Constituents of the Vietnamese medicinal plant Orthosiphon stamineus.

abstract：:In the present study, a novel series of 2-(2-(3-aryl-5-substituted-1,3,4-thiadiazol-2(3H)-ylidene)hydrazinyl)-4,4-diphenyl-1H-imidazol-5(4H)-one derivatives were designed and prepared via the reaction of the most versatile, hitherto unreported 2-(5-oxo-4,4-diphenyl-4,5-dihydro-1H-imidazol-2-yl)-N-phenylhydrazinecarbot...

journal_title：Chemical & pharmaceutical bulletin

authors： Gomha SM,Abdel-Aziz HM,Khalil KD

更新日期：2016-01-01 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：:Two new synthetic methods were established for the efficient synthesis of optically active cyclohexene antisepsis agent, ethyl (6R)-6-[N-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate [(R)-1: TAK-242)]. The first method involved recrystallization from methanol of the diastereomeric mixture (6RS,1'R)-7...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada M,Ichikawa T,Yamano T,Kikumoto F,Nishikimi Y,Tamura N,Kitazaki T

更新日期：2006-01-01 00:00:00

abstract：:To obtain optically active threo-2-amino-3-hydroxy-3-phenylpropanoic acid (1), (2RS,3SR)-2-benzoylamino-3-hydroxy-3-phenylpropanoic acid [(2RS,3SR)-2] was first optically resolved using (1S,2S)- and (1R,2R)-2-amino-1-(4-nitrophenyl)-1,3-propanediol as the resolving agents to afford (2R,3S)- and (2S,3R)-2 in yields of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Shiraiwa T,Saijoh R,Suzuki M,Yoshida K,Nishimura S,Nagasawa H

更新日期：2003-12-01 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：:Detailed chemical studies on the cytotoxic fraction from the leaves of Dysoxylum cumingianum have resulted in the isolation of two new triterpene glucosides, cumingianosides P (18) and Q (19), with an apotirucallane-type skeleton. The structures of 18 and 19 were determined by spectral examinations, and by conversion ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujioka T,Sakurai A,Mihashi K,Kashiwada Y,Chen IS,Lee KH

更新日期：1997-01-01 00:00:00

abstract：:This paper introduces a new delivery system for rapid and controlled drug release. Mixture of hydrophilic, (poly vinyl alcohol, PVA, and randomly methylated beta-cyclodextrin, RM beta-CD), and hydrophobic (poly D,L-lactide, PLA, and poly D,L-lactide-co-glycoside, PLGA) polymers were electrospun to make a multi-layered...

journal_title：Chemical & pharmaceutical bulletin

authors： Fathi-Azarbayjani A,Chan SY

更新日期：2010-02-01 00:00:00

abstract：:Optically active structural isomers (1b-f and dst-1b-f) of 3',4'-di-(O)-(-)-camphanoyl-(+)-khellactone (DCK) were synthesized and their anti-human immunodeficiency virus (HIV) activity was investigated. The value of the sensitivity index (SI) of 1b was greater than that of DCK. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishioka H,Uesugi K,Ueda N,Kondo Y,Tsuji M,Abe H,Harayama T,Hamasaki T,Baba M,Takeuchi Y

更新日期：2011-01-01 00:00:00

abstract：:Racemic 1-acetoxy-2-phenylpropane (12) and 1-acetoxy-2-(2-naphthyl)propane (33) were hydrolyzed with lipase at 35-36 degrees C for 2 and 24 h to give predominantly (S)-2-phenyl-1-propanol (11) and (S)-2-(2-naphthyl)-1-propanol (32), respectively. However, racemic 1-acetoxy-2-(1-naphthyl)propane (25) was recovered inta...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto T,Takeda Y,Iwata E,Sakamoto M,Ishida T

更新日期：1994-06-01 00:00:00

abstract：:To learn whether glycation plays a role in insolubilization or in senile cataractogenesis, the reactivity of lens protein from normal and senile cataractous lenses and individual crystallin prepared from human lens with various sugars [glucose, glucose-1-phosphate (G-1-P), glucose-6-phosphate (G-6-P) and fructose], an...

journal_title：Chemical & pharmaceutical bulletin

authors： Kamei A

更新日期：1992-10-01 00:00:00

abstract：:The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Sev...

journal_title：Chemical & pharmaceutical bulletin

authors： Ha ES,Baek IH,Cho W,Hwang SJ,Kim MS

更新日期：2014-01-01 00:00:00

abstract：:We used near infrared (NIR) spectroscopy to evaluate the degree of mixing of blended dry syrup (DS) products whose particle sizes are not specified in the Revised 16th Edition of the Japanese Pharmacopoeia, and also evaluated the degree of mixing when powder products or fine granule products were added to DS products....

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto Y,Suzuki T,Matsumoto M,Ohtani M,Hayano S,Fukami T,Tomono K

更新日期：2012-01-01 00:00:00

abstract：:The hypothesis that oxidative stress contributes to renal dysfunction in sinoaortically denervated (SAD) rats was investigated. Rats were sinoaortically denervated and received treatment with tempol (0.5 mmol/L in drinking water) for 8 weeks. Although the tempol treatment of the SAD rats had no significant effect on b...

journal_title：Chemical & pharmaceutical bulletin

authors： Sun Y,Fan J,Chai D,Zhang M

更新日期：2016-10-01 00:00:00

abstract：:We have identified a novel cardiac steroid, 11,19-epoxy-19-methoxytelocinobufagin, named marinosin (1), in the skin of the toad, Bufo marinus (L.) Schneider. The treatment of compound 1 with 50% CH3CN containing 0.1% trifluoroacetic acid yielded a 11 alpha-hydroxyhellebrigenin (2), which has not previously been isolat...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsukawa M,Akizawa T,Ohigashi M,Morris JF,Butler VP Jr,Yoshioka M

更新日期：1997-02-01 00:00:00

abstract：:Four new ursane-type triterpenes, 3beta-acetoxy-11alpha-methoxy-12-ursene (1), 3beta-acetoxy-11alpha-ethoxy-12-ursene (2), 3beta-acetoxy-11alpha-hydroperoxy-12-ursene (3), 3beta-hydroxy-11alpha-hydroperoxy-12-ursene (4), and two new oleanane-type triterpenes, 3beta-acetoxy-11alpha-ethoxy-12-oleanene (5), 3beta-acetoxy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chiang YM

更新日期：2000-05-01 00:00:00

abstract：:The metabolism of 2,4-dinitrotoluene (2,4-DNT), 2,4-dinitrobenzyl alcohol (2,4-DNB), 2,4-dinitrobenzaldehyde (2,4-DNBAl), 2,6-DNT, 2,6-DNB and 2,6-DNBAl in the microsomal and cytosol fractions prepared from unfortified male Wistar and male Sprague-Dawley (S.D.) rat livers was investigated. Data obtained by high-perfor...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori M,Kawajiri T,Sayama M,Miyahara T,Kozuka H

更新日期：1989-07-01 00:00:00

abstract：:Alkaline sucrose density gradient and agarose gel electrophoresis methods were used to observe lambda deoxyribonucleic acid (DNA) strand breaks by the reaction system of reduced glutathione (GSH) with alloxan in the presence of Fe(3+)-ethylenediaminetetraacetic acid (EDTA). When DNA was incubated in the reaction syste...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai K,Haga K,Ogiso T

更新日期：1992-08-01 00:00:00

abstract：:We recently proposed a new hydrogen-accepting parameter, S(HA), for monosubstituted (di)azines on the basis of the heat of formation calculated by the conductor-like screening model (COSMO) method. In this work, S(HA) values for monosubstituted thiophenes and furans were calculated and the results were applied to the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamagami C,Tachikawa H

更新日期：2003-10-01 00:00:00

abstract：:6-Amino-6-deoxyfumagillol (5) was synthesized by reductive amination of 6-oxo-6-deoxyfumagillol (4), which was obtained by oxidation of fumagillol (2). The reduction proceeded stereoselectively by the equatorial attack of hydride and 5 was found to have the same stereochemistry as that of 2. Several derivatives of 5 w...

journal_title：Chemical & pharmaceutical bulletin

authors： Marui S,Kishimoto S

更新日期：1992-03-01 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：: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：: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：:We studied a method of estimating the number of contacts in a solid dosage form using thermal analysis. Ibuprofen (IB) and Ethenzamide (ET) were used as model actives. IB and ET were granulated and sieved with each other. We prepared mixtures of IB and ET using different diameter granules. The number of contacts betwe...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoki S,Mizutani T,Danjo K

更新日期：2000-01-01 00:00:00

abstract：:Two different test methods were studied for the evaluation of release profiles of carbon dioxide, CO2, from effervescent suppositories. Three lots of commercial suppositories containing sodium bicarbonate and anhydrous sodium dihydrogen phosphate were used. The volume of CO2 released from these suppositories in normal...

journal_title：Chemical & pharmaceutical bulletin

authors： Hakata T,Iijima M,Okabe T,Kimura S,Sato H,Watanabe Y,Matsumoto M

更新日期：1993-02-01 00:00:00

abstract：:A new benzofuroquinoline derivative, 3,9-bis(N,N-dimethylcarbamoyloxy)-5H-benzofuro[3,2-c]quinoli ne-6-one (KCA-098), shows poor oral absorption due to practical insolubility in water. In this study, a co-grinding technique employing a water-soluble polymer was used for improvement of the dissolution rate of KCA-098. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada T,Saito N,Imai T,Otagiri M

更新日期：1999-09-01 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 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：:When the beta-acyloxy esters (+/-)-10 and (+/-)-11 were exposed to the lipase OF-360 from Candida rugosa or immobilized lipase OF-360 in a water-saturated organic solvent, the hydrolyzed product (8aS)-6 was obtained in high chemical (40%) and optical (> 99% ee) yields. The absolute structure of (8aS)-6 was confirmed b...

journal_title：Chemical & pharmaceutical bulletin

authors： Akita H,Nozawa M,Futagami Y,Miyamoto M,Saotome C

更新日期：1997-05-01 00:00:00

abstract：:A series of benzylamides of N-alkylated, N-acylated or free nine cyclic and one linear amino acids as potential anticonvulsants have been synthesized. The structures of the obtained compounds were designed on the basis of the previously determined structure and physicochemical properties/anticvonvulsant activity relat...

journal_title：Chemical & pharmaceutical bulletin

authors： Paruszewski R,Strupińska M,Stables JP,Swiader M,Czuczwar S,Kleinrok Z,Turski W

更新日期：2001-05-01 00:00:00

abstract：:A new dihydrobenzofuran neolignan, herpepropenal, was isolated from the seeds of Herpetospermum caudigerum. Its chemical structure was established based on spectroscopic analysis. In this work, the inhibitory effects of herpepropenal on hepatitis B virus DNA and on the replication and expression of hepatitis B surface...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang F,Zhang HJ,Zhang YY,Chen WS,Yuan HL,Lin HW

更新日期：2010-03-01 00:00:00