Reactions of oxalyl chloride with 1,2-cycloalkanediols in the presence of triethylamine.

abstract：:A series of phthalazine and 1,2,3-benzotriazine derivatives which have heterocyclylpiperidino groups was synthesized and tested for cardiotonic activity in anesthetized dogs. Several 6,7-dimethoxyphthalazine derivatives showed relatively potent cardiotonic activity comparable to that of amrinone. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomoto Y,Obase H,Takai H,Teranishi M,Nakamura J,Kubo K

更新日期：1990-08-01 00:00:00

abstract：:Oligonucleotides containing a dG cluster, d(TmGnTm), are models of single-stranded parts of telomeric deoxyribonucleic acid and substitutes for poly(dG). Electrophoretic and spectroscopic analyses of the oligomers indicate that the oligomers can form two alternative structures, single- and quadruple-stranded helices, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Shida T,Yokoyama K,Tamai S,Sekiguchi J

更新日期：1991-09-01 00:00:00

abstract：:Novel hybrid L-ascorbic acid (vitamin C) derivatives with other biologically active substances, 5-hydroxy-2-hydroxymethyl-beta-pyrone (kojic acid) and alpha-tocopherol (vitamin E), linked at the C-2 or C-3 hydroxyl group were synthesized, and their thermal stability and inhibitory effects on tyrosinase activity, activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morisaki K,Ozaki S

更新日期：1996-09-01 00:00:00

abstract：:Italian canned tomatoes contain the tomato glycosides esculeosides B-1 (1, 0.0052%) and B-2 (2, 0.0068%) without esculeoside A. Herein, the structure of esculeoside B-1 (1) is characterized to be 3-O-β-lycotetraosyl (5S,22R,23S,25S)-22,26-epimino-16β,23-epoxy-3β,23,27-trihydroxycholestane 27-O-β-D-glucopyranoside. We ...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Fujiwara Y,Ikeda T,Ono M,Murakami K,Zhou JR,Yokomizo K,Nohara T

更新日期：2013-01-01 00:00:00

abstract：:A novel fucan sulfate (Hor-1) was isolated from the hot water extract of an edible brown alga, Sargassum horneri (Turner) C. Agardh. The fucan sulfate was revealed to have sugar linkage types, sulfate content and uronic acid content different from those of sodium hornan (Na-HOR), another fucan sulfate isolated from th...

journal_title：Chemical & pharmaceutical bulletin

authors： Preeprame S,Hayashi K,Lee JB,Sankawa U,Hayashi T

更新日期：2001-04-01 00:00:00

abstract：:Eight new guaipyridine sesquiterpene alkaloids, rupestines F-M (1-8) were isolated from the leaves of Artemisia rupestris and their structures were elucidated on the basis of 2D-NMR data. The absolute configurations of 1-8 have been assigned by comparison of their experimental and calculated circular dichroism (CD) sp...

journal_title：Chemical & pharmaceutical bulletin

authors： He F,Nugroho AE,Wong CP,Hirasawa Y,Shirota O,Morita H,Aisa HA

更新日期：2012-01-01 00:00:00

abstract：:Numerical methods to predict the solubility of anthracene in mixed solvents have been proposed. A minimum number of 3 solubility data points in sub-binary solvents has been employed to calculate the solvent-solute interaction terms of a well established colsolvency model, i.e. the combined nearly ideal binary solvent/...

journal_title：Chemical & pharmaceutical bulletin

authors： Jouyban A,Khoubnasabjafari M,Chan HK,Clark BJ,Acree WE Jr

更新日期：2002-01-01 00:00:00

abstract：:Three new oleanane-type saponins, giganteosides L (1), M (2) and N (3) along with eight known ones were isolated from the roots of Cephalaria gigantea. Their structures were established as 3-O-[beta-D-galactopyranosyl-(1-->2)-beta-D-glucuronopyranosyl]-28-O-[beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl]-oleanol...

journal_title：Chemical & pharmaceutical bulletin

authors： Tabatadze N,Elias R,Faure R,Gerkens P,De Pauw-Gillet MC,Kemertelidze E,Chea A,Ollivier E

更新日期：2007-01-01 00:00:00

abstract：:Several benzimidazole derivatives having electron-withdrawing or -donating substituent(s) at the benzene moiety were used as models of the imidazole moiety of purine bases and their nitration with nitrogen dioxide and ozone (so-called Kyodai nitration) were examined. Products were extracted from the reaction mixture w...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaiya T,Nakamura K,Tanaka M,Miyata N,Kohda K

更新日期：2004-05-01 00:00:00

abstract：:Orally disintegrating tablets (ODTs), which are administered without water, are beneficial for elderly patients and patients with dysphagia. Masking the unpleasant taste of a drug is an important factor associated with adherence of patients consuming ODTs. We prepared cocoa powder-containing ODTs of bitter-tasting reb...

journal_title：Chemical & pharmaceutical bulletin

authors： Takano H,Uchida S,Kashiwagura Y,Tanaka S,Hakamata A,Odagiri K,Inui N,Watanabe H,Namiki N

更新日期：2019-01-01 00:00:00

abstract：:This study demonstrates the structure-activity relationship of Col-003, a potent collagen-heat-shock protein 47 (Hsp47) interaction inhibitor. Col-003 analogues were successfully synthesized by Pd(0)-catalyzed cross-coupling reactions of 5-bromosalicylaldehyde derivatives with alkyl-metal species, and the inhibitory a...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Saito M,Ito S,Ogawa K,Goshima N,Nagata K,Doi T

更新日期：2020-03-01 00:00:00

abstract：:The purpose of this study was to predict the stability of octreotide in a mixed infusion containing sodium bisulfite (SBS). In aqueous solution the hydrolysis of octreotide was found to be accelerated by pH, and by increasing concentrations of SBS. Equations for the degradation rate constants (kobs) of pH and SBS were...

journal_title：Chemical & pharmaceutical bulletin

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

更新日期：2014-01-01 00:00:00

abstract：:Fe2+-dependent lipid peroxidation in phosphatidylcholine (PC) liposomes, assessed by thiobarbituric acid-reactive substances (TBARS) production, was stimulated in the presence of Fe3+ in a concentration-dependent manner. The rates of nitroblue tetrazolium (NBT) reduction and Fe2+ oxidation (Fe2+ disappearance and Fe3+...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohyashiki T,Kadoya A,Kushida K

更新日期：2002-02-01 00:00:00

abstract：:In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have...

journal_title：Chemical & pharmaceutical bulletin

authors： Yi W,Cao R,Chen Z,Yu L,Wen H,Yan Q,Ma L,Song H

更新日期：2010-05-01 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：:A new spiroketallactone, epi-danshenspiroketallactone A (1) and a new C18-norditerpenoid, normiltioane (2) along with 21 known compounds, were isolated from cell cultures of Salvia miltiorrhiza. Their structures were elucidated on the basis of extensive spectroscopic analyses. In the in vitro assays, the compounds 9-1...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang DW,Liu X,Xie D,Chen R,Tao XY,Zou JH,Dai J

更新日期：2013-01-01 00:00:00

abstract：:Two novel triterpenoid saponins, ardisicrenoside C (1) [3 beta-O-(alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->4)- [beta-D-glucopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)-16 alpha, 28-dihydroxy-olean-12-en-30-oic acid 30-O-beta-D-glucopyranosyl ester] and ardisicrenoside D (2) [3 beta-O-(beta-D-xylopyr...

journal_title：Chemical & pharmaceutical bulletin

authors： Jia Z,Koike K,Nikaido T,Ohmoto T,Ni M

更新日期：1994-11-01 00:00:00

abstract：:We designed a single unit type controlled release tablet containing nateglinide to decrease both postprandial blood glucose level (PBG) and fasting blood glucose level (FBG) in normal beagle dogs. The tablet contains 60 mg of nateglinide in an immediate release portion, and 90 mg of nateglinide in a controlled release...

journal_title：Chemical & pharmaceutical bulletin

authors： Makino C,Sakai H,Yabuki A

更新日期：2010-09-01 00:00:00

abstract：:Synthesis and pharmacological evaluation of novel thienopyridazinones and related compounds are described. A thiophene ring was found to be able to replace the benzene ring of a phthalazinone without loss of biological activities. This observation supports our hypothesis that the benzene ring plays an important role i...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Maruyama N,Koga T,Kamei K,Akima M,Kuroki T,Hamana M,Ohi N

更新日期：1995-02-01 00:00:00

abstract：:Herein we report the development of novel, potent and non-peptide luteinizing hormone releasing hormone (LHRH) antagonists. The optimization towards derivatives free from mechanism-based CYP3A4 inhibition is described. The identification of a main metabolite guided us towards structural modifications of the benzyl moi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hashimoto K,Kataoka M,Tatsuta M,Yasoshima K,Yamamoto M,Yura T,Yamamoto N,Urbahns K,Gupta JB,Li Y

更新日期：2005-10-01 00:00:00

abstract：:Two new monodesmosidic triterpene saponins were isolated from the roots of Gypsophila oldhamiana (Caryophyllaceae). Their structures were elucidated on the basis of spectral data to be quillaic acid, alpha-L-arabinopyranosyl-(1-->4)-alpha-L-arabinopyranosyl-(1-->3)-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-...

journal_title：Chemical & pharmaceutical bulletin

authors： Luo JG,Kong LY,Takaya Y,Niwa M

更新日期：2006-08-01 00:00:00

abstract：:During the search for new antitrypanosomal drug leads, four antitrypanosomal compounds, of three depsipeptides and one nortriterpenoid, were isolated from cultures of the mutant strain IU-3 of the insect pathogenic fungus Ophiocordyceps coccidiicola NBRC 100683. Their structures were identified by the analysis of high...

journal_title：Chemical & pharmaceutical bulletin

authors： Ganaha M,Yoshii K,Ōtsuki Y,Iguchi M,Okamoto Y,Iseki K,Ban S,Ishiyama A,Hokari R,Iwatsuki M,Otoguro K,Ōmura S,Hashimoto T,Noji M,Umeyama A

更新日期：2016-01-01 00:00:00

abstract：:Treatment composed of a gastric mucoadhesive antibiotic with slow release drug delivery is expected to be effective for the eradication of Helicobacter pylori (H. pylori). In this study, we evaluated the slow release property of the tetracycline-sucralfate acidic complex. Tetracycline was the antibiotic selected becau...

journal_title：Chemical & pharmaceutical bulletin

authors： Higo S,Takeuchi H,Yamamoto H,Hino T,Kawashima Y

更新日期：2008-10-01 00:00:00

abstract：:Water-soluble porphyrins containing four platinum(II) complexes per molecule, [5alpha,10beta,15alpha,20beta-tetrakis(2-trans-(alpha,beta,alpha,beta-trans-Pt) and cis-(alpha,beta,alpha,beta-cis-Pt) [PtCl(NH(3))(2)]N-2-aminophenylporphyrin)], were synthesized and characterized. The binding of synthetic nucleotide polyme...

journal_title：Chemical & pharmaceutical bulletin

authors： Munakata H,Imai H,Nakagawa S,Osada A,Uemori Y

更新日期：2003-05-01 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：:A new oleanan-type triterpene and three new cincholic acid glycosides were isolated from Peruvian "Una de Gato" (Cat's claw, plant of origin: Uncaria tomentosa), a traditional herbal medicine in Peru. Their structures were determined by spectroscopic analysis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima M,Hashimoto K,Sandoval M,Aimi N,Takayama H

更新日期：2004-10-01 00:00:00

abstract：:Biodegradable pasty-type copolyesters with a relatively low molecular weight of 4500 were synthesized by direct copolycondensation of epsilon-caprolactone (CL) and delta-valerolactone (VL) in the absence of catalysts to evaluate in vivo capabilities of the polymer for implantable controlled release devices in drug del...

journal_title：Chemical & pharmaceutical bulletin

authors： Imasaka K,Yoshida M,Fukuzaki H,Asano M,Kumakura M,Mashimo T,Yamanaka H,Nagai T

更新日期：1991-08-01 00:00:00

abstract：:Several E-ring-modified analogues of (RS)-camptothecin were synthesized by total synthesis via Friedländer condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camp...

journal_title：Chemical & pharmaceutical bulletin

authors： Ejima A,Terasawa H,Sugimori M,Ohsuki S,Matsumoto K,Kawato Y,Yasuoka M,Tagawa H

更新日期：1992-03-01 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：: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