Uncinoside A and B, two new antiviral chromone glycosides from Selaginella uncinata.

abstract：:Manidipine dihydrochloride or benidipine hydrochloride will change to hydrate form in part, when differential scanning calorimetric (DSC) measurement is carried out together with lactose monohydrate. This interaction was accelerated by compressing their mixture. It can be suggested that the interaction may cause by th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hosaka S,Sato M,Ozawa Y,Hamada C,Takahashi Y,Kitamori N

更新日期：2005-05-01 00:00:00

abstract：:Infection with Helicobacter pylori (H. pylori) plays an important role in the pathogenesis of gastritis, peptic ulcer and gastric cancer, and the 13C-urea breath test (13C-UBT) is a convenient and non-invasive method for the detection of H. pylori in the stomach. We have examined the sensitivity, specificity and accur...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajiwara M,Iida K,Takatori K,Taniguchi Y,Kimura K

更新日期：1997-04-01 00:00:00

abstract：:The purpose of this study was to develop and test a novel and simple method for evaluating the disintegration time of rapidly disintegrating tablets (RDTs) in vitro, since the conventional disintegration test described in the pharmacopoeia produces poor results due to the difference of its environmental conditions fro...

journal_title：Chemical & pharmaceutical bulletin

authors： Hoashi Y,Tozuka Y,Takeuchi H

更新日期：2013-01-01 00:00:00

abstract：:Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developed a synthesis based on the photocyclization of tertiary ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aragon PJ,Yapi AD,Pinguet F,Chezal JM,Teulade JC,Blache Y

更新日期：2007-09-01 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：:A simple method to synthesize (+/-)-2-O-(4-coumaroyl)-3-(4-hydroxyphenyl)lactic acid (1), a key intermediate in rosmarinic acid biosynthesis in higher plant cells, was established by condensation of protected 4-coumaric acid and (+/-)-3-(4-hydroxyphenyl)lactic acid followed by deprotection. A stable supply of 1 thus a...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuno M,Nagatsu A,Ogihara Y,Mizukami H

更新日期：2001-12-01 00:00:00

abstract：:2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor γ (PPARγ) and PPARα agonist activities and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otake K,Azukizawa S,Takahashi K,Fukui M,Shibabayashi M,Kamemoto H,Kasai M,Shirahase H

更新日期：2011-01-01 00:00:00

abstract：:The title compound, PNU-97018 [systemic name: 2-butyl-3,6,7,8,9,11-hexahydro-6,9-dimethyl-3-([2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl)-6,9-ethano-4H-imidazo[4,5-d]-pyridazino[1,2-a]pyridazin-4-one] is a newly developed angiotensin II receptor antagonist. The compound and its methanolate and ethanolate were ch...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishii H,Yamaguchi K,Seki H,Sakamoto S,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2002-08-01 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：:A novel series of 2-acyl-3-carboxyl-tetrahydroisoquinoline derivatives were synthesized and biologically evaluated. Among them, (S)-2-{(E)-3-furan-2-ylacryloyl}-7-[(2E,4E)-5-(2,4,6-trifluorophenyl)penta-2,4-dienyloxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (compound 17u) was identified as a potent protein ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Morishita K,Shoji Y,Fukui M,Ito Y,Kitao T,Ozawa SI,Hirono S,Shirahase H

更新日期：2018-01-01 00:00:00

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

authors： Dodo K,Minato T,Hashimoto Y

更新日期：2009-02-01 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：:In order to confirm the proposed structures of two metabolites 3 and 4 of the gastroprokinetic agent mosapride [4-amino-5-chloro-2-ethoxy-N-([4-(4-fluorobenzyl)-2-morpholinyl] methyl)benzamide, 2], the compounds were synthesized and their biological activity was examined. The structures of the metabolites were confirm...

journal_title：Chemical & pharmaceutical bulletin

authors： Kato S,Morie T,Yoshida N

更新日期：1995-04-01 00:00:00

abstract：:The aim of this study was to search for a novel choline acetyltransferase (ChAT) activator from plants traditionally grown in Korea. An ethanol extract from Chaenomeles sinensis Koehne showed the highest ChAT-activating effect in vitro in an assay that used human neuroblastoma cells and [(14)C]acetyl-CoA. The active c...

journal_title：Chemical & pharmaceutical bulletin

authors： Kwon YK,Choi SJ,Kim CR,Kim JK,Kim HK,Choi JH,Song SW,Kim CJ,Park GG,Park CS,Shin DH

更新日期：2015-01-01 00:00:00

abstract：:We developed new intravenous sedative-hypnotic compounds with the isoindolin-1-one skeleton focusing on the water-soluble property and in vivo safety. We synthesized approximately 170 derivatives and evaluated their hypnotic effects by intravenous administration of the compounds to mice. A series of the 2-phenyl-3-[2-...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanamitsu N,Osaki T,Itsuji Y,Yoshimura M,Tsujimoto H,Soga M

更新日期：2007-12-01 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 competitive inclusion complexations in the ternary phenacetin/competitors/beta-cyclodextrin (beta-CyD) systems were investigated by the solubility method, where m-bromobenzoic acid (m-BBA) and o-toluic acid (o-TA) were used as competitors. The solubility changes of the drug and competitors as a function of beta-Cy...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono N,Hirayama F,Arima H,Uekama K

更新日期：2001-01-01 00:00:00

abstract：:Regioselectivity in N-acetylation of nitro-0-phenylenediamine, a widely used hair dye component, by rat liver cytosolic N-acetyltransferases was studied in relation to its substituent effects on enzymatic N-acetylation of mono-substituted anilines. Nitro-p-phenylenediamine was acetylated specifically at the N4-positio...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakao M,Goto Y,Matsuki Y,Hiratsuka A,Watabe T

更新日期：1990-09-01 00:00:00

abstract：:A gas chromatography-selected ion monitoring procedure with chemical ionization is described for the determination of bromovalerylurea (BVU) in human plasma. BVU was extracted with ether after addition of 2-bromo-2-methylpropylurea as an internal standard. The lower limit of BVU quantification by this method was 2 ng/...

journal_title：Chemical & pharmaceutical bulletin

authors： Kokatsu J,Yomoda R,Suwa T

更新日期：1992-06-01 00:00:00

abstract：:A series of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6,7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishikawa H,Tabusa F,Miyamoto H,Kano M,Ueda H,Tamaoka H,Nakagawa K

更新日期：1989-08-01 00:00:00

abstract：:Freshwater cyanobacteria produce lethal toxins such as microcystins and anatoxins. During the purification of microcystins in bloom samples we found that a toxic cyanobacterium produced not only microcystins but also other types-peptides in early 1990. Since then we have isolated approximately thirty peptides from fre...

journal_title：Chemical & pharmaceutical bulletin

authors： Harada K

更新日期：2004-08-01 00:00:00

abstract：:Stomatitis induced by radiation therapy or cancer chemotherapy is a factor in sleep disorders and/or eating disorders, markedly decreasing patient quality of life. In recent years, disintegrating oral films that are easy to handle have been developed; therefore, we focused on the formulation of these films. We prepare...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawano Y,Sasatsu M,Mizutani A,Hirose K,Hanawa T,Onishi H

更新日期：2016-06-01 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：:A series of 2-alkylamino-5- or 6-aralkyl-substituted benzazoles were synthesized and tested for histamine H2-receptor antagonist and anti-stress ulcer activities. These new compounds showed little or no histamine H2-receptor antagonist activity in contrast to imidazo[1,2-a]pyridine analogues (I). On antiulcer assay, h...

journal_title：Chemical & pharmaceutical bulletin

authors： Katsura Y,Inoue Y,Tomoi M,Takasugi H

更新日期：1992-08-01 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：:Melt pelletization of lactose 450 M was carried out in an 8-l high shear mixer using PEG 3000 as the meltable binder. The pore size and size distribution of the melt pellets were determined using mercury intrusion porosimetry. The pore size distribution of melt pellets was found to be bimodal. With a higher binder con...

journal_title：Chemical & pharmaceutical bulletin

authors： Wong TW,Chan LW,Heng PW

更新日期：2000-11-01 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 discovery of a novel class of state-dependent voltage-gated sodium channel (NaV)1.7 inhibitors is described. By the modification of amide or urethane bond in NaV1.7 blocker III, structure-activity relationship studies that led to the identification of novel NaV1.7 inhibitor 2i (DS01171986) were performed. Compound...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Kobayashi H,Suzuki S,Shibuya S,Kimoto H,Domon Y,Kubota K,Kitano Y,Yokoyama T,Shimizugawa A,Koishi R,Fujiwara C,Asano D,Shinozuka T

更新日期：2020-01-01 00:00:00

abstract：:Asymmetric total synthesis of benzene analogues of galbonolide, a 14-membered antifungal macrolide, possessing a benzene ring instead of a conjugated diene structure, was achieved starting from chiral 1-aryl-1-propanol obtained by enzyme-catalyzed kinetic resolution with high enantioselectivity. Representatively, a me...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakoh H,Sakuraba S,Sugimoto Y,Imamura H,Jona H,Yamada K,Bamba-Nagano R,Hashizume T,Morishima H

更新日期：2004-01-01 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