Development of an automated synthesis system for preparation of glucuronides using a solid-phase extraction column loaded with microsomes.

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

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

更新日期：1992-06-01 00:00:00

abstract：:A series of 1,2,3,4-tetrahydroisoquinoline derivatives containing the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton were prepared and evaluated for their in vitro binding affinities to muscarinic receptors and for antagonism of bradycardia in vivo. Among them, compound 3f had the highest affinity for ...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe T,Kinoyama I,Takizawa K,Hirano S,Shibanuma T

更新日期：1999-05-01 00:00:00

abstract：:A new cyclic tetrapeptide (1), along with known congeners (2, 3), was isolated from the fungus Phoma sp. derived from the giant jellyfish Nemopilema nomurai. The absolute configuration of 1 was determined using the modified Mosher's method and Marfey's method. Compound 1 displayed a weak suppressive effect on the prod...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim EL,Li JL,Xiao B,Hong J,Yoo ES,Yoon WD,Jung JH

更新日期：2012-01-01 00:00:00

abstract：:A new pentacyclic cucurbitane glucoside, named aoibaclyin (1) and a new triterpene (2) have been isolated from the EtOH extract of the fruits of Gymnopetalum integrifolium Kurz (Cucurbitaceae), together with three known compounds, bryoamaride (3), 25-O-acetylbryoamaride (4) and beta-sitosterol 3-O-beta-D-glucopyranosi...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekine T,Kurihara H,Waku M,Ikegami F,Ruangrungsi N

更新日期：2002-05-01 00:00:00

abstract：:The absorption of insulin (from porcine pancreas) from the rectum of rabbits after the administration of hollow-type suppositories containing insulin and five kinds of cyclodextrins (CyDs) was investigated. Three types of suppositories were employed: suppository I containing insulin (approximately 26 IU/mg) and variou...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe Y,Matsumoto Y,Seki M,Takase M,Matsumoto M

更新日期：1992-11-01 00:00:00

abstract：:Six new triterpenoid glycosides called julibrosides A1-A4, B1 and C1 were isolated from Albizziae Cortex, the dried stem bark of Albizzia julibrissin Durazz. Their structures were determined based on spectral and chemical evidence. Julibrosides B1 and C1 had new sapogenols, designated julibrogenin B and C, respectivel...

journal_title：Chemical & pharmaceutical bulletin

authors： Kinjo J,Araki K,Fukui K,Higuchi H,Ikeda T,Nohara T,Ida Y,Takemoto N,Miyakoshi M,Shoji J

更新日期：1992-12-01 00:00:00

abstract：:Two new friedelane-type triterpenes named 12alpha-hydroxyfriedelane-3,15-dione and 3beta-hydroxyfriedelan-25-al, together with six known compounds were isolated from the stems of Drypetes paxii Hutch. (Euphorbiaceae). Their structures were established on the basis of conventional 1 dimensional (1D) NMR methods, 2D shi...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiozem DD,Trinh-Van-Dufat H,Wansi JD,Mbazoa Djama C,Fannang VS,Seguin E,Tillequin F,Wandji J

更新日期：2009-10-01 00:00:00

abstract：:Two new cycloartane glycosides, named aquilegiosides K and L, have been isolated from the dried underground parts of Aquilegia vulgaris. Their structures were determined by two dimensional (2D) NMR spectroscopic analysis and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshimitsu H,Nishida M,Nohara T

更新日期：2008-11-01 00:00:00

abstract：:The bulbs of Habranthus brachyandrus (Amaryllidaceae) have been extensively analyzed for their chemical constituents, resulting in the isolation of eight flavan derivatives (1-8), four of which are new naturally occurring compounds; a new hydroxybutyric acid glucoside (9); three known phenolic compounds (10-12); and s...

journal_title：Chemical & pharmaceutical bulletin

authors： Jitsuno M,Yokosuka A,Sakagami H,Mimaki Y

更新日期：2009-10-01 00:00:00

abstract：:The effect of chromomycin A3 binding on the geometry of DNA duplex (plasmid pBR322) has been examined using topoisomerase I relaxation followed by gel electrophoresis. To determine the equilibrium constant of this drug-DNA binding-dissociation reaction in the same concentration range (ca. 10(-5) M) in the same buffer ...

journal_title：Chemical & pharmaceutical bulletin

authors： Utsuno K,Kojima K,Maeda Y,Tsuboi M

更新日期：1998-11-01 00:00:00

abstract：:Polycomb repressive complex 2 (PRC2) is an attractive drug target for anti-cancer treatment. Among the three core subunits (EZH2, EED and SUZ12) of PRC2, EZH2 is the catalytic subunit that methylates histone H3 lysine 27 (H3K27), while EED is the regulatory subunit. Besides the small-molecule inhibitors of EZH2, those...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhu K,Du D,Yang R,Tao H,Zhang H

更新日期：2020-01-01 00:00:00

abstract：:To estimate membrane potential in synaptosomes with the use of tetraphenylphosphonium (TPP+), an equation relating the amount of TPP+ accumulated in synaptosomes with membrane potential was derived from the following two assumptions. (1) TPP+ molecules were distributed into plasma membranes, mitochondria and cytosol o...

journal_title：Chemical & pharmaceutical bulletin

authors： Aiuchi T,Matsunaga M,Nakaya K,Nakamura Y

更新日期：1989-12-01 00:00:00

abstract：:Certain amide-containing anthraquinone, xanthone, and carbazole derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal carcinoma (NPC-TW01), lung carcinoma (NCI-H661), and leukemia (Jurkat). Among them, 2-(9,10...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen LC,Juang SH,Chang KM,Tzeng CC,Chen JJ,Chen IL,Wang TC

更新日期：2014-01-01 00:00:00

abstract：:The reaction of lauroyl isothiocyanate and 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile was used to synthesize the title compound 2. Compound 2 could serve as the main building block in the synthesis of many target heterocyclic systems. Various fused pyrimidines were synthesized in the reactions of compo...

journal_title：Chemical & pharmaceutical bulletin

authors： Hemdan MM,Abd El-Mawgoude HK

更新日期：2015-01-01 00:00:00

abstract：:The metabolic pathway of butylated hydroxytoluene (BHT) to the ring-oxygenated metabolites 2,6-di-tert-butylhydroquinone (BHQ) and 2,6-di-tert-butyl-p-benzoquinone (BBQ) was examined in rats. After intraperitoneal administration of 3,5-di-tert-butyl-4-hydroxybenzoic acid (BHT-acid), which had been regarded as one of t...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto K,Tajima K,Takemura M,Mizutani T

更新日期：1991-02-01 00:00:00

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

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

更新日期：1989-08-01 00:00:00

abstract：:A novel cytolytic factor, dolabellanin P, was purified to apparent homogeneity from the purple fluid of the sea hare, Dolabella auricularia. Purified dolabellanin P is a single polypeptide of 60 kDa. The amino acid composition and the N-terminus of the factor were also determined. This factor nonspecifically lysed all...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamazaki M,Tansho S,Kisugi J,Muramoto K,Kamiya H

更新日期：1989-08-01 00:00:00

abstract：:A model based on solubility parameters is proposed to predict the solubility curves of antihelmintic drugs at several temperatures, including aqueous and non-aqueous mixtures. The solubility of the drugs was measured in ethanol-water and ethanol-ethyl acetate mixtures at 15-35 degrees C (mebendazole) and at 25 degrees...

journal_title：Chemical & pharmaceutical bulletin

authors： Bustamante P,Muela S,Escalera B,Peña A

更新日期：2010-05-01 00:00:00

abstract：:Telmisartan (anti-hypertensive) is insoluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less (bioavailability 42%). In the present study an attempt has been made to prepare immediate release tablets of...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekar V,Chellan VR

更新日期：2008-04-01 00:00:00

abstract：:In the previous paper, we described a series of the 2-arylethenesulfonamide derivatives, a novel class of ETA-selective endothelin (ET) receptor antagonists, including the compounds 1a, b. Compound 1a showed excellent oral antagonistic activities and pharmacokinetic profiles, and the monopotassium salt of 1 (YM-598 mo...

journal_title：Chemical & pharmaceutical bulletin

authors： Harada H,Kazami J,Watanuki S,Tsuzuki R,Sudoh K,Fujimori A,Tokunaga T,Tanaka A,Tsukamoto S,Yanagisawa I

更新日期：2001-12-01 00:00:00

abstract：:4-(2-Pyridinylamino)-1,1,1-trifluoro-3-penten-2-ones 3, obtained from the reaction of commercially available 2-aminopyridine derivatives and 4-methoxy-1,1,1-trifluoro-3-penten-2-one 2, were converted to 6-(dimethylamino)-4-(2-pyridinylamino)-3,5-hexadien-2-ones 4 by treatment with dimethylformamide dimethyl acetal. Az...

journal_title：Chemical & pharmaceutical bulletin

authors： Cocco MT,Conglu C,Onnis V

更新日期：2001-06-01 00:00:00

abstract：:From the herb of Luffa acutangula ROXB. (Cucurbitaceae), seven oleanane-type triterpene saponins, acutosides A--G, were isolated and their structures were determined. Acutoside A is oleanolic acid 3-O-beta-D-glucopyranosyl-(1----2)-beta-D-glucopyranoside. Acutosides B, D, E, F and G have a common prosapogenin structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagao T,Tanaka R,Iwase Y,Hanazono H,Okabe H

更新日期：1991-03-01 00:00:00

abstract：:During a search for novel, orally-active inhibitors of upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1), we found a new series of 10H-pyrazino[2,3-b][1,4]benzothiazine derivatives to be potent ICAM-1 inhibitors. Of these compounds, N-[1-(10H-Pyrazino[2,3-b][1,4]benzothiazin-8-ylmet...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaneko T,Clark RS,Ohi N,Kawahara T,Akamatsu H,Ozaki F,Kamada A,Okano K,Yokohama H,Muramoto K,Ohkuro M,Takenaka O,Kobayashi S

更新日期：2002-07-01 00:00:00

abstract：:Investigation of an acetone extract of the leaves and twigs of Taxus sumatrana has resulted in the isolation of two new bicyclic taxoids, tasumatrols M (1), and N (2) and a new baccatin III derivative, tasumatrol O (3) together with the previous known 7-deacetylcanadensene (4) and 2alpha,7beta,13alpha-triacetoxy-5alph...

journal_title：Chemical & pharmaceutical bulletin

authors： Shen YC,Hsu SM,Lin YS,Cheng KC,Chien CT,Chou CH,Cheng YB

更新日期：2005-07-01 00:00:00

abstract：:Fibrinogen-related peptides, monomeric cyclic peptides through a disulfide bond [cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-NH2), cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-Gly-NH2), cyclo(H-Cys-Arg-Gly-Asp-Cys-NH2) and cyclo(H-Cys-Arg-Gly-Asp-Cys-Gly-NH2)], were prepared by the solid phase method with disulfide bond formation on the solid...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakiuchi M,Izuno Y,Maeda M,Ueda K,Fujiwara K,Kunitada S,Kawasaki K

更新日期：1996-05-01 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：:This paper discusses a process for making a novel granular detergent with an interspersion particle comprising an anionic surfactant and a polymeric polycarboxalate. This process contains three steps to develop the interspersion particles with anionic surfactant and polymeric ploycarboxalate. The first step was to for...

journal_title：Chemical & pharmaceutical bulletin

authors： Ebihara F,Watano S

更新日期：2003-06-01 00:00:00

abstract：:α,β-Unsaturated amides were incorporated as viable dipolarophiles in a catalytic asymmetric 1,3-dipolar cycloaddition of azomethine imines. The use of a 7-azaindoline auxiliary was essential to acquire sufficient reactivity with excellent diastereoselectivity, likely due to the chelating activation of the amide by the...

journal_title：Chemical & pharmaceutical bulletin

authors： Li Z,Kumagai N,Shibasaki M

更新日期：2020-01-01 00:00:00

abstract：:A novel method for thermodynamic stability studies of polymorphic drug substances has been developed. In order to estimate the transition temperature for an enantiotropic polymorphic pair, a formula for calculating the temperature at which the solubilities of each polymorph become equal has been derived with heat of s...

journal_title：Chemical & pharmaceutical bulletin

authors： Urakami K,Shono Y,Higashi A,Umemoto K,Godo M

更新日期：2002-02-01 00:00:00

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

authors： Yoshimatsu M,Hibino M

更新日期：2000-09-01 00:00:00