Synthesis and activity of a metabolite of (S)-6-amino-5-(6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxamido)-3-methyl-1-phenyl-2,4-(1H,3H)-pyrimidinedione (CX-659S).

abstract：:Green tea and (-)-epigallocatechin gallate (EGCG: one of main components of green tea) are well known to have preventive activities against human cancers. Previously, using a galloyl group as a core structure derived from EGCG, we developed alkyl gallate and gallamide derivatives, which showed strong antiproliferative...

journal_title：Chemical & pharmaceutical bulletin

authors： Dodo K,Minato T,Hashimoto Y

更新日期：2009-02-01 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：:The permeability of nalmefene hydrochloride (NH) across different regions of ovine nasal mucosa was investigated in vitro. Five different regions of ovine nasal mucosa (superior turbinate mucosa, middle turbinate mucosa, inferior turbinate mucosa, posterior septum mucosa, and anterior septum mucosa) were studied. The ...

journal_title：Chemical & pharmaceutical bulletin

authors： Du G,Gao Y,Nie S,Pan W

更新日期：2006-12-01 00:00:00

abstract：:Tumor necrosis factor (TNF), a cytokine produced in macrophages, also acts as an endogenous pyrogen (EP). To investigate whether TNF has a role in the fever induced by Nocardia rubra cell wall skeleton (N-CWS), the relationship between fever and TNF production was studied in guinea pigs. N-CWS injected i.v. to guinea ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohara K,Hirano Y,Ishida H,Mori J,Tensho A

更新日期：1989-10-01 00:00:00

abstract：:From Puerariae Radix, the root of Pueraria lobata (Leguminosae), six new oleanene-type triterpene glycosides, called kudzusaponins A1 (1), A2 (2), Ar (3), SA4 (5), and SB1 (6) were isolated together with kudzusaponin A3 (7), soyasaponins SA3 (8), and I (9). The structures of 1-6 were determined to be 3-O-alpha-L-rhamn...

journal_title：Chemical & pharmaceutical bulletin

authors： Arao T,Kinjo J,Nohara T,Isobe R

更新日期：1997-02-01 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：: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：:Two new C(21) steroidal glycosides, tenacissoside L (1), tenacissoside M (2), were isolated from the stems of Marsdenia tenacissima (ROXB.) WIGHT et ARN. Their structures were elucidated, respectively, by means of chemical and spectral data, including ESI-MS, HR-ESI-MS, 1D-NMR and 2D-NMR. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang S,Lai YH,Tian B,Yang L

更新日期：2006-05-01 00:00:00

abstract：:A series of joro spider toxins, novel polyamines sharing a common moiety of 2,4-dihydroxyphenylacetyl cadaverine, have been identified using various bioassays, such as inhibition of a glutamatergic transmission and insecticidal activity. In this paper, we tried to chemically find still unknown polyamine toxins in the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiba T,Akizawa T,Matsukawa M,Pan-Hou H,Yoshioka M

更新日期：1994-09-01 00:00:00

abstract：:Six new cyclic peptides, gypsophin A-F (1-6), were isolated from Gypsophila oldhamiana. Their structures were elucidated by extensive NMR and chemical degradation. Compound 3 exhibited moderate activity of antiplatelet aggregation in vitro. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang G,Luo JG,Yang MH,Wang XB,Kong LY

更新日期：2013-01-01 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

abstract：:A new series of 11-substituted 6,11-dihydrodibenz[b,e]oxepin derivatives was synthesized and evaluated for antiallergic activity. Convenient methods for the preparation of sulfides from alcohols were developed. Structure-activity relationships are described. Compound 7, 11-[2-(dimethylamin)ethyl]thio-6,11-dihydrodiben...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohshima E,Kumazawa T,Takizawa H,Harakawa H,Sato H,Obase H,Oiji Y,Ishii A,Ishii H,Ohmori K

更新日期：1991-10-01 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：:Monoterpene glucosides, perillosides A and C, obtained from the leaves of Perilla frutescens, were found to be inhibitors of aldose reductase (EC 1.1.1.21) which is considered to be a key enzyme in diabetic complications such as cataract. The apparent type of inhibition of rat lens aldose reductase by perillosides A a...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujita T,Ohira K,Miyatake K,Nakano Y,Nakayama M

更新日期：1995-06-01 00:00:00

abstract：:Chlorpheniramine (CPM) maleate was prepared as a series of resinates by the batch method. The several resinates were investigated by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and infrared (IR) spectrometry. The results from DSC and XRPD showed that the molecular state of the entrapped dr...

journal_title：Chemical & pharmaceutical bulletin

authors： Akkaramongkolporn P,Yonemochi E,Terada K

更新日期：2000-02-01 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：:Solifenacin (Sol), an antimuscarinic agent has been widely used for the treatment of overactive bladder. Transdermal formulations can be administered without water as well as absorbed slowly into the blood over a long period of time. The aim of this study was to develop cream and tape formulations of Sol, and evaluate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Uchida S,Kashiwagura Y,Tanaka S,Matsui R,Namiki N

更新日期：2019-01-01 00:00:00

abstract：:A new series of novel (2S)-2-({2-[1,4-dihydro-3,5-bis(methoxycarbonyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridin-1-yl]-2-oxoethyl}amino)-3-(4-hydroxyphenyl) propanoic acid (3a) and its analogues 3b-j has been synthesized. These compounds were evaluated for their in vitro antioxidant activity, anti-inflammatory activity an...

journal_title：Chemical & pharmaceutical bulletin

authors： Subudhi BB,Sahoo SP

更新日期：2011-01-01 00:00:00

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：:A calcium-binding protein, regucalcin, was isolated from rat liver cytosol. Rabbit-anti-regucalcin antiserum, which was raised against regucalcin conjugated by glutaraldehyde to bovine serum albumin, was applied to glutaraldehyde-fixed whole mounts and subsequently visualized using the peroxidase-antiperoxidase method...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Isogai M,Kato S,Mori S

更新日期：1991-06-01 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：:The abnormal aggregation of amyloid β-peptide (Aβ) is central to the pathogenesis of Alzheimer's disease, the major form of dementia. Aromatic π-π interactions have been suggested to play a crucial role in the aggregation of not only Aβ, but also other amyloidogenic proteins. In this study, each or all phenylalanine (...

journal_title：Chemical & pharmaceutical bulletin

authors： Genji M,Yano Y,Hoshino M,Matsuzaki K

更新日期：2017-01-01 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：:Heparan sulfate proteoglycan was extracted from bovine lens capsules by 0.45 M NaCl/2 M urea and purified using ion-exchange chromatography and gel filtration. The proteoglycan was found to consist of protein and carbohydrate in a ratio of 75 to 25. The estimated average molecular weight of the heparan sulfate proteog...

journal_title：Chemical & pharmaceutical bulletin

authors： Onodera S

更新日期：1991-04-01 00:00:00

abstract：:A novel method for thermodynamic stability studies of polymorphic drug substances has been developed. In order to estimate the transition temperature for an enantiotropic polymorphic pair, a formula for calculating the temperature at which the solubilities of each polymorph become equal has been derived with heat of s...

journal_title：Chemical & pharmaceutical bulletin

authors： Urakami K,Shono Y,Higashi A,Umemoto K,Godo M

更新日期：2002-02-01 00:00:00

abstract：:Three new cycloartane triterpene glycosides, soulieosides A (1), B (2), and C (3), were isolated from the rhizomes of Souliea vaginata, and their structures were elucidated on the basis of extensive NMR experiments and chemical methods. Soulieosides A-C were assigned as 25-O-acetylcimigenol-3-O-beta-D-(2-acetyl)xylopy...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou L,Yang J,Zou J,Tu G

更新日期：2004-05-01 00:00:00

abstract：:Chemical reactivity descriptors and lipophilicyty (log P) were evaluated via semi-empirical method for the quantum calculation of molecular electronic structure (PM3) in order to clarify the structure-cytotoxic activity relationships of disubstutited thioureas. Analysed compounds were obtained by the linkage of 2-amin...

journal_title：Chemical & pharmaceutical bulletin

authors： Filipowska A,Filipowski W,Tkacz E,Nowicka G,Struga M

更新日期：2016-01-01 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：:A new sesquiterpene 2,9-humuladien-6-ol-8-one (1) was isolated from methanol extract of Zingiber aromaticum, along with 15 known compounds. The structures of the isolated compounds were elucidated on the basis of spectroscopic analyses. The isolated compounds were tested for their inhibitory activity on the metabolism...

journal_title：Chemical & pharmaceutical bulletin

authors： Subehan,Usia T,Kadota S,Tezuka Y

更新日期：2005-03-01 00:00:00

abstract：:A convenient and economical synthesis of 4-hydroxy-2,3-dimethoxybenzaldehyde has been developed. This was used as the starting material for the first total syntheses of (+/-)-isopiline, (+/-)-preocoteine, (+/-)-oureguattidine and (+/-)-3-methoxynordomesticine in which the key step involved formation of ring C of the a...

journal_title：Chemical & pharmaceutical bulletin

authors： Nimgirawath S,Udomputtimekakul P,Taechowisan T,Wanbanjob A,Shen Y

更新日期：2009-04-01 00:00:00