Syntheses and antiulcer activities of 2-aminonorbornene derivatives.

abstract：:Tumor necrosis factor (TNF), a cytokine produced in macrophages, also acts as an endogenous pyrogen (EP). To investigate whether TNF has a role in the fever induced by Nocardia rubra cell wall skeleton (N-CWS), the relationship between fever and TNF production was studied in guinea pigs. N-CWS injected i.v. to guinea ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohara K,Hirano Y,Ishida H,Mori J,Tensho A

更新日期：1989-10-01 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：:Acidic segment of an acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor, R-106578 was synthesized by enantioselective hydrogenation of the Z-olefine (9-(Z)) using (R)-2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (BINAP)-Ru(OAc)2 as a catalyst in methanol at 100 degrees C, 5 kgf/cm2 of H2 pressure. The requisite Z-o...

journal_title：Chemical & pharmaceutical bulletin

authors： Murakami M,Kobayashi K,Hirai K

更新日期：2000-10-01 00:00:00

abstract：:The interaction of halofantrine with phosphatidylcholine and phosphatidylethanolamine bilayers has been investigated by differential scanning calorimetry. Halofantrine caused a broadening of the gel to liquid crystalline phase transition endotherm of the phosphatidylcholines. A decrease in the transition temperature T...

journal_title：Chemical & pharmaceutical bulletin

authors： Lim LY,Go ML

更新日期：1999-06-01 00:00:00

abstract：:The full structures of the two steroidal saponins from Narthecium asiaticum MAXIM. We previously identified as toxic substances by monitoring the toxicity in guinea pigs were phytochemically reinvestigation on the aerial parts of the plant. The desired toxic saponins (6,7) were isolated together with two known lignan ...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue T,Mimaki Y,Sashida Y,Kobayashi M

更新日期：1995-07-01 00:00:00

abstract：:We investigated the distribution and stability of pirarubicin in human blood obtained from 12 healthy volunteers. The distribution of pirarubicin into blood cells showed marked temperature- and concentration-dependencies and the Arrhenius plot for pirarubicin uptake in blood was biphasic. Therefore, pirarubicin appear...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagasawa K,Kitada N,Tsuji C,Ogawa M,Yokoyama T,Ohnishi N,Iwakawa S,Okumura K

更新日期：1992-10-01 00:00:00

abstract：:We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazo...

journal_title：Chemical & pharmaceutical bulletin

authors： Suh JH,Yum EK,Cho YS

更新日期：2015-01-01 00:00:00

abstract：:We synthesized the racemates of the five presumed metabolites (1b-f) of (S)-(--)-N-tert-butyl-4,4-diphenyl-2-cyclopentenylamine hydrochloride (FK584, S(--)-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate their inhibitory a...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi K,Miyao Y,Yamano K,Yamamoto T,Terai T,Kusunoki T,Tsubaki K,Shiokawa Y

更新日期：1996-06-01 00:00:00

abstract：:Conferols A (1) and B (2), the new 4-hydroxyisoflavones, have been isolated from the dichloromethane sub-fraction of the methanolic extract of Caragana conferta along with 3',5'-dihydroxy, 7,4'-dimethoxyisoflavone (3), E-cinnamic acid (4), tetracosyl 3,4-dihydroxy-E-cinnamate (5), docosyl 3,4-dihydroxy-E-cinnamate (6)...

journal_title：Chemical & pharmaceutical bulletin

authors： Khan R,Malik A,Adhikari A,Qadir MI,Choudhary MI

更新日期：2009-04-01 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：:A series of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5HT3) receptor antagonistic activities by means of assays of 5-HT3 receptor binding and the ability to antagonize the von Bezold-Jarisch reflex in rats. Replacement of the 1,4-benzoxazine ring with a 1,4...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroita T,Marubayashi N,Sano M,Kanzaki K,Inaba K,Kawakita T

更新日期：1996-11-01 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：:Applicability of a previously published equation for calculating the solubility of solutes in supercritical carbon dioxide was extended to calculate the solubility in entrained supercritical carbon dioxide employing 42 experimental data sets collected from the literature. The accuracy of the proposed model was evaluat...

journal_title：Chemical & pharmaceutical bulletin

authors： Jouyban A,Khoubnasabjafari M,Chan HK

更新日期：2005-03-01 00:00:00

abstract：:In line with the recent globalization of the drug supply chain and promotion of the use of generic drugs worldwide, quality assurance is required for drugs globally. In particular, controlling impurities is one of the biggest areas of interest regarding pharmaceutical quality, and it is desirable that the latest scien...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuhama M,Saito R,Miyazaki S

更新日期：2020-01-01 00:00:00

abstract：:Effects of somatostatin on pepsinogen secretion was investigated in the rat in vivo and in vitro. In the perfused rat stomach, somatostatin inhibited secretagogue-induced acid secretion in dose-dependent manner. However, effects of somatostatin on secretagogue-induced pepsinogen secretion were obscure. To clarify the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tani S,Tanaka T

更新日期：1990-08-01 00:00:00

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

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

更新日期：2004-06-01 00:00:00

abstract：:An improved synthesis of the key intermediates (3 and 8) for the synthesis of beta-hydroxywybutines [[R-(R*,S*)]- and [S-(R*,R*)]-4], the most probable structures for the minor base from rat liver tRNA(Phe), has been achieved by the Wittig reaction between 1-benzyl-7-formylwye (1) and the phosphorane derived from (R)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Itaya T,Kanai T

更新日期：1998-08-01 00:00:00

abstract：:To investigate the effect of the hot water extract from Artemisia leaf (Artemisia princeps Panpanini) (AFE) on the proliferation of endothelial cells, the cells from bovine aorta were cultured for up to 96 h in the presence of 1, 5, 10 or 50 micrograms/ml AFE in RPMI1640 medium supplemented with 10% fetal bovine serum...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaji T,Kaga K,Miezi N,Ejiri N,Sakuragawa N

更新日期：1990-02-01 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：:A new fluorinated analog of vitamin D2, 24-epi-26,26,26,27,27,27-hexafluoro- 1 alpha,25-dihydroxyvitamin D2, was efficiently synthesized starting from (R)-4-isopropyl-3-propionyl-2- oxazolidinone with high stereochemical control. In all four physiological test systems, the fluorinate vitamin D2 analog was found to be ...

journal_title：Chemical & pharmaceutical bulletin

authors： Iseki K,Oishi S,Namba H,Taguchi T,Kobayashi Y

更新日期：1995-11-01 00:00:00

abstract：:Adipocyte fatty acid binding protein (A-FABP; FABP4), which is predominantly expressed in macrophages and adipose tissue, regulates fatty acid storage and lipolysis, and is also an important mediator of inflammation. Here, we report a synthesis of (14)C-labeled 2-[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yl...

journal_title：Chemical & pharmaceutical bulletin

authors： Okada T,Hiromura M,Otsuka M,Enomoto S,Miyachi H

更新日期：2012-01-01 00:00:00

abstract：:Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lo...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

更新日期：2016-01-01 00:00:00

abstract：:Detailed chemical studies on the cytotoxic fraction from the leaves of Dysoxylum cumingianum have resulted in the isolation of two new triterpene glucosides, cumingianosides P (18) and Q (19), with an apotirucallane-type skeleton. The structures of 18 and 19 were determined by spectral examinations, and by conversion ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujioka T,Sakurai A,Mihashi K,Kashiwada Y,Chen IS,Lee KH

更新日期：1997-01-01 00:00:00

abstract：:Five compounds have been isolated from the dried whole plants of Selaginella uncinata, two of them were new chromone glycosides, 5-hydroxy-2,6,8-trimethylchromone 7-O-beta-D-glucopyranoside (uncinoside A) and 5-acetoxyl-2,6,8-trimethylchromone 7-O-beta-D-glucopyranoside (uncinoside B). Their structures were elucidated...

journal_title：Chemical & pharmaceutical bulletin

authors： Ma LY,Ma SC,Wei F,Lin RC,But PP,Lee SH,Lee SF

更新日期：2003-11-01 00:00:00

abstract：:Diphenhydramine, a sedating antihistamine, is an agonist of human bitter taste receptor 14 (hTAS2R14). Diphenhydramine hydrochloride (DPH) was used as a model bitter medicine to evaluate whether the umami dipeptides (Glu-Glu and Asp-Asp) and their constituent amino acids (Glu, Asp) could suppress its bitterness intens...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuno T,Morimoto S,Nishikawa H,Haraguchi T,Kojima H,Tsujino H,Arisawa M,Yamashita T,Nishikawa J,Yoshida M,Habara M,Ikezaki H,Uchida T

更新日期：2020-01-01 00:00:00

abstract：:The synthesis and structure-activity relationships of a series of new azabicycloalkanes as 5-HT3 (serotonin-3) receptor antagonists are described. Our study on the azabicycloalkaneacetamide derivatives showed that 2,3-dihydroindole as the aromatic ring moiety afforded potent 5-HT3 receptor antagonist activity, as judg...

journal_title：Chemical & pharmaceutical bulletin

authors： Kato M,Ito K,Nishino S,Yamakuni H,Takasugi H

更新日期：1995-08-01 00:00:00

abstract：:The purpose of this study was to predict the stability of imipenem in a mixed infusion. The hydrolysis of imipenem in aqueous solution was found to be accelerated by pH, and by increasing concentrations of sodium bisulfite (SBS) and L-cysteine. Equations were derived for the degradation rate constants (k(obs)) of pH, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Takasu Y,Shimizu K,Asahara K,Uchida T

更新日期：2013-01-01 00:00:00

abstract：:Different green synthesis of alkyl esters of acyclovir (acyclovir prodrugs) is described. Hexanoic, decanoic, dodecanoic and tetradecanoic acyclovir esters were synthesized reacting acyclovir and the respective acid anhydride in dimethyl sulfoxide (DMSO), in solvents from renewable sources and without solvent (T=30 °C...

journal_title：Chemical & pharmaceutical bulletin

authors： de Regil-Hernández R,Martínez-Lagos F,Rodríguez-Bayón A,Sinisterra JV

更新日期：2011-01-01 00:00:00

abstract：:Simple one-pot methods for preparation of 2-oxazolines have been developed using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM). Treatment of a mixture of carboxylic acids and 2-haloethylammonium salts with DMT-MM in methanol followed by refluxing in the presence of KOH gives oxazolines. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Takechi Y,Kimura N,Tanaka H,Kunishima M

更新日期：2008-12-01 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