Characterization of crystalline L-carnosine Zn(II) complex (Z-103), a novel anti-gastric ulcer agent: tautomeric change of imidazole moiety upon complexation.

abstract：:To reverse the adverse reactions of alkylxanthines and to develop novel inhibitors of cyclic AMP phosphodiesterase 4 (PDE4), a series of heterocycle [a]-, [b]-, [c,d]-, and [i]-condensed purines were designed and synthesized. Although all compounds did not display PDE1 and PDE3 inhibitory activities, several heterocyc...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki H,Yamamoto M,Shimura S,Miyamoto K,Yamamoto K,Sawanishi H

更新日期：2002-09-01 00:00:00

abstract：:We developed a rapid and efficient analytical technique for cyclosporine A using HPLC on a column packed with 2-µm nonporous octadecylsilyl silica particles. Under optimized conditions, cyclosporine A was separated with high resolution from other cyclic peptides within 3 min, because the mass transfer resistance in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Kato K,Nanjo K,Goda Y

更新日期：2018-01-01 00:00:00

abstract：:(+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4, 5-tetrahydro-8H-pyrido[4',3':4,5]thieno[3,2-f]triazolo[4,3-a] [1,4]diazepine (E6123) is a very potent platelet-activating factor (PAF) receptor antagonist and shows potent anti-PAF activities at the microgram level in a variety of animal models. In ord...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazawa S,Okano K,Kawahara T,Machida Y,Yamatsu I

更新日期：1992-03-01 00:00:00

abstract：:Three new anthraquinone glycosides, lasianthuoside A (1), B (2), and C (3), were isolated from the root of Lasianthus acuminatissimus MERR., The structural elucidation of these anthraquinones was mainly established on the basis of 1D and 2D NMR and HR-MS spectroscopic analysis. Ten known compounds, damnacanthol (4), d...

journal_title：Chemical & pharmaceutical bulletin

authors： Li B,Zhang DM,Luo YM,Chen XG

更新日期：2006-03-01 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：:A series of novel 1,5-diphenylpyrazole derivatives bearing hydrophilic substituents was prepared. The anti-inflammatory and analgesic activities of these compounds were evaluated by using the adjuvant arthritis and Randall-Selitto assays in rats, and the structure-activity relationships were studied. The optimal compo...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsuji K,Konishi N,Spears GW,Ogino T,Nakamura K,Tojo T,Ochi T,Shimojo F,Senoh H,Matsuo M

更新日期：1997-09-01 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：:The CHCl3 extract of the root of Angelica japonica showed high inhibitory activity against human gastric adenocarcinoma (MK-1) cell growth. From this extract, a new furanocoumarin named japoangelone and four furanocoumarin ethers of falcarindiol, named japoangelols A-D, were isolated together with caffeic acid methyl ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujioka T,Furumi K,Fujii H,Okabe H,Mihashi K,Nakano Y,Matsunaga H,Katano M,Mori M

更新日期：1999-01-01 00:00:00

abstract：:Three new fasciculol esters, fasciculic acids A (1), B (2) and C (3), having potent calmodulin antagonistic activity were isolated from the toxic mushroom Naematoloma fasciculare (Fr.) Karst. Their structures were elucidated on the basis of spectral and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi A,Kusano G,Ohta T,Ohizumi Y,Nozoe S

更新日期：1989-12-01 00:00:00

abstract：:The novel hydroxamates containing purine scaffold were designed, synthesized and screened for their biological activities as histone deacetylase (HDAC) inhibitors. Some of them exhibited excellent acti-HDACs activities and antiproliferative activities, the most promising compound was 7m'. Western blot analysis indicat...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu Z,Yang Y,Mai X,Liu B,Xiong Y,Feng L,Liao Y,Zhang Y,Wang H,Ouyang L,Liu S

更新日期：2018-01-01 00:00:00

abstract：:Diazipine and [3H]diazipine were synthesized as new 1,4-dihydropyridine photoaffinity ligands containing a phenyldiazirine group. After simple high performance liquid chromatography separation, both compounds were purified in good overall yields. [3H]Diazipine (21.2 Ci/mmol) was synthesized in two steps from commercia...

journal_title：Chemical & pharmaceutical bulletin

authors： Taki M,Kuniyasu A,Nakayama H,Kanaoka Y

更新日期：1991-07-01 00:00:00

abstract：:The adsorptive behavior of the anti-inflammatory drug meloxicam was studied by cyclic, differentia-pulse and square-wave voltammetry on a hanging mercury drop electrode (HMDE). The drug was accumulated at HMDE and a well-defined stripping peak current was obtained at -1.42 V vs. Ag/AgCl (saturated KCl) electrode in ac...

journal_title：Chemical & pharmaceutical bulletin

authors： Radi AE,Ghoneim M,Beltagi A

更新日期：2001-10-01 00:00:00

abstract：:A series of novel potentially platelet aggregation-inhibiting 1,4-benzoxazine-3(4H)-one derivatives was designed and synthesized through Smiles rearrangement, reduction and acetylation reactions. The antiaggregatory activities of the target molecules on arterial blood samples from rabbits, expressed by IC₅₀ values (μM...

journal_title：Chemical & pharmaceutical bulletin

authors： Liu C,Tan JL,Xiao SY,Liao JF,Zou GR,Ai XX,Chen JB,Xiang Y,Yang Q,Zuo H

更新日期：2014-01-01 00:00:00

abstract：:Arginine vasopressin (AVP) has a dual action mainly in the periphery, i.e., vasoconstriction and water reabsorption via V1A and V2 receptors; it may play a role in a number of diseases, including congestive heart failure (CHF), hypertension, renal disease, edema, and hyponatremia. We have attempted to develop a new se...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuhisa A,Taniguchi N,Koshio H,Yatsu T,Tanaka A

更新日期：2000-01-01 00:00:00

abstract：:Seventeen saponins isolated from the root of Pulsatilla koreana were examined for their in vitro cytotoxic activity against the human solid cancer cell lines, A-549, SK-OV-3, SK-MEL-2, and HCT15, using the SRB assay method, and their in vivo antitumor activity using BDF1 mice bearing Lewis lung carcinoma (LLC). The sa...

journal_title：Chemical & pharmaceutical bulletin

authors： Bang SC,Lee JH,Song GY,Kim DH,Yoon MY,Ahn BZ

更新日期：2005-11-01 00:00:00

abstract：:The oxalate salts and free bases of fentanyl and N-[1-(2-phenylethyl)-4-piperidyl]-N-(1-phenyl-4-pyrazolyl)propanamide, a new lead compound for long-acting analgesia, have been characterized by (1)H- and (13)C-NMR spectroscopy. The crystal structure of the hydrochloride of N-[1-(2-phenylethyl)-4-piperidyl]-N-(1-phenyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Jimeno ML,Alkorta I,Cano C,Jagerovic N,Goya P,Elguero J,Foces-Foces C

更新日期：2003-08-01 00:00:00

abstract：:The object of this study was to develop hydroxypropyl methylcellulose (HPMC) based cephalexin extended release tablet, which can release the drug for six hours in predetermined rate. Twenty-one batches of cephalexin tablets were prepared by changing various physical and chemical parameters, in order to get required th...

journal_title：Chemical & pharmaceutical bulletin

authors： Saravanan M,Sri Nataraj K,Ganesh KS

更新日期：2003-08-01 00:00:00

abstract：:The effects of storage on the crystallization, dissolution and absorption of tolbutamide from amorphous tolbutamide-2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) complex were investigated, in comparison with those of polyvinylpyrrolidone (PVP) solid dispersion. The amorphous solid complex of tolbutamide with HP-beta...

journal_title：Chemical & pharmaceutical bulletin

authors： Kimura K,Hirayama F,Arima H,Uekama K

更新日期：2000-05-01 00:00:00

abstract：:A novel macrocyclic diterpene, jatrophenone, has been isolated from the whole plant of Jatropha gossypifolia. The structure of the compound was established by detailed studies of its one- and two-dimensional (1D and 2D) NMR spectra. The compound possesses significant antibacterial activity. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ravindranath N,Venkataiah B,Ramesh C,Jayaprakash P,Das B

更新日期：2003-07-01 00:00:00

abstract：:Inhibitors of delta 4-3-ketosteroid (5 alpha) reductase, which had been prepared from rat prostate and converted testosterone to 5 alpha-dihydrotestosterone and 4-androstene-3,17-dione, were isolated from 50% ethanol extract of Populus nigra. They were identified as pinobanksin (I, 3,5,7-trihydroxyflavanone), 3,7-dime...

journal_title：Chemical & pharmaceutical bulletin

authors： Komoda Y

更新日期：1989-11-01 00:00:00

abstract：:It is well-known that baicalin-berberine complex (1) precipitates in the water decoction of numerous Chinese Medicinal formulae containing Radix Scutellariae and Rhizoma Coptidis or Cortex Phellodendri. In the current study, ionic interaction between the carboxylate ion of baicalin and the quaternary ammonium ion of b...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang JR,Tanaka T,Zhang H,Kouno I,Jiang ZH

更新日期：2012-01-01 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：:The reaction of the N-furfuryloxamic acid sodium salt (12) with 1,1'-oxalyldiimidazole (ODI) yielded the imidazolide (13) as an intermediate, and this directly reacted with 2-aminothiazole derivatives (14) or 2-aminobenzothiazole derivatives (15) under essentially neutral conditions to afford the N'-12-(substituted th...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa T,Tsutsui C

更新日期：2000-09-01 00:00:00

abstract：:An automated synthesis system using a solid-phase extraction (SPE) system and column packed with octadecylsilica (ODS), which was coated with phospholipid and loaded with dog liver microsomes, was developed for synthesis of glucuronides. Preparation of the microsome-immobilized SPE column, glucuronidation of drugs to ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kashima Y,Kitade T,Kashima Y,Okabayashi Y

更新日期：2010-03-01 00:00:00

abstract：:A novel series of quinoline azodyes (5-(4'-derivatives phenyldiazo)-8-hydroxy-7-quinolinecarboxaldehyde)) (HL1-HL5) has been prepared and characterized by elemental analyses, 1H-NMR and IR spectra. The IR spectral data indicate that the compounds can exist in two resonance structures. Proton-ligand dissociation consta...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Sonbati AZ,El-Bindary AA,Shoair AGF,Younes RM

更新日期：2001-10-01 00:00:00

abstract：:The objective of this study was to synthesize several new pregnane derivatives and evaluate them as antiandrogens. From the commercially available 16-dehydropregnenolone acetate (7), two new steroidal compounds were synthesized: 17alpha-hydroxy-17beta-methyl-16beta-phenyl-D-homoandrosta-1,4,6-triene-3,20-dione (18) an...

journal_title：Chemical & pharmaceutical bulletin

authors： Cabeza M,Heuze I,Bratoeff E,Ramírez E,Martínez R

更新日期：2001-05-01 00:00:00

abstract：:The aqueous ethanolic extract from the fresh stems of Opuntia dillenii HAW. showed potent radical scanvenging activity. Three new compounds, opuntioside I, 4-ethoxyl-6-hydroxymethyl-alpha-pyrone, and kaempferol 7-O-beta-D-glucopyranosyl-(1-->4)-beta-D-glucopyranoside, were isolated from the extract. The structures of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Qiu Y,Chen Y,Pei Y,Matsuda H,Yoshikawa M

更新日期：2002-11-01 00:00:00

abstract：:The tumor microenvironment is considered as one of the important targets for anticancer drug discovery. In particular, nutrient deficiency may be observed in tumor microenvironment; biakamides A-D (1-4) isolated from marine sponge Petrosaspongia sp. as growth inhibitors against cancer cells adapted to glucose-deprived...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida R,Matsumoto H,Ichii S,Kobayashi M,Arai M,Kotoku N

更新日期：2019-03-01 00:00:00

abstract：:The Stille coupling reaction of the stannylindole 13 with the 5-iodoimidazole derivative 14 (or 27) in the presence of PdCl(2)(PPh(3))(2) gave the corresponding indole-imidazole coupling product 15 (or 28), thereby affording a synthetic approach to 10-methylgranulatimide (7), 15-methylgranulatimide (11), and 10, 15-di...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Nishiyachi M,Nakashima N,Murase M,Kotani E

更新日期：2003-02-01 00:00:00

abstract：:A series of about fifty novel 5-arylfuro[2,3-d]pyrimidine derivatives were synthesized as potential inhibitors of dihydrofolate reductase (DHFR) arising from different species. Weak enzyme inhibition was observed for most of the compounds, with only a few reaching IC50 values less than 30 microM. With regards to antib...

journal_title：Chemical & pharmaceutical bulletin

authors： Wahid F,Monneret C,Dauzonne D

更新日期：1999-02-01 00:00:00