Synthesis of carboxyl-terminal extension analogs of dermorphin and evaluation of their opioid receptor-binding and opioid activities.

abstract：:A new 9,19-cyclolanostane-type triterpene xyloside (1), from the rhizomes of Cimicifuga racemosa, has been isolated together with four known saponins; cimiaceroside A, 25-O-methylcimigenol-3-O-beta-D-xylopyranoside, 27-deoxyactein and 23-O-acetylshengmanol-3-O-beta-D-xylopyranoside. The structure of the new compound w...

journal_title：Chemical & pharmaceutical bulletin

authors： Bedir E,Khan IA

更新日期：2000-03-01 00:00:00

abstract：:The phosphorylation of several D-glucose derivatives has been achieved using inorganic sodium cyclo-triphosphate hexahydrate (P3m), Na3P3O9 x 6H2O, in aqueous solution. In the phosphorylation of D-glucuronic acid, 6-phosphoryl-D-glucose and D-xylose, beta-D-glucuronic acid 1-triphosphate, 6-phosphoryl-beta-D-glucose 1...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue H,Watanabe M,Nakayama H,Tsuhako M

更新日期：2000-06-01 00:00:00

abstract：:In the course of our chemotaxonomic study of the liverworts growing in Madagascar, mastigophoric acid methyl ester, along with eleven known compounds were isolated from Mastigophora diclados. Isolated metabolites showed that the Malagasy Mastigophora is more related to the samples from Borneo and Japan than to the Tai...

journal_title：Chemical & pharmaceutical bulletin

authors： Harinantenaina L,Asakawa Y

更新日期：2004-11-01 00:00:00

abstract：:One novel sesquiterpene with new skeleton, (6S)-2-methyl-6-(4-hydroxyphenyl-3-methyl)-2-hepten-4-one (1), two new bisabolane sesquiterpenes, (6S)-2-methyl-6-(4-hydroxyphenyl)-2-hepten-4-one (2), (6S)-2-methyl-6-(4-formylphenyl)-2-hepten-4-one (3), and two calebin derivatives, 4''-(4'''-hydroxyphenyl-3'''-methoxy)-2''-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng Y,Qiu F,Takahashi K,Liang J,Qu G,Yao X

更新日期：2007-06-01 00:00:00

abstract：:A simple one-step synthesis was accomplished for the preparation of N-phosphoramidophosphonates by a direct reaction of phosphoramidate (1) with heterocyclic aldehydes (2a-j) and dialkyl phosphites at 60-70 degrees C in the presence of tetramethylguanidine. The tetramethylguanidine not only catalyses this reaction but...

journal_title：Chemical & pharmaceutical bulletin

authors： Veera Narayana Reddy M,Balakrishna A,Kumar MA,Reddy GC,Sankar AU,Reddy CS,Krishna TM

更新日期：2009-12-01 00:00:00

abstract：:From the MeOH extract of the aerial part of Vietnamese Orthosiphon stamineus, five new isopimarane-type diterpenes [orthosiphols F-J (1-5)] and two new diterpenes [staminols A (6) and B (7)] with a novel carbon-framework, to which we proposed the name "staminane", and three new highly-oxygenated staminane-type diterpe...

journal_title：Chemical & pharmaceutical bulletin

authors： Tezuka Y,Stampoulis P,Banskota AH,Awale S,Tran KQ,Saiki I,Kadota S

更新日期：2000-11-01 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：:5,15-Unsymmetrically disubstituted and beta-unsubstituted porphyrins such as 5-R, 15-(3,5-dimethoxyphenyl) porphyrins [where R=2-benzyloxy-1-naphthyl (1), 2-(2-naphthylmethoxy)-1-naphthyl (2), anthryl (3), or 2,4,6-triphenylphenyl (4)] and 5-(2-benzyloxy-1-naphthyl), 10,15,20-tri(3,5-dimethoxyphenyl) porphyrin (1') we...

journal_title：Chemical & pharmaceutical bulletin

authors： Tohara A,Sato M

更新日期：2008-07-01 00:00:00

abstract：:The copper ions in the imidazole-clusters of histidine-oligopeptide, His(His)nGly (n = 18) and N-acetyl-His(His)nGly(n = 8 and 18), showed the d-d transition bands at 520 nm and 630 nm and oxidase-like activities. Those with the d-d bands at 480 nm and 550 nm did not have the activity. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda J,Hanaki A,Nakajima T

更新日期：1995-02-01 00:00:00

abstract：:Polyamines, especially spermine, inhibit N-methyl-D-aspartate (NMDA) receptors as open channel blockers. Two types of water-soluble NMDA receptor antagonist, ACCn (1) and TGCn (2), with a 1,4,7,10-tetraazacyclododecane cyclic polyamine group, were synthesized and the effects of both compounds on NMDA receptors were st...

journal_title：Chemical & pharmaceutical bulletin

authors： Masuko T,Metori K,Kizawa Y,Kusama T,Miyake M

更新日期：2005-04-01 00:00:00

abstract：:In order to gain an understanding of protein binding of sulfadimethoxine (SDM) and its major metabolite, N4-acetylsulfadimethoxine (N4-AcSDM), the binding of SDM and N4-AcSDM to human and rabbit serum albumin (HSA and RSA) was investigated using circular dichroism (CD), fluorescence and dialysis techniques. The CD spe...

journal_title：Chemical & pharmaceutical bulletin

authors： Otagiri M,Nakamura H,Maruyama T,Imamura Y,Takadate A

更新日期：1989-02-01 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：:Diphenhydramine, a sedating antihistamine, is an agonist of human bitter taste receptor 14 (hTAS2R14). Diphenhydramine hydrochloride (DPH) was used as a model bitter medicine to evaluate whether the umami dipeptides (Glu-Glu and Asp-Asp) and their constituent amino acids (Glu, Asp) could suppress its bitterness intens...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuno T,Morimoto S,Nishikawa H,Haraguchi T,Kojima H,Tsujino H,Arisawa M,Yamashita T,Nishikawa J,Yoshida M,Habara M,Ikezaki H,Uchida T

更新日期：2020-01-01 00:00:00

abstract：:Binding sites of polyphenolic compounds on human serum albumin (HSA) were investigated using induced Cotton effects on the circular dichroism (CD) spectra. Polyphenolic compounds used in this study are known to be metabolites from tannins and their related polyphenols in food and medicinal plants. The present investig...

journal_title：Chemical & pharmaceutical bulletin

authors： Nozaki A,Kimura T,Ito H,Hatano T

更新日期：2009-09-01 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：:Protein nitration at tyrosine residues proceeds to form 3-nitrotyrosine; this product is today used as a biomarker of nitrative stress. We have developed an efficient method with which to identify nitrated peptides and to quantify protein nitration levels in different biological samples by a combination of the chemica...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsumoto H,Taguchi R,Kohda K

更新日期：2010-04-01 00:00:00

abstract：:Two new iridoid glycosides, 7 beta,8 beta-epoxy-8 alpha-dihydrogeniposide (1) and 8-epiapodantheroside (2), were isolated, together with six known (3-8) and three artifact (9-11) iridoids, from the leaves of Gardenia jasminoides cv. fortuneana Hara. Their structures were established based on chemical and spectral data...

journal_title：Chemical & pharmaceutical bulletin

authors： Machida K,Takehara E,Kobayashi H,Kikuchi M

更新日期：2003-12-01 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：:The complexations of sulfasalazine (H3Suz) with some of transition metals have been investigated. Three types of complexes, [Mn(HSuz)-2(H2O)4] x 2H2O, [M(HSuz)-2(H2O)2] x xH2O (M=Hg(II), ZrO(II) and VO(II), x=4, 8 and 6, respectively) and [M(HSuz)-2(Cl)(H2O)3] x xH2O (M=Cr(III) and Y(III), x=5 and 6, respectively) wer...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Wahed MG,Refat MS,El-Megharbel SM

更新日期：2008-11-01 00:00:00

abstract：:A series of N-azabicycloalkyl-1-alkyl-2-oxo-1,2-dihydro-3-quinolinecarboxamides were synthesized and tested for serotonin 5-HT4 receptor-stimulating effects in the regulation of electrically-evoked contraction in guinea pig muscle. Among them, N-azabicycloalkyl-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c,...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki M,Ohuchi Y,Asanuma H,Kaneko T,Yokomori S,Ito C,Isobe Y,Muramatsu M

更新日期：2000-12-01 00:00:00

abstract：:Three new compounds were isolated from a MeOH extract of the leaves of Syzygium samarangense, one new cyanogenic glucoside, taxiphyllin 6'-O-gallate (1), one new megastigmane glucoside, actinidioionoside 6'-O-gallate (2), and one new sulfated flavonoid rhamnoside, myricetrin 2″-O-sulfate (3), together with 14 known co...

journal_title：Chemical & pharmaceutical bulletin

authors： Samy MN,Sugimoto S,Matsunami K,Otsuka H,Kamel MS

更新日期：2014-01-01 00:00:00

abstract：:Microcrystalline cellulose (MCC) granules were prepared by wet granulation using a high-shear mixer. Physical characteristics of the granules were investigated using near IR spectrometry, thermogravimetry and isothermal water vapor adsorption. Near IR spectra of dried MCC granules prepared for various granulation time...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Kikuchi H,Yonemochi E,Terada K,Yamamoto K

更新日期：2001-04-01 00:00:00

abstract：:The purpose of the present study was to determine the thermodynamic stability orders of co-crystals by co-crystal former (CCF) exchange reactions. Caffeine (CA) was employed as a model drug. The CCF exchange reaction was performed by liquid-assisted grinding using ethanol. When oxalic acid (OX) was added to CA-citric ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mukaida M,Sugano K,Terada K

更新日期：2015-01-01 00:00:00

abstract：:Doxazosin mesylate (DXM) sustained release pellets were prepared by an extrusion-spheronization and fluid-bed coating technique. The core pellets containing DXM were prepared by extrusion-spheronization technique, and coated by a fluid-bed coater to control the release of DXM. The factors affecting to properties of pe...

journal_title：Chemical & pharmaceutical bulletin

authors： Ha JM,Kim JY,Oh TO,Rhee YS,Chi SC,Kuk H,Park CW,Park ES

更新日期：2013-01-01 00:00:00

abstract：:New triazine-type dehydrocondensing reagents, such as ROMP-Trz-Cl and ROMP(OH)-Trz-Cl, were synthesized by a ring opening metathesis polymerization (ROMP) method, and these showed higher loading than conventional polymer-supported condensing reagents. These polymers effect the formation of amides in good yields by add...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Kameyama S,Tani S,Kunishima M

更新日期：2007-05-01 00:00:00

abstract：:Four new cyclopropyl-triterpenes, 27-nor-3beta-hydroxy-25-oxocycloartane (1), (22E)-25,26,27-trinor-3beta-hydroxycycloart-22-en-24-al (2), 3beta-acetoxy-15alpha-hydroxy-13,27-cyclours-11-ene (3), 3beta-acetoxy-12alpha-formyloxy-13,27-cycloursan-11alpha-ol (4), together with (23E)-27-nor-3beta-hydroxycycloart-23-en-25-...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiang YM,Su JK,Liu YH,Kuo YH

更新日期：2001-05-01 00:00:00

abstract：:Starting from benzo- or thienocycloalkaneacetic acids, we have prepared a series of 1-(3-p-fluorobenzoylpropyl)-4-(1-oxo-benzo- or thienocycloalkyl-2-ethyl)piperazines 8a-e containing both semirigid and linear butyrophenones pharmacophores. The affinities of these compounds for dopamine (D2) and 5-hydroxytryptamine (5...

journal_title：Chemical & pharmaceutical bulletin

authors： Raviña E,Fueyo J,Masaguer CF,Negreira J,Cid J,Loza I,Honrubia A,Tristán H,G-Ferreiro T,Fontenla JA,Rosa E,Calleja JM,De Ceballos ML

更新日期：1996-03-01 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：:Even though β-lapachone is a promising compound with antitumor, antiinflammatory, antineoplastic, and wound-healing effects, there are still issues concerning its chemical stability and degradation mechanisms. The objective of this study was to obtain degradation profiles of β-lapachone and evaluate its chemical stabi...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim KH,Park SH,Adhikary P,Cho JH,Kang NG,Jeong SH

更新日期：2016-01-01 00:00:00

abstract：:The title compound, PNU-97018 [systemic name: 2-butyl-3,6,7,8,9,11-hexahydro-6,9-dimethyl-3-([2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl)-6,9-ethano-4H-imidazo[4,5-d]-pyridazino[1,2-a]pyridazin-4-one] is a newly developed angiotensin II receptor antagonist. The compound and its methanolate and ethanolate were ch...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishii H,Yamaguchi K,Seki H,Sakamoto S,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2002-08-01 00:00:00