQ,Huang H,Zhou XF,Yang B,Liu Y

更新日期：2010-10-01 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：:Bis[2-[(E)-2-octenoylamino]ethyl] disulfide (compd. I-3) inhibited collagen- and arachidonic acid-induced rat platelet aggregation, although not adenosine 5'-diphosphate (ADP)-induced rat platelet aggregation. Based on these results, we then investigated the inhibitory effect of compd. I-3 on thromboxane B2 formation ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimura T,Nakajima H,Tsujikawa K,Yasuda N,Haruyama M,Okabe M,Iwai M,Yokoyama K

更新日期：1989-03-01 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：:Adriamycin linked to oxidized dextran (ADM-OXD) via Schiff's base formation was compared with free adriamycin with regard to antitumor activity, acute toxicity and plasma pharmacokinetics in rats following i.v. administration. ADM-OXD showed higher activity against Walker carcinosarcoma 256 than free adriamycin. On th...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda Y,Munechika K,Kikukawa A,Kanoh Y,Yamanouchi K,Yokoyama K

更新日期：1989-06-01 00:00:00

abstract：:The asymmetric platinum complexes cis-Pt(LL')Cl2 (L = NH3, L' = CH3NH2, (CH3)2NH, C2H5NH2 and (C2H5)2NH and LL' = N,N-dimethylethylenediamine),--one of the NH3 groups of cis-Pt(NH3)2Cl2 was substituted by alkylamine--, were synthesized and their cytotoxic effects have been measured using L-1210 cells. The IC50 values ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirano T,Inagaki K,Fukai T,Alink M,Nakahara H,Kidani Y

更新日期：1990-10-01 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：:A novel floating sustained release tablet having a cavity in the center was developed by utilizing the physicochemical properties of L-menthol and the penetration of molten hydrophobic polymer into tablets. A dry-coated tablet containing famotidine as a model drug in outer layer was prepared with a L-menthol core by d...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuda M,Goto A

更新日期：2011-01-01 00:00:00

abstract：:2,3-Epoxy-4-hydroxy-4-((E,E)-3,6-octadienyl)cyclopentanone (dl-carbacerulenin 5) was synthesized via the epoxyketones 15a and 15b as a mimic of the active form of the antibiotics cerulenin 1, a potent inhibitor of fatty acid synthetase (FAS). The monobenzyl ethers (12 and 13), synthetic intermediates of 15, were prepa...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimazawa R,Ogawa Y,Morisaki N,Funabashi H,Kawaguchi A,Iwasaki S

更新日期：1992-11-01 00:00:00