Inhibition of adenosine 3',5'-cyclic monophosphate phosphodiesterase by flavonoids from licorice roots and 4-arylcoumarins.

abstract：:A new neolignan, (7R,8R)-5-O-demethylbilagrewin (1), together with four known lignans (2-5), were isolated from the heartwood of Santalum album (Santalaceae). The structure of 1 was determined by analysis of extensive spectroscopic data. The isolated compounds and derivatives were evaluated for their cytotoxic activit...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuo Y,Mimaki Y

更新日期：2010-04-01 00:00:00

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

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

abstract：:Anhydrous theophylline was prepared by heating theophylline monohydrate at temperatures between 60 degrees C and 140 degrees C. The effects of dehydration temperatures on the moisture absorption and dissolution behavior of anhydrous theophylline were investigated in this study. The hydration rate of anhydrous theophyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2001-12-01 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：:In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-(spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Kakefuda A,Nagaoka H,Yamamoto O,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:Novel sialosyl donors, 4-pentenoic acid ester of N-acetylneuraminic acids (Neu5Ac) and 4-pentenyl glycoside of Neu5Ac were successfully prepared from the corresponding per-O-acetylated 2-hydroxy and 2-chloro derivatives of Neu5Ac, respectively and applied to the synthesis of O-sialosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda K,Fukuyo J,Sato K,Sato M

更新日期：2005-11-01 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：:We describe here (2+2) cycloaddition reaction of alkyl enol ethers with acrylates catalyzed by triethylsilyl triflic imide (Et3SiNTf2), which was in situ generated from triethylsilane and triflic imide. The reaction efficiently provides substituted cyclobutanes bearing alkoxy function in a stereoselective manner. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takasu K,Miyakawa Y,Ihara M,Tokuyama H

更新日期：2008-08-01 00:00:00

abstract：:Doxazosin mesylate (DXM) sustained release pellets were prepared by an extrusion-spheronization and fluid-bed coating technique. The core pellets containing DXM were prepared by extrusion-spheronization technique, and coated by a fluid-bed coater to control the release of DXM. The factors affecting to properties of pe...

journal_title：Chemical & pharmaceutical bulletin

authors： Ha JM,Kim JY,Oh TO,Rhee YS,Chi SC,Kuk H,Park CW,Park ES

更新日期：2013-01-01 00:00:00

abstract：:Ginsenoside Rb1 is an important saponin of ginseng(s); however, Rb1, with 3-O- and 20-O-sugar moieties, has low bioavailability. Here, we report the derivatization of ginsenoside Rb1 to completely generate six types of highly bioactive minor ginsenoside Rg3 and its derivatives by FeCl3 catalysis, the reaction conditio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yu H,Wang Y,Liu C,Yang J,Xu L,Li G,Song J,Jin F

更新日期：2018-01-01 00:00:00

abstract：:In our series of studies on potassium channel openers, several thienylcyanoguanidine derivatives were synthesized and evaluated for smooth muscle relaxation activity in vitro. Among the newly synthesized compounds, N-cyano-N'-(5-cyano-3-thienyl)-N"-tert-pentylguanidine (4b) and N-(5-bromo-3-thienyl)-N'-cyano-N"-tert-p...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshiizumi K,Ikeda S,Nishimura N,Yoshino K

更新日期：1997-12-01 00:00:00

abstract：:Sixteen derivatives of 1-(beta-D-arabinofuranosyl)-2-thiocytosine (araSC), including five 5'-esters, three 3'-esters, five N4-amides and three 5'-phosphodiesters, were synthesized and their reactivity to mouse tissue homogenates, including plasma, liver and intestine, and antitumor activity in mice bearing P388 cells ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawaguchi T,Ichikawa T,Hasegawa T,Saneyoshi M,Wakayama T,Kato H,Yukita A,Nagata T

更新日期：2000-04-01 00:00:00

abstract：:Possible utility of hydroxyalkylated beta-cyclodextrin (beta-CyD) derivatives as parenteral drug carriers was investigated, using nimodipine, a dihydropyridine derivative with calcium antagonistic action, as a model drug. The aqueous solubility of nimodipine increased linearly with increase in the concentration of hyd...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida A,Yamamoto M,Itoh T,Irie T,Hirayama F,Uekama K

更新日期：1990-01-01 00:00:00

abstract：:A new polyhydroxy sterol ester, (25S)-5alpha-cholestane-3beta,6alpha,7alpha,8,15alpha,16beta-hexahydroxyl-26-O-14'Z-eicosenoate (1), together with seven known steroid derivatives (2-8), were isolated from the EtOH extract of the whole body of China Sea starfish Asterina pectinifera. The structure of 1 was determined b...

journal_title：Chemical & pharmaceutical bulletin

authors： Peng Y,Zheng J,Huang R,Wang Y,Xu T,Zhou X,Liu Q,Zeng F,Ju H,Yang X,Liu Y

更新日期：2010-06-01 00:00:00

abstract：:Two new acetylenic glucosides, 4',6'-acetonide-8Z-decaene-4,6-diyne-1-O-beta-D-glucopyranoside named carthamoside A(1) (1) and 4,6-decadiyne-1-O-beta-D-glucopyranoside named carthamoside A(2) (2), along with one known acetylenic glucoside, 8Z-decaene-4,6-diyne-1-O-beta-D-glucopyranoside (3), have been isolated from th...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou YZ,Ma HY,Chen H,Qiao L,Yao Y,Cao JQ,Pei YH

更新日期：2006-10-01 00:00:00

abstract：:The synthesis and biological evaluation of [2-Valine-A] insulin ([Val2-A]insulin) is reported. In this insulin, the isoleucine residue in position A2, invariant in the majority of mammalian insulins, is substituted by valine. The same substitution, along with four others, occurs naturally in the insulin produced by th...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohta N,Burke GT,Katsoyannis PG

更新日期：1989-03-01 00:00:00

abstract：:The purpose of the present study was to determine the thermodynamic stability orders of co-crystals by co-crystal former (CCF) exchange reactions. Caffeine (CA) was employed as a model drug. The CCF exchange reaction was performed by liquid-assisted grinding using ethanol. When oxalic acid (OX) was added to CA-citric ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mukaida M,Sugano K,Terada K

更新日期：2015-01-01 00:00:00

abstract：:A new monomethylated ganglioside, DSG-A (3), was obtained, together with four known gangliosides, compounds (1, 2, 4, 5), from the lipid fraction of the chloroform/methanol extract of the ovary of the sea urchin Diadema setosum. The structures of the new ganglioside was determined on the basis of chemical and spectros...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada K,Tanabe K,Miyamoto T,Kusumoto T,Inagaki M,Higuchi R

更新日期：2008-05-01 00:00:00

abstract：:The mechanism of the electrochemical oxidation of 2,5-dihydroxybenzoic acid and 3,4-dihydroxybenzaldehyde in the presence of 3-hydroxy-1H-phenalene-1-one as a nucleophile has been studied in water/acetonitrile (80/20 v/v) solution using cyclic voltammetry and controlled-potential coulometry methods. The results indica...

journal_title：Chemical & pharmaceutical bulletin

authors： Nematollahi D,Amani A

更新日期：2008-04-01 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：:From the bark of Cryptomeria japonica were isolated sugikurojins I (1) and J (2), and an abietane derivative (3) was obtained for the first time as a natural product. These structures were elucidated primarily through extensive NMR experiments. Sugikurojin I (1) has a unique skeleton incorporating an abietane diterpen...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa K,Suzuki K,Umeyama A,Arihara S

更新日期：2006-04-01 00:00:00

abstract：:We studied the hydrolysis of a neuropeptide kyotorphin (L-Tyr-L-Arg) by an enkephalin-degrading aminopeptidase purified from cytosol of rat brain in vitro. The purified enzyme was homogeneous as judged by sodium dodecyl sulfate (SDS)-polyacrylamide gel electrophoresis (PAGE), gel filtration and isoelectric focusing. T...

journal_title：Chemical & pharmaceutical bulletin

authors： Akasaki K,Tsuji H

更新日期：1991-07-01 00:00:00

abstract：:When 8-bromoadenosine was incubated with cysteine at pH 7.2 and 37°C, an exclusive product was generated. This product was identified as a cysteine substitution derivative of adenosine at the 8 position, 8-S-L-cysteinyladenosine. The reaction accelerated as pH increased from mildly acidic to basic conditions. The isol...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Ogishi A,Shinohara T,Suito S

更新日期：2018-01-01 00:00:00

abstract：:A series of N-(trifluoromethyl-2-pyridinyl)alkane- and arenesulfonamides 2-5 have been synthesized by the substitution reaction of 2-chloro(trifluoromethyl)pyridines 6 with alkane- and arenesulfonamides 7. Their inhibitory activities against secretory phospholipase A₂ of porcine pancreas were examined and the analog N...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakayama H,Morita Y,Kimura H,Ishihara K,Akiba S,Uenishi J

更新日期：2011-01-01 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：:From the leaves of Cananga odorata var. odorata, three relatively large molecules, namely two aryl naphthalene lignan diesters of canangafruticoside A and one cyclobutane lignan diester of canangafruticoside A, were isolated along with four known compounds. The structures of the new compounds were elucidated based on ...

journal_title：Chemical & pharmaceutical bulletin

authors： Katsui H,Sugimoto S,Matsunami K,Otsuka H,Lhieochaiphant S

更新日期：2017-01-01 00:00:00

abstract：:The objective of this investigation was to clarify the influence of water-soluble polymers on the dissolution behavior of nifedipine from solid dispersions with combined carriers. All the solid dispersions of nifedipine were prepared by the fusion method using nicotinamide and 4 different water-soluble polymers, hydro...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki H,Sunada H

更新日期：1998-03-01 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：:Prolyl endopeptidase (PEP, EC 3.4.21.26) is an enzyme playing a role in the metabolism of proline-containing neuropeptides which have been suggested to be involved in learning and memory processes. In screening for PEP inhibitors from fourteen traditional Kampo formulas, we found that Tokaku-joki-to shows a significan...

journal_title：Chemical & pharmaceutical bulletin

authors： Fan W,Tezuka Y,Kadota S

更新日期：2000-07-01 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