Design and synthesis of a novel water-soluble NMDA receptor antagonist with a 1,4,7,10-tetraazacyclododecane group.

abstract：:Three new cardiac glycosides named cheiranthoside VIII (1), cheiranthoside IX (2) and cheiranthoside X (3) were isolated from the seeds of Erysimum cheiranthoides. Based on spectroscopic data, the structures of 1-3 were characterized as strophanthidin 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-antiaropyranoside, cheiran...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei ZH,Nakayama H,Kuniyasu A,Tai BS,Nohara T

更新日期：2002-06-01 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：:We synthesized some 4,4'- and 2,2'-dihydroxytriphenylmethane derivatives 3a--e and 4a--c by condensation of phenol 1 and aromatic aldehyde 2 in moderate to good yields (30--83%). Most of them showed significant antiviral activity against herpes simplex virus type 1 (anti-HSV-1 activity) in a plaque reduction assay. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Mibu N,Yokomizo K,Uyeda M,Sumoto K

更新日期：2005-09-01 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 crystal of bovine trypsin complexed with a potent inhibitor, 4-[4-(N,N- dimethylcarbamoylmethoxycarbonylmethyl)phenoxycarbonylphenyl ]guanidinium (FOY-305) in the novel orthorhombic from with a low molecular packing density was studied by the X-ray diffraction method. Using synchrotron radiation, the intensity dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto O,Taga T,Matsushima M,Higashi T,Machida K

更新日期：1990-08-01 00:00:00

abstract：:Biological activity of thioaurones was not tested so far and the group constitute completely unexplored source of new molecules of pharmacological interest. We report synthesis and evaluation of cytotoxic activity of thioaurone derivatives bearing p-hydroquinone system in ring A. Their activity was found to depend str...

journal_title：Chemical & pharmaceutical bulletin

authors： Konieczny MT,Konieczny W,Okabe S,Tsujimoto H,Suda Y,Wierzba K

更新日期：2006-03-01 00:00:00

abstract：:We have attempted to prepare micronized drug particles and to maintain the micronized state long-term in order to improve the solubility of a practically insoluble drug, griseofulvin (GF). GF nanoparticles (GFNPs) prepared by high-pressure homogenization were micronized to about 45 nm (mean particle size). GFNPs were ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kamiya S,Nozawa Y,Miyagishima A,Kurita T,Sadzuka Y,Sonobe T

更新日期：2006-02-01 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：:In order to synthesize four stereoisomers of cystathionine (CYT), D- and L-homocysteines (D- and L-Hcy) were synthesized from methionine (Met) by a facile procedure. L-Met was reacted with dichloroacetic acid in concentrated hydrochloric acid under reflux to give (4S)-1,3-thiazane-2,4-dicarboxylic acid hydrochloride [...

journal_title：Chemical & pharmaceutical bulletin

authors： Shiraiwa T,Nakagawa K,Kanemoto N,Kinda T,Yamamoto H

更新日期：2002-08-01 00:00:00

abstract：:Two novel prenylflavanes (1, 2) and a glycoside (3) of 1 were isolated along with six known compounds, isoquercitrin (4), astragalin (5), scopolin (6), skimmin (7), roseoside II (8) and benzyl D-glucopyranoside (9), from the leaves of Morus alba. The inhibitory activities of compounds 1, 2 and 3 on the oxidation of hu...

journal_title：Chemical & pharmaceutical bulletin

authors： Doi K,Kojima T,Makino M,Kimura Y,Fujimoto Y

更新日期：2001-02-01 00:00:00

abstract：:To investigate the effect of the hot water extract from Artemisia leaf (Artemisia princeps Panpanini) (AFE) on the proliferation of endothelial cells, the cells from bovine aorta were cultured for up to 96 h in the presence of 1, 5, 10 or 50 micrograms/ml AFE in RPMI1640 medium supplemented with 10% fetal bovine serum...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaji T,Kaga K,Miezi N,Ejiri N,Sakuragawa N

更新日期：1990-02-01 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：:Dryocrassyl formate, sitostanyl formate, and 12alpha-hydroxyfern-9(11)-ene were isolated from the fresh fronds of Cyathea podophylla. Their structures were elucidated by spectroscopic techniques and synthesis. Ten known triterpenoids, three derivatives of phytol, a stanol, and beta-tocopherol were also identified from...

journal_title：Chemical & pharmaceutical bulletin

authors： Arai Y,Hattori T,Hamaguchi N,Masuda K,Takano A,Shiojima K

更新日期：2003-11-01 00:00:00

abstract：:Interaction between Mn2+ ion and the two forms of DNA duplex (supercoiled and linearized pUC119 DNA) in solution has been examined by isothermal titration calorimetry. Although DNA condensation reaction heat was observed at 323 K, this was not the case at 298 K. DNA condensation was entropically driven and supercoiled...

journal_title：Chemical & pharmaceutical bulletin

authors： Utsuno K

更新日期：2008-03-01 00:00:00

abstract：:Two enkephalin-containing peptides, peptide E and dynorphin(1-24), were synthesized by conventional solution methods employing a new Trp derivative, Nin-(2,4,6-triisopropylphenylsulfonyl)tryptophan [Trp(Tps)]. All protecting groups employed including the Tps group were removed by treatment with 1 M trifluoromethanesul...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa K,Kawamoto T,Futaki S,Kiyama S,Akita T,Moritoki H,Kiso Y

更新日期：1989-10-01 00:00:00

abstract：:The aim of this study was to evaluate the effects of Magnolin (MGL) on inhibition of human breast cancer cells, and explore the underlying molecular mechanisms. The viability of the treated cells was assessed with the Cell Counting Kit-8 (CCK-8) assay, and the proliferation was analyzed in terms of EdU uptake, colony ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang J,Zhang S,Huang K,Shi L,Zhang Q

更新日期：2020-01-01 00:00:00

abstract：:Chemical and pharmacological studies of Panax vietnamensis (Vietnamese ginseng; VG) have been reported since its discovery in 1973. However, the content of each saponin in different parts of VG has not been reported. In this study, 17 ginsenosides in the different underground parts of P. vietnamensis were analyzed by ...

journal_title：Chemical & pharmaceutical bulletin

authors： Le TH,Lee GJ,Vu HK,Kwon SW,Nguyen NK,Park JH,Nguyen MD

更新日期：2015-01-01 00:00:00

abstract：:Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi S,Kojima T,Hashimoto K,Saito B,Sumi H,Ishikawa T,Ikeda Y

更新日期：2015-01-01 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：:To investigate the possible mechanism of the stimulatory effect of a hot water extract from Artemisia leaf (Artemisia princeps PANPANINI) (AFE) on the proliferation of endothelial cells, cells from bovine aorta were cultured for 72 h in RPMI1640 medium supplemented with 10% fetal calf serum in the presence of 5 microg...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaji T,Kaga K,Miezi N,Hayashi T,Ejiri N,Sakuragawa N

更新日期：1990-09-01 00:00:00

abstract：:To experimentally clarify a possible stereostructure-activity relationship proposed for H2-receptor antagonists, three 5-aminophenylimidazoles (1, 2 and 3), in which respective amino groups are located on the ortho, meta and para positions of the benzene ring, were synthesized and examined for their conformational cha...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida T,In Y,Inoue M,Kurihara T,Moriomoto K,Morisaka K,Shibata K

更新日期：1990-07-01 00:00:00

abstract：:The purpose of this study was to elucidate the effect of high-temperature storage on the stability of ranitidine, specifically with respect to the potential formation of N-nitrosodimethylamine (NDMA), which is classified as a probable human carcinogen. Commercially available ranitidine reagent powders and formulations...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe Y,Yamamoto E,Yoshida H,Usui A,Tomita N,Kanno H,Masada S,Yokoo H,Tsuji G,Uchiyama N,Hakamatsuka T,Demizu Y,Izutsu KI,Goda Y,Okuda H

更新日期：2020-10-01 00:00:00

abstract：:A series of novel 1-(6,7-dimethoxy-4-quinazolinyl)piperidines carrying substituted hydantoin and 2-thiohydantoin rings was synthesized and examined for cardiotonic activity in anesthetized dogs. Introduction of isopropyl and sec-butyl group at the 5-position of the hydantoin and thiohydantoin rings led to potent inotr...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomoto Y,Takai H,Hirata T,Teranishi M,Ohno T,Kubo K

更新日期：1990-11-01 00:00:00

abstract：:A 2,2'-[2,3-naphthylenebis(oxy)]-bis(N,N-diisopropyl(acetamide)) ligand (L) and its Gd(III) complex have been prepared and characterized. The crystal and molecular structure of the complex was determined by single-crystal X-ray diffraction. The interactions of complex with calf thymus DNA were investigated by UV-vis, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei K,Liu W,Huang X,Wang D

更新日期：2006-08-01 00:00:00

abstract：:Improved synthesis of the trans-3,5-disubstituted pyrrolidin-3-ylthio side-chain of the novel carbapenem 1 was achieved via stereoselective reduction of the 1-aryl-1-butanone derivative 5 and successive intramolecular cyclization of the resulting chiral alcohol 6. The 1-aryl-1-butanone derivative 5 was obtained by a c...

journal_title：Chemical & pharmaceutical bulletin

authors： Hashihayata T,Sakoh H,Goto Y,Hirose M,Sakuraba S,Imamura H,Sugimoto Y,Yamada K,Morishima H

更新日期：2001-11-01 00:00:00

abstract：:A new flavonol triglycoside, isorhamnetin 3-O-beta-D-xylopyranosyl-(1"-->3)-alpha-L-rhamnopyranosyl-(1'''-->6")-beta-D-galactopyranoside, has been isolated from the leaves of Hammada scoparia together with two known compounds, isorhamnetin 3-O-beta-D-apiofuranosyl-(1'''-->2")[alpha-L-rhamnopyranosyl-(1"-->6")]-beta-D-...

journal_title：Chemical & pharmaceutical bulletin

authors： Ben Salah H,Jarraya R,Martin MT,Veitch NC,Grayer RJ,Simmonds MS,Damak M

更新日期：2002-09-01 00:00:00

abstract：:Acidic segment of an acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor, R-106578 was synthesized by enantioselective hydrogenation of the Z-olefine (9-(Z)) using (R)-2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (BINAP)-Ru(OAc)2 as a catalyst in methanol at 100 degrees C, 5 kgf/cm2 of H2 pressure. The requisite Z-o...

journal_title：Chemical & pharmaceutical bulletin

authors： Murakami M,Kobayashi K,Hirai K

更新日期：2000-10-01 00:00:00

abstract：:Novel potent regulators of tumor necrosis factor alpha (TNF-alpha) production by a human promyelocytic leukemia cell line, HL-60, were prepared. All the compounds showed inducer-specific and bidirectional regulation of TNF-alpha production, i.e., they enhanced 12-O-tetradecanoylphorbol-13-acetate-induced TNF-alpha pro...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyachi H,Azuma A,Hioki E,Kobayashi Y,Iwasaki S,Hashimoto Y

更新日期：1996-10-01 00:00:00

abstract：:The stereoselective introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one was accomplished using Birch reduction and an enolate trapping reaction. It was determined that the allyl group was introduced via an unexpected conformation-flipped from the initi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hiroya K,Takahashi T,Shimomae K,Sakamoto T

更新日期：2005-02-01 00:00:00

abstract：:To find novel PPAR ligands, we prepared several 3-{3 or 4-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}propanoic acid derivatives which were designed based on the structure of our previous PPARgamma ligand 1. In PPAR binding affinity assays, compound 4, which had an ethoxy group at the C-2 position of the propanoic acid o...

journal_title：Chemical & pharmaceutical bulletin

authors： Usui S,Fujieda H,Suzuki T,Yoshida N,Nakagawa H,Ogura M,Makishima M,Miyata N

更新日期：2007-07-01 00:00:00