Synthesis of diazipine and [3H]diazipine: novel dihydropyridines as photoaffinity probes of calcium channels.

abstract：:We describe herein a manganese(IV) oxide-mediated oxidation of N-p-methoxyphenyl (PMP)-protected glycine derivatives for the synthesis of α-imino carboxylic acid derivatives. Using this methodology, utilization of unstable glyoxic acid derivatives was avoided. Furthermore, using this methodology we synthesized novel α...

journal_title：Chemical & pharmaceutical bulletin

authors： Inokuma T,Jichu T,Nishida K,Shigenaga A,Otaka A

更新日期：2017-01-01 00:00:00

abstract：:We discovered that the reactivity of some conjugated and electron-deficient hydrocarbons was quite different in the presence of transition metal catalysts. In this review we report our development and applications of the highly selective palladium and nickel-catalyzed cycloaddition reactions of unsaturated hydrocarbon...

journal_title：Chemical & pharmaceutical bulletin

authors： Saito S

更新日期：2005-09-01 00:00:00

abstract：:To investigate the possible binding mode of E-64 (N-[N-(L-3-trans-carboxyoxirane-2-carbonyl)-L-leucyl]agmatine), a potent cysteine protease inhibitor, to papain active site, molecular dynamics simulations were applied to two complex forms: R- and S- configurational forms of E-64 C2 atom for the covalent bond formation...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto D,Ohishi H,Ishida T,Inoue M,Sumiya S,Kitamura K

更新日期：1990-09-01 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：:Analysis of the structural requirements of compound 1 (SR48968), a potent NK2 receptor antagonist, revealed that the 4-phenyl group of the piperidine is essential for binding with the NK2 receptor and occupies an equatorial position. Energy calculation of a variety of substituted 4-phenyl piperidines revealed that spi...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Fujii M,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:Polymorphic behaviours of paracetamol and propyphenazone and interaction between these two compounds were investigated using differential scanning calorimetry (DSC), X-ray powder diffraction and Fourier transform-infrared (FT-IR)-spectroscopy. Binary mixtures containing various ratios of the compounds were prepared as...

journal_title：Chemical & pharmaceutical bulletin

authors： Zalac S,Khan MZ,Gabelica V,Tudja M,Mestrović E,Romih M

更新日期：1999-03-01 00:00:00

abstract：:A new monomethylated ganglioside, DSG-A (3), was obtained, together with four known gangliosides, compounds (1, 2, 4, 5), from the lipid fraction of the chloroform/methanol extract of the ovary of the sea urchin Diadema setosum. The structures of the new ganglioside was determined on the basis of chemical and spectros...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada K,Tanabe K,Miyamoto T,Kusumoto T,Inagaki M,Higuchi R

更新日期：2008-05-01 00:00:00

abstract：:Electrochemical oxidation of catechols in the presence of phenyl-Meldrum's acid as a nucleophile in aqueous solution has been studied in detail by means of cyclic voltammetry and controlled potential coulometry. The results indicate that the o-benzoquinone derived from catechols participates in Michael addition reacti...

journal_title：Chemical & pharmaceutical bulletin

authors： Nematollahi D,Bamzadeh M,Shayani-Jam H

更新日期：2010-01-01 00:00:00

abstract：:The syntheses and anti-inflammatory activities of novel thieno[2,3-b]pyridine and thieno[2,3-b:5,4-c']-dipyridine derivatives are described. These compounds were designed by modification of the quinoline template of a new type of disease-modifying antirheumatic drug (DMARD), TAK-603, and prepared by the Friedländer re...

journal_title：Chemical & pharmaceutical bulletin

authors： Baba A,Mori A,Yasuma T,Unno S,Makino H,Sohda T

更新日期：1999-07-01 00:00:00

abstract：:Four new compounds 1-4 were obtained from an oxidative coupling reaction of (E)-isorhapontigenin using FeCl(3) as oxidant. Their structures and stereochemistry were determined on the basis of spectroscopic evidence [UV, IR, MS, (1)H-, (13)C-NMR, NOE and 2D NMR], and their possible formation mechanisms were also discus...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao CS,Zhou LX,Lin M

更新日期：2004-02-01 00:00:00

abstract：:Two coumarins and one polyacetylene, 5-0-(3-chloro-2-hydroxy-3-methylbutyl)-8-methoxypsoralen (1), 2',3'-dihydro-jatamansin (2), and 10-chloro-1-heptadecene-4,6-diyne-3,8,9-triol (3), along with 15 known compounds (4-18), were isolated from the methanol extract of Niphogeton ternata. Their structures were elucidated b...

journal_title：Chemical & pharmaceutical bulletin

authors： Duan H,Takaishi Y,Fujimoto Y,Garzon C,Osorio C,Duque C

更新日期：2002-01-01 00:00:00

abstract：:16 alpha-Hydroxyandrost-4-ene-3,17,19-trione (10) was synthesized from the 16 alpha-hydroxy-6 beta,19-epoxy-17-one 3 via protection of the 16 alpha-hydroxy function as its tert-butyldimethylsilyl ether or acetate. Reductive cleavage of the epoxy ring of the silyl ether 4 or the acetate 5 with zinc dust gave the 19-alc...

journal_title：Chemical & pharmaceutical bulletin

authors： Numazawa M,Hoshi K,Konno T,Nagaoka M

更新日期：1990-07-01 00:00:00

abstract：:The mechanism of the deprotonation of 2-butanone (1) with methoxide anion (2) was studied by ab initio molecular orbital (MO) methods. Calculations of the thermodynamic stabilities of each complex and the regioselectivity of the reaction were performed using a static isodensity surface polarized continuum model (IPCM)...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda H,Yukawa M,Niiya T

更新日期：2006-05-01 00:00:00

abstract：:The full structures of the two steroidal saponins from Narthecium asiaticum MAXIM. We previously identified as toxic substances by monitoring the toxicity in guinea pigs were phytochemically reinvestigation on the aerial parts of the plant. The desired toxic saponins (6,7) were isolated together with two known lignan ...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue T,Mimaki Y,Sashida Y,Kobayashi M

更新日期：1995-07-01 00:00:00

abstract：:The biotransformation of 2α,5α,10β-triacetoxy-14-oxo-taxa-4(20),11-diene (1) by cultured Gingko cells afforded four products. Their structures were identified on the basis of analyses of the chemical and spectroscopic (IR, MS, ¹H- and ¹³C-NMR) data. Among them, 2, 3 and 5 were three new compounds, and 4 displayed pote...

journal_title：Chemical & pharmaceutical bulletin

authors： Xie D,Zhang Y,Zou J,Yin D,Chen X,Dai J

更新日期：2011-01-01 00:00:00

abstract：:4-(2-Pyridinylamino)-1,1,1-trifluoro-3-penten-2-ones 3, obtained from the reaction of commercially available 2-aminopyridine derivatives and 4-methoxy-1,1,1-trifluoro-3-penten-2-one 2, were converted to 6-(dimethylamino)-4-(2-pyridinylamino)-3,5-hexadien-2-ones 4 by treatment with dimethylformamide dimethyl acetal. Az...

journal_title：Chemical & pharmaceutical bulletin

authors： Cocco MT,Conglu C,Onnis V

更新日期：2001-06-01 00:00:00

abstract：:The intercalation reaction of diclofenac sodium (DFS) with layered inorganic compounds, gamma-titanium phosphate (gamma-TiP), proton type titanium oxide (H-TiO2) and sodium type synthetic mica (Na-TSM), was examined on. The direct reaction of DFS in ethanol-water mixed solvent resulted in the large amount accommodatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Tajima T,Suzuki N,Watanabe Y,Kanzaki Y

更新日期：2005-11-01 00:00:00

abstract：:Molecular interactions between iodine and various neuroleptics were investigated by UV/Vis spectroscopy. Iodine was found to form charge transfer complexes in a 1:1 stoichiometry and of n-sigma type with these molecules. The values of the formation constants Kc of these iodinated complexes indicate a strong donor-acce...

journal_title：Chemical & pharmaceutical bulletin

authors： Comby F,Jambut-Absil AC,Buxeraud J,Raby C

更新日期：1989-01-01 00:00:00

abstract：:Fatty acid synthesis (FAS) is an essential metabolism during the whole growth and development process of the bacterial. Several key enzymes which involved in this biosynthetic pathway have been considered as useful targets for the development of new antibacterial agents. Among them, β-ketoacyl-acyl carrier protein syn...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou Y,Yang YS,Song XD,Lu L,Zhu HL

更新日期：2017-01-01 00:00:00

abstract：:A new method has been developed for the umpolung α-heteroarylation of ketones via an N-alkoxyenamine. The treatment of ketones with tris(heteroaryl)aluminum reagents in the presence of isoxazolidine gave the corresponding α-heteroarylated ketones in moderate to good yields. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyoshi T,Takeda N,Fukami M,Sato S,Ueda M,Miyata O

更新日期：2014-01-01 00:00:00

abstract：:To expand the sequence of double-stranded DNA (dsDNA) targets in a triplex formation, 2',4'-BNAs (2'-O,4'-C-methylene bridged nucleic acids) having imidazoles as a nucleobase were synthesized and incorporated into oligonucleotides. Triplex-forming ability of the modified oligonucleotides was evaluated by using melting...

journal_title：Chemical & pharmaceutical bulletin

authors： Hari Y,Obika S,Inohara H,Ikejiri M,Une D,Imanishi T

更新日期：2005-07-01 00:00:00

abstract：:Sixteen derivatives of 1-(beta-D-arabinofuranosyl)-2-thiocytosine (araSC), including five 5'-esters, three 3'-esters, five N4-amides and three 5'-phosphodiesters, were synthesized and their reactivity to mouse tissue homogenates, including plasma, liver and intestine, and antitumor activity in mice bearing P388 cells ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawaguchi T,Ichikawa T,Hasegawa T,Saneyoshi M,Wakayama T,Kato H,Yukita A,Nagata T

更新日期：2000-04-01 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：:An improved synthetic route has been developed for the preparation of methyl 1-fluoroindan-1-carboxylate (FICA Me ester) from 1-indanone. Methyl 4-methyl-1-fluoroindan-1-carboxylate (4-Me-FICA Me ester) was also prepared following the same procedure. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koyanagi J,Kamei T,Ishizaki M,Nakamura H,Takahashi T

更新日期：2014-01-01 00:00:00

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：:A new cardenolide diglycoside (1) was isolated from Nerium oleander together with ten known cardenolide diglycosides 2-11. The structure of compound 1 was established on the basis of their spectroscopic data. The in vitro anti-inflammatory activity of compounds 1-11 was examined on the basis of inhibitory activity aga...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhao M,Bai L,Toki A,Hasegawa R,Sakai J,Hasegawa T,Ogura H,Kataoka T,Bai Y,Ando M,Hirose K,Ando M

更新日期：2011-01-01 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：:The rates of release of nicotinamide (NAA) from fatty acid (FA)-NAA complexes, FA-NAA, were determined at various temperatures, and the thermodynamic quantities for the release of NAA were estimated. The results were compared with the previous results obtained for FA-thiamine disulfide (TDS) complexes, (FA)6(TDS). The...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokoyama S,Ueda F,Fujie T

更新日期：1991-12-01 00:00:00

abstract：:A series of benzylidene 2-aminoimidazolones derivatives were synthesized. Most compounds displayed strong inhibitory activity on the proliferation of human HepG2 cells in vitro. The active compounds were further evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against five human ca...

journal_title：Chemical & pharmaceutical bulletin

authors： Ling Y,Wang ZQ,Xiao YA,Zhu C,Shen L,Wang XM,Hui Y,Wang XY

更新日期：2013-01-01 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