Ebenamariosides A-D: Triterpene Glucosides and Megastigmanes from the Leaves of Diospyros maritima.

abstract：:Solifenacin (Sol), an antimuscarinic agent has been widely used for the treatment of overactive bladder. Transdermal formulations can be administered without water as well as absorbed slowly into the blood over a long period of time. The aim of this study was to develop cream and tape formulations of Sol, and evaluate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Uchida S,Kashiwagura Y,Tanaka S,Matsui R,Namiki N

更新日期：2019-01-01 00:00:00

abstract：:A series of optically active substituted 1,2-dihydro-6-oxo-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids was prepared via optically active 2-methyl-4,5-difluoroindoline (10) and tested for antibacterial activities. Among them, (2S)-9-[(3R,1'S)-3-(1'-amino)ethyl-1-pyrrolidinyl]-8-fluoro-1,2-dihydro- 2- methyl-6-oxo-6H-...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsuji K,Tsubouchi H,Ishikawa H

更新日期：1995-10-01 00:00:00

abstract：:Four hypotensive peptides called elapherine-A, -B, -C and -D were isolated from the body of Elaphe climacophora after removal of the internal organs. Elapherine-A, which had the lowest molecular weight, exhibited a prolonged fall for 5 min in the blood pressure of spontaneously hypertensive rats, whereas elapherin-B, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsujibo H,Sato H,Taniguchi T,Kamatani Y,Kenny PT,Nomoto K,Inamori Y

更新日期：1990-04-01 00:00:00

abstract：:We investigated the chemical modifications of the nitroquinazoline derivative (1) through the replacement of the NH group at the C(4)-position with several N-alkyl groups to increase the lipophilicity at the C(4)-position. Among them, we found that the N-methyl analogue (5a) showed a 2-fold loss in the inhibitory acti...

journal_title：Chemical & pharmaceutical bulletin

authors： Tobe M,Isobe Y,Tomizawa H,Nagasaki T,Aoki M,Negishi T,Hayashi H

更新日期：2003-09-01 00:00:00

abstract：:Thirty-four extracts of crude drugs and medicinal plants have been screened for activity against Oncomelania nosophora, the intermediate host of the Japanese strain of Schistosoma japonicum. Strong molluscicidal activity was found in the MeOH extract of Anemarrhenae Rhizoma. Although timosaponin A-III, one of the main...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeda O,Tanaka S,Yamasaki K,Kohda H,Iwanaga Y,Tsuji M

更新日期：1989-04-01 00:00:00

abstract：:A calcium-binding protein, regucalcin, was isolated from rat liver cytosol. Rabbit-anti-regucalcin antiserum, which was raised against regucalcin conjugated by glutaraldehyde to bovine serum albumin, was applied to glutaraldehyde-fixed whole mounts and subsequently visualized using the peroxidase-antiperoxidase method...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Isogai M,Kato S,Mori S

更新日期：1991-06-01 00:00:00

abstract：:This study clearly demonstrates that clathrated water molecules can contribute to both chemical stabilization and destabilization of clathrates. The solid-state stabilities for two isomorphic clathrates of cephalosporin, cefazolin sodium and FK041, were investigated in terms of the effects of water content. The isomor...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimura H,Gato K,Kitamura S,Kitagawa T,Kohda S

更新日期：2002-06-01 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：:Using tissue engineering technique to repair cartilage damage caused by osteoarthritis is a promising strategy. However, the regenerated tissue usually is fibrous cartilage, which has poor mechanical characteristics compared to hyaline cartilage. Chondrocyte hypertrophy plays an important role in this process. Thus, i...

journal_title：Chemical & pharmaceutical bulletin

authors： Cao Z,Dou C,Dong S

更新日期：2017-01-01 00:00:00

abstract：:Three new steroidal glycosides, named solaviasides A, B, and C, have been isolated from the fruits of Solanum viarum DUNAL (syn. S. khasianum var. chatterjeeanum, Solanaceae), along with seven known ones. Their chemical structures were determined on the basis of spectroscopic data and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Kakiuchi T,Ebisawa H,Shiono Y,Nakamura T,Kai T,Ikeda T,Miyashita H,Yoshimitsu H,Nohara T

更新日期：2009-06-01 00:00:00

abstract：:Superoxide is involved in the pathogenesis of various diseases, such as inflammation, ischemia-reperfusion injury and carcinogenesis. Superoxide dismutases (SODs) catalyze the disproportionation reaction of superoxide to produce oxygen and hydrogen peroxide, and can protect living cells against the toxicity of free ra...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamura M,Urano Y,Kikuchi K,Higuchi T,Hirobe M,Nagano T

更新日期：2000-10-01 00:00:00

abstract：:An efficient one-pot step by step t-BuOK-mediated procedure for the synthesis of N-arylindoles has been developed in moderate to good yields. The protocol involves the consecutive deprotection of N-arylsulfonylindoles as latent indoles and subsequent S(N)Ar reactions with activated aryl halides. This tandem reaction a...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu H,Fan LL

更新日期：2009-03-01 00:00:00

abstract：:A powder solid dispersion system (SD) of indomethacin (IM) with crospovidone (CrosPVP) possesses good fluidity and can be used for tablet formulation. Tablets of SD can be prepared by direct compression and have adequate hardness and a small variation in weight. Forces during the tableting process were measured with a...

journal_title：Chemical & pharmaceutical bulletin

authors： Shibata Y,Fujii M,Okada H,Noda S,Kondoh M,Watanabe Y

更新日期：2005-07-01 00:00:00

abstract：:Four new lignans, 3',4'-O,O-demethylenehinokinin (1), chamalignolide (2), 8'beta-hydroxyhinokinin (3) and 7beta,8beta-epoxyzuonin A (4), as well as (-)-hinokinin (5), and (-)-zuonin A (6), were isolated from the heartwood of Chamaecyparis obtusa var. formosana. The structures of these lignans were unambiguously determ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chen CH,Lin YL

更新日期：2002-07-01 00:00:00

abstract：:New antitumor alkylglycerophospholipids, in which primarily the phosphocholine moiety of the platelet activating factor (PAF) molecule was modified, were synthesized from 1-alkyl-2-substituted glycerols by introducing polar head phosphoryl groups having methylene bridges of various lengths (from 2 to 14 carbons). They...

journal_title：Chemical & pharmaceutical bulletin

authors： Ukawa K,Imamiya E,Yamamoto H,Mizuno K,Tasaka A,Terashita Z,Okutani T,Nomura H,Kasukabe T,Hozumi M

更新日期：1989-05-01 00:00:00

abstract：:The disintegration kinetics of egg phosphatidylcholine small unilamellar liposomes in various bile salts (nine species) were investigated by monitoring turbidity changes with a stopped-flow apparatus. The pseudo-first-order rate constants obtained as a function of bile salt concentration (up to 25 mM) were analyzed ba...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagata M,Yotsuyanagi T,Ikeda K

更新日期：1990-05-01 00:00:00

abstract：:A full account is given of the first chemical synthesis of the antitumor antibiotic guanine 7-oxide (5) and its 9-substituted derivatives (24a--k and 26). Coupling of appropriate primary amines (17a--e, g--k) with phenacyl bromide (16) produced, after treatment with HCl, the corresponding N-substituted phenacylamine h...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawa K,Nishii M,Inagaki J,Nohara F,Saito T,Itaya T,Fujii T

更新日期：1992-02-01 00:00:00

abstract：:Mycobacterial cell walls have diverse adjuvant activities, and in particular, cell wall skeleton (CWS) of Mycobacterium bovis BCG has been expected as a drug for tumor immunotherapy. However, its molecular structure-biological activity relationship has not been fully elucidated despite more than 30 years of intensive ...

journal_title：Chemical & pharmaceutical bulletin

authors： Uenishi Y,Okada T,Okabe S,Sunagawa M

更新日期：2007-06-01 00:00:00

abstract：:We used near infrared (NIR) spectroscopy to evaluate the degree of mixing of blended dry syrup (DS) products whose particle sizes are not specified in the Revised 16th Edition of the Japanese Pharmacopoeia, and also evaluated the degree of mixing when powder products or fine granule products were added to DS products....

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto Y,Suzuki T,Matsumoto M,Ohtani M,Hayano S,Fukami T,Tomono K

更新日期：2012-01-01 00:00:00

abstract：:Eight dermorphin (DM) analogs extended at the C-terminus, based on the sequence of prepro-DM deduced from the cDNA, were synthesized by a simultaneous solid-phase method in which a pair of peptides was synthesized in a single vessel. Six peptides (three pairs) were obtained in satisfactory yields (17-37%). In the opio...

journal_title：Chemical & pharmaceutical bulletin

authors： Ambo A,Sasaki Y,Suzuki K

更新日期：1994-04-01 00:00:00

abstract：:Two new acylated flavonol glycosides, named amurenosides A and B, together with quercetin 3-(2,6-di-O-alpha-rhamnopyranosyl-beta-galactopyranoside), have been isolated from the whole plant of Vicia amurensis. Their structures were elucidated as quercetin 3-O-alpha-L-(3-feruloylrhamnopyranosyl)(1-->6)-[alpha-L-rhamnopy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kang SS,Chang YS,Kim JS

更新日期：2000-08-01 00:00:00

abstract：:A rapid tandem mass spectrometric (MS-MS) method for the quantification of Oxcarbazepine (OXB) in human plasma using imipramine as an internal standard (IS) has been developed and validated. Chromatographic separation was achieved isocratically on a C18 reversed-phase column within 3.0 min, using a mobile phase of ace...

journal_title：Chemical & pharmaceutical bulletin

authors： Srinubabu G,Ratnam BV,Rao AA,Rao MN

更新日期：2008-01-01 00:00:00

abstract：:Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we ...

journal_title：Chemical & pharmaceutical bulletin

authors： Dohi M,Momose W,Yamashita K,Hakomori T,Sato S,Noguchi S,Terada K

更新日期：2017-02-01 00:00:00

abstract：:Alkylidenemalonates were readily dimerized in the presence of SmI2 to give 2,3-disubstituted 1,1,4,4-butanetetracarboxylates as mixtures of meso and racemic isomers in moderate to good yields. The structure of the less polar isomer of tetraethyl 2,3-diphenyl-1,1,4,4-butanetetracarboxylate was determined by X-ray cryst...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita M,Okuyama K,Kawasaki I,Nakamura S,Nagamine R,Tsujita T,Ohta S

更新日期：2000-11-01 00:00:00

abstract：:Novel 9alpha and 9beta-hydroxy grayanotoxin II derivatives were prepared by photo-sensitized oxygenation of iso-grayanotoxin II and oxidation of grayanotoxin II tetraacetate with selenium dioxide respectively. The lethal dosage of 9alpha and 9beta-hydroxy grayanotoxin II were lower than that of grayanotoxin II. In add...

journal_title：Chemical & pharmaceutical bulletin

authors： Terai T,Osakabe K,Katai M,Sakaguchi K,Narama I,Matsuura T,Katakawa J,Tetsumi T

更新日期：2003-03-01 00:00:00

abstract：:A new series of 3-(5-3-methyl-5-[(3-methyl-7-5-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-1,3,4-thiadiazol-2-ylbenzo[b]furan-5-yl)methyl]benzo[b]furan-7-yl-1,3,4-thiadiazol-2-yl)-2-(aryl)-1,3-thiazolan-4-one 5a-j has been synthesized by the reaction of N2-[(E)-1-(4-methylphenyl)methylidene]-5-(3-methyl-5-[3-methyl-7-(5-[(E)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Reddy CS,Rao DC,Yakub V,Nagaraj A

更新日期：2010-06-01 00:00:00

abstract：:Analysis of the structural requirements of compound 1 (SR48968), a potent NK2 receptor antagonist, revealed that the 4-phenyl group of the piperidine is essential for binding with the NK2 receptor and occupies an equatorial position. Energy calculation of a variety of substituted 4-phenyl piperidines revealed that spi...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Fujii M,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 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：:The bitter and sweet forms of a plant species differing with alkaloid contents may provide a model system for investigation of alkaloid biosynthesis at a molecular level. The pattern and concentration of quinolizidine alkaloids were determined by capillary GC-MS in bitter and sweet plants of Lupinus angustifolius. Bit...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirai MY,Suzuki H,Yamazaki M,Saito K

更新日期：2000-10-01 00:00:00

abstract：:A quantitative structure property relationship (QSPR) study was performed to develop a model that relates the structures of 150 drug organic compounds to their aqueous solubility (log S(w)). Molecular descriptors derived solely from 3D structure were used to represent molecular structures. A subset of the calculated d...

journal_title：Chemical & pharmaceutical bulletin

authors： Ghasemi J,Saaidpour S

更新日期：2007-04-01 00:00:00