Synthesis and biological activities of metabolites of mosapride, a new gastroprokinetic agent.

abstract：:2,8-Dimethyl-1-oxa-8-azaspiro[4,5]decan-3-one (17), designed by incorporating the tetrahydrofuran ring moiety of muscarone into an 8-azaspiro[4,5]decane skeleton, and related 1-oxa-8-azaspiro[4.5]decanes were synthesized and assessed as M1 muscarinic agonists for the symptomatic treatment of dementia of Alzheimer's ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsukamoto S,Fujii M,Yasunaga T,Matsuda K,Wanibuchi F,Hidaka K,Furuya T,Tamura T

更新日期：1995-05-01 00:00:00

abstract：:A high-performance liquid chromatographic method involving postcolumn fluorescence derivatization is described for the quantification of five fragment peptides (methionine-enkephalin-Thr-Ser-Glu-Lys, methionine-enkephalin-Lys, methionine-enkephalin-Arg, leucine-enkephalin-Lys and leucine-enkephalin-Arg) released by tr...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang GQ,Kai M,Ohkura Y

更新日期：1991-09-01 00:00:00

abstract：:The MeOH extract of the stem barks of Drypetes tessmanniana (Euphorbiaceae) afforded two new triterpene derivatives characterized as 3beta-O-(E)-3,5-dihydroxycinnamoyl-11-oxo-olean-12-ene and 3beta,6alpha-dihydroxylup-20(29)-ene together with seven known compounds. Their structures were established on the basis of spe...

journal_title：Chemical & pharmaceutical bulletin

authors： Dongfack MD,Van-Dufat HT,Lallemand MC,Wansi JD,Seguin E,Tillequin F,Wandji J

更新日期：2008-09-01 00:00:00

abstract：:A series of 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives was synthesized and evaluated for its ability to reverse a scopolamine-induced learned impairment in a one-trial passive avoidance task (antiamnestic activity). 2-(4-Allyl-1-piperazinyl)-4-pentyloxyquinazoline (4) showed more potent antiamnestic activity th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori M,Iemura R,Hara H,Sukamoto T,Ito K,Ohtaka H

更新日期：1991-02-01 00:00:00

abstract：:Density functional theory (DFT) calculations at the B3LYP/6-31G(d) and B3LYP/6-31G+(d) levels demonstrated that O-furfuryl S-alkyl dithiocarbonate (1) undergoes aromatic [3,3]-sigmatropic rearrangement to the energetically unfavorable S-(2-methylene-2,3-dihydrofuran-3-yl) S-alkyl dithiocarbonate (2'), which then rearr...

journal_title：Chemical & pharmaceutical bulletin

authors： Eto M,Yamaguchi K,Yoshitake Y,Harano K

更新日期：2011-01-01 00:00:00

abstract：:Particles of poorly water-soluble drugs were prepared to develop a dry powder inhaler (DPI). Spray freeze-drying (SFD) technique using a four-fluid nozzle (4N), which has been developed by authors, was applied in this research. Ciclosporin and mannitol were used as a poorly water-soluble model drug and a dissolution-e...

journal_title：Chemical & pharmaceutical bulletin

authors： Niwa T,Mizutani D,Danjo K

更新日期：2012-01-01 00:00:00

abstract：:We describe here a Tf₂NH-catalyzed formal (3+3) cycloaddition of silyl enol ethers with acrylates as a new domino reaction. In the domino sequence, the catalyst activates Michael addition, deprotonation of the resulting silyloxonium cation and intramolecular Claisen condensation. It was found that reaction modes signi...

journal_title：Chemical & pharmaceutical bulletin

authors： Azuma T,Takemoto Y,Takasu K

更新日期：2011-01-01 00:00:00

abstract：:The purpose of this study was to predict the stability of imipenem in a mixed infusion. The hydrolysis of imipenem in aqueous solution was found to be accelerated by pH, and by increasing concentrations of sodium bisulfite (SBS) and L-cysteine. Equations were derived for the degradation rate constants (k(obs)) of pH, ...

journal_title：Chemical & pharmaceutical bulletin

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

更新日期：2013-01-01 00:00:00

abstract：:Two new naphthopyrones, cassiasides B2 (1) and C2 (2), were isolated from the seeds (Cassiae Semen) of Cassia obtusifolia L. The structures of the two new compounds 1 and 2 were established as rubrofusarin 6-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-glucopyranosyl-(1-->3)-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-gluc...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitanaka S,Nakayama T,Shibano T,Ohkoshi E,Takido M

更新日期：1998-10-01 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：: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：:Novel C(7)-derivatives of 1-cyclopropyl-6-fluoro-4-quinolone carboxylic acid (3a-o) have been synthesized and evaluated for in vitro antibacterial activity. Compounds 3e (3-aminocyclobutyl), 3g (1-aminocyclopropyl), 3m ((2-aminomethyl)vinyl), and 3o ((1-aminomethyl)vinyl) showed significant inhibitory activity, compar...

journal_title：Chemical & pharmaceutical bulletin

authors： Todo Y,Nitta J,Miyajima M,Fukuoka Y,Ikeda Y,Yamashiro Y,Saikawa I,Narita H

更新日期：1994-10-01 00:00:00

abstract：:A series of substituted 4-oxoquinoline-3-carboxylic acids having a methyl group at the 8-position was prepared and tested for their antibacterial activity. 7-(trans-3-Amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-1,4-dihydro-6- fluoro-8-methyl-4-oxoquinoline-3-carboxylic acid (21) exhibited highly potent antibacterial ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyamoto H,Ueda H,Otsuka T,Aki S,Tamaoka H,Tominaga M,Nakagawa K

更新日期：1990-09-01 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

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：:Four new cycloartane glycosides were isolated from the aerial parts of Thalictrum fortunei (Ranunculaceae). The chemical structures of these new glycosides were elucidated as 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-fucopyranosyl (22S,24Z)-cycloart-24-en-3beta,22,26-triol 26-O-beta-D-glucopyranoside, 3-O-beta-D-glucop...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang XT,Zhang LH,Ye WC,Zhang XL,Yin ZQ,Zhao SX,Yao XS

更新日期：2006-01-01 00:00:00

abstract：:Chemical investigation of the soft coral Sinularia leptoclados has afforded three new sesquiterpenoids, leptocladols A (1), B (2), and 1-epi-chabrolidione A (3). The relative structures of 1-3 were determined on the basis of extensive spectroscopic analysis. The relative configuration of 1 was further confirmed by a s...

journal_title：Chemical & pharmaceutical bulletin

authors： Su JH,Chiang MY,Wen ZH,Dai CF,Hsu CH,Sheu JH

更新日期：2010-02-01 00:00:00

abstract：:The percutaneous penetration of R-(+)- and S-(-)-propranolol (PL) through rat excised skin was investigated in vitro. The flux of S-(-)-PL after application to normal skin was high compared with that of R-(+)-PL. On the other hand, in damaged rat skin, the flux of R-(+)-PL was almost equivalent to that of S-(-)-PL. It...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki K,Kaiho F,Inagaki A,Dohi M,Hazemoto N,Haga M,Hara H,Kato Y

更新日期：1992-04-01 00:00:00

abstract：:Fourteen new bisnor- and norditerpene dilactones, makilactones E-R, having a 7alpha : 8alpha-epoxy-9,11-enolide substructure, were isolated from a methanolic extract of the root and the bark of Podocarpus macrophyllus D. DON (Podocarpaceae) with thirteen known bisnor- and norditerpenoids, and the structures of those n...

journal_title：Chemical & pharmaceutical bulletin

authors： Sato K,Inaba Y,Park HS,Akiyama T,Koyama T,Fukaya H,Aoyagi Y,Takeya K

更新日期：2009-07-01 00:00:00

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：:Tumor necrosis factor (TNF), a cytokine produced in macrophages, also acts as an endogenous pyrogen (EP). To investigate whether TNF has a role in the fever induced by Nocardia rubra cell wall skeleton (N-CWS), the relationship between fever and TNF production was studied in guinea pigs. N-CWS injected i.v. to guinea ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohara K,Hirano Y,Ishida H,Mori J,Tensho A

更新日期：1989-10-01 00:00:00

abstract：:A new cytotoxic substance, designated russuphelin A (1), has been isolated from the mushroom Russula subnigricans Hongo (Basidiomycetes). The structure was elucidated as 2,6-bis(2,6-dichloro-4-hydroxyphenyloxy)-1,4-dimethoxy-benzene on the basis of spectroscopic data and confirmed by total synthesis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi A,Agatsuma T,Matsuda M,Ohta T,Nunozawa T,Endo T,Nozoe S

更新日期：1992-12-01 00:00:00

abstract：:The latex of Euphorbia nivulia afforded three new ingol diterpenes, 3-acetyl-8-methoxyl-7-angolyl-12-hydroxylingol (7), 3,12-diacetyl-7-hydroxy-8-methoxylingol (8), and 3,12-diacetyl-7-angolyl-8-hydroxylingol (9) along with five known ingol diterpenes 2-6 and a known triterpene cyclonivulinol (1). Their structures wer...

journal_title：Chemical & pharmaceutical bulletin

authors： Ravikanth V,Lakshmi Niranjan Reddy V,Vijender Reddy A,Ravinder K,Prabhakar Rao T,Siva Ram T,Anand Kumar K,Prakesh Vamanarao D,Venkateswarlu Y

更新日期：2003-04-01 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：:Poorly water-soluble drugs N-5159, griseofulvin (GFV), glibenclamide (GBM) and nifedipine (NFP) were ground in a dry process with polyvinylpyrrolidone (PVP) and sodium dodecyl sulfate (SDS). Different crystallinity behavior of each drug during grinding was shown in the ternary Drug/PVP/SDS system. However, when each t...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh K,Pongpeerapat A,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2003-02-01 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：:N-Terminal tripeptide analogs of fibrin alpha-chain were synthesized and their inhibitory effect on fibrinogen/thrombin clotting was examined. A new water-soluble active ester, 3-pyridinium ester, was used for the synthesis. Among the synthetic peptides, H-Gly-Pro-Arg-hexamethyleneimine exhibited the highest inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawasaki K,Tsuji T,Hirase K,Miyano M,Imoto Y,Iwamoto M

更新日期：1991-03-01 00:00:00

abstract：:An improved synthesis of the key intermediates (3 and 8) for the synthesis of beta-hydroxywybutines [[R-(R*,S*)]- and [S-(R*,R*)]-4], the most probable structures for the minor base from rat liver tRNA(Phe), has been achieved by the Wittig reaction between 1-benzyl-7-formylwye (1) and the phosphorane derived from (R)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Itaya T,Kanai T

更新日期：1998-08-01 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 series of imidazo[1,2-alpha]pyridinyl-2-oxobenzoxazolidines (4a-i), -3-oxo-2H-1,4-benzoxazines (5a-q), their thio-analogues (4j-p and 5r-t) and 5,6,7,8-tetrahydroimidazo[1,2-alpha]pyridinyl derivatives (8 and 9) were synthesized and tested for anti-stress ulcer activity in rats. Several compounds were found to be mo...

journal_title：Chemical & pharmaceutical bulletin

authors： Katsura Y,Nishino S,Takasugi H

更新日期：1991-11-01 00:00:00