Synthesis and platelet-activating factor (PAF)-antagonistic activities of trisubstituted piperazine derivatives.


:2- or 3-Substituted 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclohepten-8- ylcarbonyl)-4-(3,4,5-trimethoxybenzoyl)- and 4-(3,4,5-trimethoxybenzyl)piperazines (2a-s, 3a, b) were prepared and evaluated for antagonistic activities against platelet-activating factor (PAF)-induced platelet aggregation and blood pressure reduction. The 2-methoxymethyl derivative (2f) showed the most potent activities in this series. The enantiomers (R)-(+)-2f and (S)-(-)-2f were synthesized from carbobenzoxy-O-benzyl-L- and D-serine in several steps. In the binding experiment, (S)-(-)-2f showed thirty times greater affinity than the R isomer for the PAF receptor.


Fukushi H,Mabuchi H,Terashita Z,Nishikawa K,Sugihara H




Has Abstract


1994-03-01 00:00:00












  • Design, Synthesis and Biological Evaluation of Oxindole-Based Chalcones as Small-Molecule Inhibitors of Melanogenic Tyrosinase.

    abstract::The enzyme tyrosinase regulates melanogenesis and skin hyperpigmentation by converting L-3,4-dihydroxyphenylalanine (L-DOPA) into dopaquinone, a key step in the melanin biosynthesis. The present work deals with design and synthesis of various oxindole-based chalcones as monophenolase and diphenolase activity inhibitor...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Suthar SK,Bansal S,Narkhede N,Guleria M,Alex AT,Joseph A

    更新日期:2017-01-01 00:00:00

  • Effect of metal ions on transcription of the ada gene which encodes O6-methylguanine-DNA methyltransferase of Escherichia coli.

    abstract::The effect of metal ions on transcription of the ada gene of Escherichia coli which is promoted by Ada protein in the presence of methylated deoxyribonucleic acid (DNA) was examined in a reconstituted system. Their effect on the O6-methylguanine-DNA methyltransferase (MGTase) activity of Ada protein was also examined....

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Takahashi K,Suzuki M,Sekiguchi M,Kawazoe Y

    更新日期:1992-09-01 00:00:00

  • Constituents of Crinoidea. 5. Isolation and structure of a new glycosyl inositolphosphoceramide-type ganglioside from the feather star Comanthina schlegeli.

    abstract::A new glycosyl inositolphosphoceramide-type ganglioside, CSP2, was obtained from the polar lipid fraction of the chloroform/methanol extract of the feather star Comanthina schlegeli together with a known same type of ganglioside CJP2. The structure of this ganglioside has been determined on the basis of chemical and s...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Inagaki M,Shiizaki M,Hiwatashi T,Miyamoto T,Higuchi R

    更新日期:2007-11-01 00:00:00

  • Paracetamol-propyphenazone interaction and formulation difficulties associated with eutectic formation in combination solid dosage forms.

    abstract::Polymorphic behaviours of paracetamol and propyphenazone and interaction between these two compounds were investigated using differential scanning calorimetry (DSC), X-ray powder diffraction and Fourier transform-infrared (FT-IR)-spectroscopy. Binary mixtures containing various ratios of the compounds were prepared as...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Zalac S,Khan MZ,Gabelica V,Tudja M,Mestrović E,Romih M

    更新日期:1999-03-01 00:00:00

  • Structure-activity relationships for a collection of structurally diverse inhibitors of purine nucleoside phosphorylase.

    abstract::Values of inhibition constants, Ki, and concentrations required for 50% inhibition, IC50, for a collection of structurally diverse competitive inhibitors of calf spleen purine nucleoside phosphorylase have been determined employing inosine as substrate. These values have been employed to create predictive quantitative...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Andricopulo AD,Yunes RA

    更新日期:2001-01-01 00:00:00

  • CCR5 antagonists as anti-HIV-1 agents. 1. Synthesis and biological evaluation of 5-oxopyrrolidine-3-carboxamide derivatives.

    abstract::A novel lead compound, N-(3-[4-(4-fluorobenzoyl)piperidin-1-yl]propyl)-1-methyl-5-oxo-N-phenylpyrrolidine-3-carboxamide (1), was identified as a CCR5 antagonist by high-throughput screening using [(125)I]RANTES and CCR5-expressing CHO cells. The IC(50) value of 1 was 1.9 microM. In an effort to improve the binding aff...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Imamura S,Ishihara Y,Hattori T,Kurasawa O,Matsushita Y,Sugihara Y,Kanzaki N,Iizawa Y,Baba M,Hashiguchi S

    更新日期:2004-01-01 00:00:00

  • Two new phenolic amides from the seeds of Pharbitis nil.

    abstract::Two new phenolic amides, pharnilatins A (1) and B (2), were isolated from the seeds of Pharbitis nil. These new compounds possess a p-coumaroyl unit with a structurally unique side chain, (2S,3S)-2,3-dihydroxyputrescine. The chemical structures and absolute stereochemistries of the new compounds were determined on the...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kim KH,Choi SU,Son MW,Lee KR

    更新日期:2010-11-01 00:00:00

  • Development and application of spectrophotometric methods for the determination of citalopram hydrobromide in dosage forms.

    abstract::Study was carried out to develop two simple, fast, accurate and sensitive spectrophotometric methods (A and B) for the determination of citalopram hydrobromide in commercial tablet formulations. In method A, UV spectrophotometer determined the contents of citalopram hydrobromide in tablets at 240 nm in methanol solven...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Raza A

    更新日期:2006-04-01 00:00:00

  • Rational design and synthesis of 4-o-substituted phenylmethylenethiosemicarbazones as novel tyrosinase inhibitors.

    abstract::In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yi W,Cao R,Chen Z,Yu L,Wen H,Yan Q,Ma L,Song H

    更新日期:2010-05-01 00:00:00

  • Use of Phthalimidoacetyl Isothiocyanate as a Scaffold in the Synthesis of Target Heterocyclic Systems, and Their Antimicrobial Assessment.

    abstract::Phthalimidoacetyl isothiocyanate underwent addition-cyclization reactions with some nitrogen and carbon nucleophilic reagents. Simultaneous or subsequent cyclization of the obtained adducts gave target heterocyclic systems such as 1,2,4-triazoles, 1,3-diazines, 1,3-oxazines and thiourea attached to a phthalimido moiet...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Hemdan MM,El-Sayed AA

    更新日期:2016-01-01 00:00:00

  • First synthesis of a alpha-trifluoromethyl allenol ether via the Julia-Lythgoe process.

    abstract::Alpha-trifluoromethyl allenol ethers 9a-e were prepared in moderate to good yields by the Julia-Lythgoe process using beta-ethoxy-beta-trifluoromethyl vinylic sulfone 3. Several reactions of 9c were examined to give alpha,beta-unsaturated trifluoromethyl ketone derivatives 11 and 12. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yoshimatsu M,Hibino M

    更新日期:2000-09-01 00:00:00

  • Structure-activity relationship of bis-galloyl derivatives related to (-)-epigallocatechin gallate.

    abstract::Green tea and (-)-epigallocatechin gallate (EGCG: one of main components of green tea) are well known to have preventive activities against human cancers. Previously, using a galloyl group as a core structure derived from EGCG, we developed alkyl gallate and gallamide derivatives, which showed strong antiproliferative...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Dodo K,Minato T,Hashimoto Y

    更新日期:2009-02-01 00:00:00

  • Tannins and related polyphenols of euphorbiaceous plants. XI. Three new hydrolyzable tannins and a polyphenol glucoside from Euphorbia humifusa.

    abstract::Three new hydrolyzable tannins, euphormisins M1, M2, and M3, were isolated from Euphorbia humifusa WILLD., and respectively characterized as 1,3,6-tri-O-galloyl-4-O- brevifolincarboxyl-beta-D-glucose (19), an oxidative metabolite (23) of geraniin, and 1,3,6-tri-O-galloyl-alpha-D-glucose (18), by spectroscopic and chem...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yoshida T,Amakura Y,Liu YZ,Okuda T

    更新日期:1994-09-01 00:00:00

  • Novel Orally Disintegrating Tablets Produced Using a High-Pressure Carbon Dioxides Process.

    abstract::It is well known that high-pressure carbon dioxide (CO2) lowers the glass transition temperature (Tg) of polymers. We therefore investigated whether Tg depression of high-pressure CO2 results in interparticle bridging of a polymer and the tablet characteristics that makes the manufacture of an orally disintegrating ta...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kobayashi M,Shinozuka D,Kondo H,Sako K,Otake K

    更新日期:2018-01-01 00:00:00

  • Pyrrole Oligoglycosides from the Starfish Acanthaster planci Suppress Lipopolysaccharide-Induced Nitric Oxide Production in RAW264.7 Macrophages.

    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

    pub_type: 杂志文章


    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

  • Synthesis and antimicrobial activity of pyridines bearing thiazoline and thiazolidinone moieties.

    abstract::Two series of new pyridines bearing thiazoline (3a--n) and thiazolidinone (5a--e) moieties were prepared via the cyclization of the corresponding substituted pyridyl thiourea (2a--g) with an appropriately substituted phenacyl bromide or chloroacetic acid, respectively. The antimicrobial activity was determined for rep...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Hassan HY,el-Koussi NA,Farghaly ZS

    更新日期:1998-05-01 00:00:00

  • Decomposition of linear dodecylbenzenesulfonate by simultaneous treatment with ozone and ultraviolet irradiation: rapid disappearance of formed mutagens.

    abstract::The decomposition products and mutagenic activity in Salmonella typhimurium strains TA98, TA100 and TA104 in the presence and absence of S9 mix of linear dodecylbenzenesulfonate (DBS) in aqueous solution after ozone treatment alone or simultaneous treatment with ozone and ultraviolet (UV) irradiation (ozone/UV treatme...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Murakami K,Matsumoto H,Kinouchi T,Ohnishi Y

    更新日期:1992-06-01 00:00:00

  • Preparation and properties of a mitomycin C-albumin conjugate.

    abstract::Mitomycin C, an anti-neoplastic agent, was covalently attached to bovine serum albumin through various kinds of spacers such as glutaryl, succinyl, trans-aconityl, methylsuccinyl and the trimellityl group. The prior acylation of albumin not only prevented protein polymerization in the presence of carbodiimide, but als...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kaneo Y,Tanaka T,Iguchi S

    更新日期:1990-09-01 00:00:00

  • Production of sesquiterpene-type phytoalexins by hairy roots of Hyoscyamus albus co-treated with cupper sulfate and methyl jasmonate.

    abstract::The production of sesquiterpene-type phytoalexins with a vetispyradiene skeleton by Hyoscyamus albus hairy roots induced by methyl jasmonate (MeJA) was reported in a previous paper. The production pattern on co-treatment with cupper sulfate and MeJA (CuSO(4)-MeJA) showed a TLC profile differing from that on treatment ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kawauchi M,Arima T,Shirota O,Sekita S,Nakane T,Takase Y,Kuroyanagi M

    更新日期:2010-07-01 00:00:00

  • Synthesis of macromolecular prodrugs of procaine, histamine and isoniazid.

    abstract::The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Giammona G,Giannola LI,Carlisi B,Bajardi ML

    更新日期:1989-08-01 00:00:00

  • Sesquiterpenes from Ainsliaea fragrans and their inhibitory activities against cyclooxygenases-1 and 2.

    abstract::One new guaiane-type sesquiterpene glycoside, 2'-O-E-caffeoyl-8alpha-hydroxy-11alpha,13-dihydro-3beta-O-beta-D-glucozaluzanin C (1), was isolated from the whole herb of Ainsliaea fragrans (Compositae), together with five known sesquiterpene lactones: 8alpha-hydroxy-11alpha,13-dihydro-3beta-O-beta-D-glucozaluzanin C (2...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Wang H,Wu T,Yan M,Liu G,Li P,Zhang XQ,Ye WC,Zhang LY

    更新日期:2009-06-01 00:00:00

  • Formation and conformation of baicalin-berberine and wogonoside-berberine complexes.

    abstract::It is well-known that baicalin-berberine complex (1) precipitates in the water decoction of numerous Chinese Medicinal formulae containing Radix Scutellariae and Rhizoma Coptidis or Cortex Phellodendri. In the current study, ionic interaction between the carboxylate ion of baicalin and the quaternary ammonium ion of b...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Wang JR,Tanaka T,Zhang H,Kouno I,Jiang ZH

    更新日期:2012-01-01 00:00:00

  • Studies on the constituents of Ailanthus integrifolia.

    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

    pub_type: 杂志文章


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

    更新日期:1994-08-01 00:00:00

  • Studies on cardiotonic agents. I. Synthesis of some quinazoline derivatives.

    abstract::A series of quinazoline derivatives with various 4-heterocyclylpiperidino groups at the 4-position was synthesized and tested for cardiotonic activity in anesthetized dogs. Among them, several 6,7-dimethoxyquinazoline derivatives showed potent cardiotonic activity. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Nomoto Y,Obase H,Takai H,Hirata T,Teranishi M,Nakamura J,Kubo K

    更新日期:1990-06-01 00:00:00

  • Benzylidene 2-aminoimidazolones derivatives: synthesis and in vitro evaluation of anti-tumor carcinoma activity.

    abstract::A series of benzylidene 2-aminoimidazolones derivatives were synthesized. Most compounds displayed strong inhibitory activity on the proliferation of human HepG2 cells in vitro. The active compounds were further evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against five human ca...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ling Y,Wang ZQ,Xiao YA,Zhu C,Shen L,Wang XM,Hui Y,Wang XY

    更新日期:2013-01-01 00:00:00

  • Application of a self-organizing map to quantitative structure-activity relationship analysis of carboquinone and benzodiazepine.

    abstract::Self-organizing map (SOM) of Kohonen seems to be a promising approach beyond the standard one to regression for some classification problems encountered in the field of pharmacy. We apply them, therefore, to the quantitative structure-activity relationship (QSAR) in carboquinones and benzodiazepines, and show their us...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kawakami J,Hoshi K,Ishiyama A,Miyagishima S,Sato K

    更新日期:2004-06-01 00:00:00

  • CTRP12 Ameliorated Lipopolysaccharide-Induced Cardiomyocyte Injury.

    abstract::C1q/tumor necrosis factor (TNF)-related protein 12 (CTRP12) is a secretory protein that participates in the regulation of glucose and lipid metabolism in obesity and diabetes. Its role in cardiovascular disease, particularly sepsis-induced cardiac injury, is unclear. Here, we stimulated cardiomyocytes with lipopolysac...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Zhou MQ,Jin E,Wu J,Ren F,Yang YZ,Duan DD

    更新日期:2020-01-01 00:00:00

  • Flavonol glycosides from Muehlenbeckia platyclada and their anti-inflammatory activity.

    abstract::A new flavonol, morin-3-O-alpha-rhamnopyranoside (1), along with four known flavonols, kaempferol 3-O-alpha-rhamnopyranoside (2), kaempferol 3-O-beta-glucopyranoside (3), quercetin 3-O-alpha-rhamnopyranoside (4) and (+)-catechin (5), were isolated from the methanolic extract of Muehlenbeckia platyclada. The structures...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yen CT,Hsieh PW,Hwang TL,Lan YH,Chang FR,Wu YC

    更新日期:2009-03-01 00:00:00

  • Prolonged Distribution of Tranilast in the Eyes after Topical Application onto Eyelid Skin.

    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

    pub_type: 杂志文章


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

    更新日期:2020-01-01 00:00:00

  • Seven-membered vibsane-type diterpenes with a 5,10-cis relationship from Viburnum awabuki.

    abstract::New five seven-membered vibsane-type diterpenes named 5-epi-vibsanin C, 5-epi-vibsanin H, 5-epi-vibsanin K, 18-O-methyl-5-epi-vibsanin K and 5-epi-vibsanin E have been isolated from the leaves of Viburnum awabuki (Caplifoliaceae). Their structures have been elucidated by analyses of spectroscopic data and comparison o...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Fukuyama Y,Minami H,Matsuo A,Kitamura K,Akizuki M,Kubo M,Kodama M

    更新日期:2002-03-01 00:00:00