Preparation of 9-hydroxy grayanotoxin derivatives and their acute toxicity in mice.

abstract：:Telmisartan (anti-hypertensive) is insoluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less (bioavailability 42%). In the present study an attempt has been made to prepare immediate release tablets of...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekar V,Chellan VR

更新日期：2008-04-01 00:00:00

abstract：:We designed a single unit type tablet formulation containing nateglinide to decrease both postprandial blood glucose level (PBG) and fasting blood glucose level (FBG) in normal beagle dogs. The tablet was a dry coated tablet comprising both a core tablet (an erosion matrix tablet: a controlled release portion(nateglin...

journal_title：Chemical & pharmaceutical bulletin

authors： Makino C,Sakai H,Okano A,Yabuki A

更新日期：2009-09-01 00:00:00

abstract：:Italian canned tomatoes contain the tomato glycosides esculeosides B-1 (1, 0.0052%) and B-2 (2, 0.0068%) without esculeoside A. Herein, the structure of esculeoside B-1 (1) is characterized to be 3-O-β-lycotetraosyl (5S,22R,23S,25S)-22,26-epimino-16β,23-epoxy-3β,23,27-trihydroxycholestane 27-O-β-D-glucopyranoside. We ...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Fujiwara Y,Ikeda T,Ono M,Murakami K,Zhou JR,Yokomizo K,Nohara T

更新日期：2013-01-01 00:00:00

abstract：:We synthesized some 4,4'- and 2,2'-dihydroxytriphenylmethane derivatives 3a--e and 4a--c by condensation of phenol 1 and aromatic aldehyde 2 in moderate to good yields (30--83%). Most of them showed significant antiviral activity against herpes simplex virus type 1 (anti-HSV-1 activity) in a plaque reduction assay. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Mibu N,Yokomizo K,Uyeda M,Sumoto K

更新日期：2005-09-01 00:00:00

abstract：:Three new steroidal glycosides, named solaviasides A, B, and C, have been isolated from the fruits of Solanum viarum DUNAL (syn. S. khasianum var. chatterjeeanum, Solanaceae), along with seven known ones. Their chemical structures were determined on the basis of spectroscopic data and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Kakiuchi T,Ebisawa H,Shiono Y,Nakamura T,Kai T,Ikeda T,Miyashita H,Yoshimitsu H,Nohara T

更新日期：2009-06-01 00:00:00

abstract：:Atranorin, lichexanthone, and the (+)-usnic, diffractaic, divaricatic, perlatolic, psoromic, protocetraric, and norstictic acids isolated from the lichens Parmotrema dilatatum (VAIN.) HALE, Usnea subcavata MOTYKA, Usnea sp., Ramalina sp., Cladina confusa (SANT.) FOLMM. & AHTI, Dirinaria aspera HÄSÄNEN, and Parmotrema ...

journal_title：Chemical & pharmaceutical bulletin

authors： Brandão LF,Alcantara GB,Matos Mde F,Bogo D,Freitas Ddos S,Oyama NM,Honda NK

更新日期：2013-01-01 00:00:00

abstract：:Present studies were undertaken on the preparation of synthetic analogues of bis- or tetra-coumarins and their activity against HIV-1 integrase (HIV-1 IN). Among these coumarin analogues, compounds 14, 16 and 18 were found to be potent molecules against HIV-1 IN at IC50 values of 0.96, 0.58, and 0.49 microM, respectiv...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiang CC,Mouscadet JF,Tsai HJ,Liu CT,Hsu LY

更新日期：2007-12-01 00:00:00

abstract：:Vanadate stimulated the release of rat hepatic lipase activity from liver slices into an incubation medium in a time- and dose-dependent manner. Insulin, however, failed to have this stimulatory action, and the release by heparin was recognized, but was not additive to that by vanadate. Amiloride, an inhibitor of tyro...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita T,Mikami F,Kanagawa A,Sera M,Ueki H

更新日期：1991-12-01 00:00:00

abstract：:Casearins G-R, new cytotoxic clerodane diterpenes have been isolated from the leaves of Casearia sylvestris Sw. (Flacourtiaceae). Their structures have been elucidated by spectroscopic methods and chemical conversions, and their structure-activity relationships have been discussed. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Nakayama M,Kojima H,Takeya K,Itokawa H,Schenkel EP,Motidome M

更新日期：1991-03-01 00:00:00

abstract：:We synthesize optically active (R)-terbutaline 2, which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of...

journal_title：Chemical & pharmaceutical bulletin

authors： Uchimoto H,Ikeda M,Tanida S,Ohhashi K,Chihara Y,Shigeta T,Arimitsu K,Yamashita M,Nishide K,Kawasaki I

更新日期：2017-01-01 00:00:00

abstract：:Enantioselective fluorinating agents, (R)- and (S)-,N-fluoro-3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (BNBT-F, 2) are readily prepared in 3 steps from racemic 3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (5) via optical resolution and fluorination. These agents m...

journal_title：Chemical & pharmaceutical bulletin

authors： Shibata N,Liu Z,Takeuchi Y

更新日期：2000-12-01 00:00:00

abstract：:A rapid method for the separation and purification of uridine diphosphate-glucuronosyltransferases (GT) was developed with the use of chromatofocusing on a high-performance liquid chromatograph. GT isoenzymes solubilized from hepatic microsomes of Wistar rats were separated on a Mono P column, a pre-packed column for ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takanashi H,Homma H,Matsui M

更新日期：1989-06-01 00:00:00

abstract：:A series of bicyclic thiazoline derivatives (4a-s) was synthesized and evaluated for hepatoprotective activity against galactosamine-induced and monoclonal antibody-induced acute liver injuries in rats. The structure-activity relationships were investigated. Among the compounds synthesized, ethyl 3-(N-methylcarbamoyl)...

journal_title：Chemical & pharmaceutical bulletin

authors： Hasegawa M,Nakayama A,Hosokami T,Kurebayashi Y,Ikeda T,Shimoto Y,Ide S,Honda Y,Suzuki N

更新日期：1995-01-01 00:00:00

abstract：:Two major and two minor forms of dihydrodiol dehydrogenase with similar molecular weights of around 36000 were purified from monkey liver cytosol. All the forms oxidized trans-dihydrodiols of benzene and naphthalene and reduced aromatic aldehydes, but showed differences in charge, specificity for other substrates and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakagawa M,Harada T,Hara A,Nakayama T,Sawada H

更新日期：1989-10-01 00:00:00

abstract：:Tetrasubstituted (Z)-alkenes were readily prepared through the Horner-Wadsworth-Emmons reactions of methyl 2-[bis(2,2,2-trifluoroethyl)phosphono]propionate with aryl alkyl ketones by employing Sn(OSO(2)CF(3))(2) and N-ethylpiperidine. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sano S,Takehisa T,Ogawa S,Yokoyama K,Nagao Y

更新日期：2002-09-01 00:00:00

abstract：:Eight new guaipyridine sesquiterpene alkaloids, rupestines F-M (1-8) were isolated from the leaves of Artemisia rupestris and their structures were elucidated on the basis of 2D-NMR data. The absolute configurations of 1-8 have been assigned by comparison of their experimental and calculated circular dichroism (CD) sp...

journal_title：Chemical & pharmaceutical bulletin

authors： He F,Nugroho AE,Wong CP,Hirasawa Y,Shirota O,Morita H,Aisa HA

更新日期：2012-01-01 00:00:00

abstract：:Two new triterpenoid glycosides called medicago-saponins P1 (1) and P2 (2) were isolated together with five known glycosides from the aerial parts of Medicago polymorpha L. (Leguminosae). The structures of 1 and 2 were determined to be 3-O-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl caulophyllogenin 28-O-...

journal_title：Chemical & pharmaceutical bulletin

authors： Kinjo J,Uemura H,Nakamura M,Nohara T

更新日期：1994-06-01 00:00:00

abstract：:In an investigation of a new class of deoxyribonucleic acid (DNA)-intercalating antitumor agents, novel acridinyl-substituted uracils have been synthesized and evaluated for activity against L1210 leukemia in vivo, and against bacteria and fungus. These compounds were prepared by the novel enamine reaction between 9-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Kimura M,Okabayashi I,Kato A

更新日期：1989-03-01 00:00:00

abstract：:Two enkephalin-containing peptides, peptide E and dynorphin(1-24), were synthesized by conventional solution methods employing a new Trp derivative, Nin-(2,4,6-triisopropylphenylsulfonyl)tryptophan [Trp(Tps)]. All protecting groups employed including the Tps group were removed by treatment with 1 M trifluoromethanesul...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa K,Kawamoto T,Futaki S,Kiyama S,Akita T,Moritoki H,Kiso Y

更新日期：1989-10-01 00:00:00

abstract：:Three new acylated flavonol glycosides, cypellogins A (1), B (2) and C (3), along with eight known phenolic compounds, were isolated from the dried leaves of Eucalyptus cypellocarpa, and their structures were elucidated using spectroscopic methods, including 2D NMR experiments and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kasajima N,Ito H,Hatano T,Yoshida T,Kaneda M

更新日期：2005-10-01 00:00:00

abstract：:Four new bicyclic hexapeptides, named as RA-XI, -XII, XIII and -XIV were isolated from Rubia cordifolia and showed potent antitumor activities against P-388. The structures were elucidated from spectroscopic and chemical evidences. RA-XII, XIII and -XIV were proved to be unique bicyclic hexapeptidic glucosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Yamamiya T,Takeya K,Itokawa H

更新日期：1992-05-01 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：:A series of optically active substituted 1,2-dihydro-6-oxo-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids was prepared via optically active 2-methyl-4,5-difluoroindoline (10) and tested for antibacterial activities. Among them, (2S)-9-[(3R,1'S)-3-(1'-amino)ethyl-1-pyrrolidinyl]-8-fluoro-1,2-dihydro- 2- methyl-6-oxo-6H-...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsuji K,Tsubouchi H,Ishikawa H

更新日期：1995-10-01 00:00:00

abstract：:A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The "in vitro" antibacterial activity of these compounds and their corresponding alpha-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobi...

journal_title：Chemical & pharmaceutical bulletin

authors： Rival Y,Grassy G,Michel G

更新日期：1992-05-01 00:00:00

abstract：:Novel saponins that retain a free carboxyl group at the C-17 position and various sugars linked at the C-3 position of hederagenin aglycone were synthesized via stereospecific glycosylation. Since these natural products represented by Pulsatilla saponin D (PSD) were obtained in very small amounts, the total synthesis ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim M,Park Y,Chung WY,Park KK,Jung M

更新日期：2015-01-01 00:00:00

abstract：:Possible utility of hydroxyalkylated beta-cyclodextrin (beta-CyD) derivatives as parenteral drug carriers was investigated, using nimodipine, a dihydropyridine derivative with calcium antagonistic action, as a model drug. The aqueous solubility of nimodipine increased linearly with increase in the concentration of hyd...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida A,Yamamoto M,Itoh T,Irie T,Hirayama F,Uekama K

更新日期：1990-01-01 00:00:00

abstract：:Three new cardiac glycosides named cheiranthoside VIII (1), cheiranthoside IX (2) and cheiranthoside X (3) were isolated from the seeds of Erysimum cheiranthoides. Based on spectroscopic data, the structures of 1-3 were characterized as strophanthidin 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-antiaropyranoside, cheiran...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei ZH,Nakayama H,Kuniyasu A,Tai BS,Nohara T

更新日期：2002-06-01 00:00:00

abstract：:α,β-Unsaturated amides were incorporated as viable dipolarophiles in a catalytic asymmetric 1,3-dipolar cycloaddition of azomethine imines. The use of a 7-azaindoline auxiliary was essential to acquire sufficient reactivity with excellent diastereoselectivity, likely due to the chelating activation of the amide by the...

journal_title：Chemical & pharmaceutical bulletin

authors： Li Z,Kumagai N,Shibasaki M

更新日期：2020-01-01 00:00:00

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：:An effective procedure for decontamination of beta-lactam antibiotic residues or contaminants in the pharmaceutical manufacturing environment was investigated. Decontamination with solutions of hydrochloric acid, sodium hydroxide, hydrogen peroxide and hydroxylamine as agents for degradation was assessed. According to...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukutsu N,Kawasaki T,Saito K,Nakazawa H

更新日期：2006-09-01 00:00:00