Regioselective N-acetylation as a route of nitro-9-phenylenediamine metabolism by rat liver cytosol.

abstract：:Novel 1,2,3,4-tetrahydroisoquinoline derivatives bearing directly a cyclic amine at the 2-position were prepared and examined for their bradycardic activities in isolated right atria and in anesthetized rats. The structure-activity relationships (SAR) study revealed that the 2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinol...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakefuda A,Watanabe T,Taguchi Y,Masuda N,Tanaka A,Yanagisawa I

更新日期：2003-04-01 00:00:00

abstract：:A series of 7-substituted-6-fluoro-1-fluoromethyl-4-oxo-4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives (2a-1) was prepared and evaluated for antibacterial activity. These compounds were obtained by deacylation of 4-benzoyloxy-2-(1-chloro-2-fluoroethyl)thio-6,7- difluoroquinoline-3-carboxylate (10) and...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuoka M,Segawa J,Amimoto I,Masui Y,Tomii Y,Kitano M,Kise M

更新日期：1999-12-01 00:00:00

abstract：:From the quaternary alkaloidal fraction of the dried tubers of Stephania cepharantha, two new isoquinoline alkaloids, stecepharine and tetradehydroreticuline have been isolated along with the known compounds, magnoflorine, menisperine, steponine, cyclanoline, oblongine, cis-N-methylcapaurine and 2'-N-methylisotetrandr...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanahashi T,Su U,Nagakura N,Nayeshiro H

更新日期：2000-03-01 00:00:00

abstract：:Using tissue engineering technique to repair cartilage damage caused by osteoarthritis is a promising strategy. However, the regenerated tissue usually is fibrous cartilage, which has poor mechanical characteristics compared to hyaline cartilage. Chondrocyte hypertrophy plays an important role in this process. Thus, i...

journal_title：Chemical & pharmaceutical bulletin

authors： Cao Z,Dou C,Dong S

更新日期：2017-01-01 00:00:00

abstract：:Gellan gum based floating beads containing clarithromycin (FBC) were prepared by iontotropic gelation method for stomach-specific drug delivery against Helicobacter pylori. The scanning electron microscope photograph indicated that prepared beads were spherical in shape with rough outer surface. Formulation variables ...

journal_title：Chemical & pharmaceutical bulletin

authors： Rajinikanth PS,Mishra B

更新日期：2009-10-01 00:00:00

abstract：:Four new cembrane diterpenes (1-4) and fifteen known cembranoids (5-19) were isolated from an Okinawan soft coral Lobophytum crassum. The structures of these four new cembranoids were determined on the basis of spectroscopic evidence. In particular, the absolute stereochemistry of 1, 2, 5 and 6 were elucidated by the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wanzola M,Furuta T,Kohno Y,Fukumitsu S,Yasukochi S,Watari K,Tanaka C,Higuchi R,Miyamoto T

更新日期：2010-09-01 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：:A new route to (+)-estrone has been developed starting from the chiral building block having a bicyclo[3.2.1]octane framework based on the inherent stereochemical chemical nature of the chiral building block. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hanada K,Miyazawa N,Ogasawara K

更新日期：2003-01-01 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：:A new resveratrol dimer and a new C-glucosyl resveratrol were isolated from stem wood of Hopea utilis along with nine stilbenoid derivatives comprising bergenin and (+)-lyoniresinol. The structures have been elucidated on the basis of the spectroscopic evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka T,Ito T,Ido Y,Nakaya K,Iinuma M,Chelladurai V

更新日期：2001-06-01 00:00:00

abstract：:Electron spin resonance studies showed that addition of rat liver microsomes to the reaction system of alloxan with reduced nicotinamide adenine dinucleotide phosphate (NADPH) resulted in a marked increase in the generation of alloxan radicals (AH.), whereas heat-denatured microsomes were without such effect. Oxidatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai K,Haga K,Ogiso T

更新日期：1992-02-01 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：:Isoliquiritigenin, glabridin, licoarylcoumarin and licoricidin were identified as strong inhibitors of adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase in waste materials which were obtained during the industrial extraction of glycyrrhizin from licorice roots. The structure-activity relationships of 12 fl...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusano A,Nikaido T,Kuge T,Ohmoto T,Delle Monache G,Botta B,Botta M,Saitoh T

更新日期：1991-04-01 00:00:00

abstract：:Three new quinovic acid glycosides, named gongganosides A (1), B (2), and C (3), were isolated from the bark of Bhesa paniculata (Celastraceae), an Indonesian medicinal plant collected in Sumatra Island. The chemical structures have been elucidated on the basis of chemical and physicochemical evidence as quinovic acid...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohashi K,Kojima H,Tanikawa T,Okumura Y,Kawazoe K,Tatara N,Shibuya H,Kitagawa I

更新日期：1994-08-01 00:00:00

abstract：:Using the unique character of the chiral Pd complexes 1 and 2, highly efficient catalytic asymmetric reactions have been developed. In contrast to conventional Pd(0)-catalyzed reactions, these complexes function as an acid-base catalyst. Thus active methine and methylene compounds were activated to form chiral palladi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hamashima Y

更新日期：2006-10-01 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：: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：: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

abstract：:Cigarette smoke, a collection of many toxic chemicals, contributes to the pathogenesis of smoking-related diseases such as chronic obstructive pulmonary disease and cancer. Much work has been done on the chemical analysis of ingredients in cigarette smoke, but there are few reports on the active ingredients that can m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi Y,Horiyama S,Honda C,Suwa K,Nakamura K,Kunitomo M,Shimma S,Toyoda M,Sato H,Shizuma M,Takayama M

更新日期：2013-01-01 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：:In continuation of our efforts to discover novel nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) as potentially "Safe NSAIDs," we report herein the design, synthesis and evaluation of 21 new NO-NSAIDs of commonly used NSAIDs such as aspirin, diclofenac, naproxen, flurbiprofen, ketoprofen, suli...

journal_title：Chemical & pharmaceutical bulletin

authors： Borhade N,Pathan AR,Halder S,Karwa M,Dhiman M,Pamidiboina V,Gund M,Deshattiwar JJ,Mali SV,Deshmukh NJ,Senthilkumar SP,Gaikwad P,Tipparam SG,Mudgal J,Dutta MC,Burhan AU,Thakre G,Sharma A,Deshpande S,Desai DC,Dubash

更新日期：2012-01-01 00:00:00

abstract：:Novel sialosyl donors, 4-pentenoic acid ester of N-acetylneuraminic acids (Neu5Ac) and 4-pentenyl glycoside of Neu5Ac were successfully prepared from the corresponding per-O-acetylated 2-hydroxy and 2-chloro derivatives of Neu5Ac, respectively and applied to the synthesis of O-sialosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda K,Fukuyo J,Sato K,Sato M

更新日期：2005-11-01 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：:Transfer of aprindine from the blood into the intestinal lumen or into the peritoneal cavity was examined after intravenous administration of the drug at a dose of 5 mg/kg in rats. The amount of the drug transferred from the blood into the intestinal lumen was much greater than into the peritoneal cavity. The average ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arimori K,Hashimoto Y,Nakano M

更新日期：1991-12-01 00:00:00

abstract：:The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydr...

journal_title：Chemical & pharmaceutical bulletin

authors： Giammona G,Giannola LI,Carlisi B,Bajardi ML

更新日期：1989-08-01 00:00:00

abstract：:A series of carbamates of the phenolic compound 1 were prepared and evaluated in vivo as its prodrug. Each carbamate was orally administered to rats, and plasma concentrations of the parent compound 1 were measured with the passage of time. We judged which carbamate was suitable for the prodrug of 1 from both the AUC ...

journal_title：Chemical & pharmaceutical bulletin

authors： Igarashi Y,Yanagisawa E,Ohshima T,Takeda S,Aburada M,Miyamoto K

更新日期：2007-02-01 00:00:00

abstract：:A new pregnane glycoside, a dibenzylbutyrolactone lignan, 5-hydroxymatairesinol dimethyl ether, and three new flavonoids, including one 8-methylflavan-3-ol, and two 8-methylflavones, together with five known flavonoids and two known alkaloids were isolated from the rhizomes of Tupistra chinensis. The structures of all...

journal_title：Chemical & pharmaceutical bulletin

authors： Pan WB,Wei LM,Wei LL,Wu YC

更新日期：2006-07-01 00:00:00

abstract：:Liposome uptake by HepG2 human hepatoma cells was investigated in comparison with the uptake by J774 murine macrophage-like cells. HepG2 cells accumulated liposomes (egg yolk phosphatidylcholine (EPC)/Chol; 75/25, diameter 0.2 micron) at 37 degrees C comparably to J774 macrophage-like cells. Confocal microscopic obser...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishiwata H,Sato SB,Kobayashi S,Oku M,Vertut-Doï A,Miyajima K

更新日期：1998-12-01 00:00:00

abstract：:We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Hirono S

更新日期：2019-01-01 00:00:00

abstract：:Polypropyleneglycol (PPG) was used as a dispersion medium for the preparation of microspheres (MS) consisting of starch, gelatin, whey protein or dextran. Aqueous solutions of the polymers were dispersed in PPG at various initial temperatures and then the systems were cooled to 0.5 degrees C to allow water in the disp...

journal_title：Chemical & pharmaceutical bulletin

authors： Seki T,Shinohara K,Kato N,Uchida M,Natsume H,Morimoto K,Juni K

更新日期：2007-03-01 00:00:00