Structures and solid state tautomeric forms of two novel antileukemic tropoloisoquinoline alkaloids, pareirubrines A and B, from Cissampelos pareira.

abstract：:To improve the oral bioavailability of a dermorphin tetrapeptide analog, N(alpha)-1-iminoethyl-Tyr-D-MetO-Phe-MebetaAla-OH (III), which has a potent analgesic activity after oral administration, various derivatives were synthesized to increase lipophilicity by esterification of the C-terminal carboxyl group and/or acy...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawa T,Araki M,Miyamae T,Okayama T,Hagiwara M,Sakurada S,Morikawa T

更新日期：2003-07-01 00:00:00

abstract：:A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PA...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki H,Ogiku T,Sai H,Moritani Y,Ohtani A,Ohmizu H

更新日期：2009-09-01 00:00:00

abstract：:The methanolic extracts from the wood and bark of Cotylelobium melanoxylon were found to inhibit plasma glucose elevation after sucrose loading in rats and triglyceride elevation after olive oil loading in mice. A new stilbene dimer, melanoxylin A, together with the known stilbene dimers [(+)-ampelopsin F, (+)-isoampe...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuda H,Asao Y,Nakamura S,Hamao M,Sugimoto S,Hongo M,Pongpiriyadacha Y,Yoshikawa M

更新日期：2009-05-01 00:00:00

abstract：:Novel neutral glycosphingolipids isolated from the plerocercoids of a tapeworm, Spirometra erinacei, may be expected to be involved in host-parasite interactions. We have synthesized this glycosphingolipid analogue containing 2-branched fatty alkyl residue in place of ceramide. Glycosylation of nonreducing-end trisacc...

journal_title：Chemical & pharmaceutical bulletin

authors： Hada N,Kuroda M,Takeda T

更新日期：2000-08-01 00:00:00

abstract：:Three new monoterpenoids, called genipacetal, genipamide, and genipaol, were isolated from the fruit of Genipa americana L. (Rubiaceae), along with the four known iridoids genipin, gardendiol, deacetyl asperulosidic acid methyl ester, and shanzhiside. Their chemical structures were determined on the basis of spectrosc...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Ishimatsu N,Masuoka C,Yoshimitsu H,Tsuchihashi R,Okawa M,Kinjo J,Ikeda T,Nohara T

更新日期：2007-04-01 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：:Two monomethylated GM(3)-Type ganglioside molecular species, 1 and 2, have been obtained from the polar lipid fraction of the chloroform/methanol extract of the starfish Luidia maculata. The structures of these gangliosides have been determined on the basis of chemical and spectroscopic evidence as 1-O-[8-O-methyl-(N-...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawatake S,Inagaki M,Isobe R,Miyamoto T,Higuchi R

更新日期：2002-10-01 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：: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：:Three new limonoids, cipadesins D--F (1--3), together with 8,15-dihydroxy-13E-labdane, beta-sitosterol and beta-daucosterol, were isolated from the leaves and bark of Cipadessa cinerascens. Their structures were elucidated by spectral evidence. X-Ray crystallographic analysis confirmed the structure of 1. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yuan XH,Li BG,Xu CX,Zhou M,Qi HY,Zhang GL

更新日期：2007-06-01 00:00:00

abstract：:New five seven-membered vibsane-type diterpenes named 5-epi-vibsanin C, 5-epi-vibsanin H, 5-epi-vibsanin K, 18-O-methyl-5-epi-vibsanin K and 5-epi-vibsanin E have been isolated from the leaves of Viburnum awabuki (Caplifoliaceae). Their structures have been elucidated by analyses of spectroscopic data and comparison o...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Minami H,Matsuo A,Kitamura K,Akizuki M,Kubo M,Kodama M

更新日期：2002-03-01 00:00:00

abstract：:Several kinds of loline-type alkaloids, norloline, loline, N-acetylnorloline, N-acetylloline, N-formylnorloline, N-formylloline and N-methylloline were detected in the urine of race-horses. Furthermore, a new compound of the alkaloids, N-senecioylnorloline, was also found and identified. These compounds were mainly id...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeda A,Suzuki E,Kamei K,Nakata H

更新日期：1991-04-01 00:00:00

abstract：:The complete amino acid sequence of a new abortifacient protein, karasurin, was determined. Karasurin, which was isolated from fresh root tubers of Trichosanthes kirilowii Maximowicz var, japonicum Kitamura (Cucurbitaceae), was a highly basic protein with pI 10.1 and molecular weight of 28,000. Intact karasurin was cl...

journal_title：Chemical & pharmaceutical bulletin

authors： Toyokawa S,Takeda T,Kato Y,Wakabayashi K,Ogihara Y

更新日期：1991-05-01 00:00:00

abstract：:A novel macrocyclic diterpene, jatrophenone, has been isolated from the whole plant of Jatropha gossypifolia. The structure of the compound was established by detailed studies of its one- and two-dimensional (1D and 2D) NMR spectra. The compound possesses significant antibacterial activity. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ravindranath N,Venkataiah B,Ramesh C,Jayaprakash P,Das B

更新日期：2003-07-01 00:00:00

abstract：:Virulence (vir) gene expression of Agrobacterium tumefaciens is activated by plant phenolic compounds such as alpha-hydroxyacetosyringone (HOAS), acetosyringone (AS), methyl syringate, coniferyl alcohol and sinapyl alcohol. Inositol was found to be a potentiating factor of vir-inducing activity, which enhanced the vir...

journal_title：Chemical & pharmaceutical bulletin

authors： Song YN,Shibuya M,Ebizuka Y,Sankawa U

更新日期：1991-10-01 00:00:00

abstract：:A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted-1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydr...

journal_title：Chemical & pharmaceutical bulletin

authors： Megally Abdo NY,Kamel MM

更新日期：2015-01-01 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：:An efficient synthesis of 5-bromo-2-methoxy-6-methylaminopyridine-3-carboxylic acid (1), a carboxylic acid moiety of a potent dopamine D2 and D3 and serotonin-3 (5-HT3) receptors antagonist, (R)-5-bromo-N-(1-ethyl-4-methylhexahydro-1 ,4-diazepin-6-yl)-2-methoxy-6-methylaminopyridine-3-carboxamide, is described. Reacti...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirokawa Y,Horikawa T,Kato S

更新日期：2000-12-01 00:00:00

abstract：:A novel series of 2-acyl-3-carboxyl-tetrahydroisoquinoline derivatives were synthesized and biologically evaluated. Among them, (S)-2-{(E)-3-furan-2-ylacryloyl}-7-[(2E,4E)-5-(2,4,6-trifluorophenyl)penta-2,4-dienyloxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (compound 17u) was identified as a potent protein ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Morishita K,Shoji Y,Fukui M,Ito Y,Kitao T,Ozawa SI,Hirono S,Shirahase H

更新日期：2018-01-01 00:00:00

abstract：:A new flavonol triglycoside, isorhamnetin 3-O-beta-D-xylopyranosyl-(1"-->3)-alpha-L-rhamnopyranosyl-(1'''-->6")-beta-D-galactopyranoside, has been isolated from the leaves of Hammada scoparia together with two known compounds, isorhamnetin 3-O-beta-D-apiofuranosyl-(1'''-->2")[alpha-L-rhamnopyranosyl-(1"-->6")]-beta-D-...

journal_title：Chemical & pharmaceutical bulletin

authors： Ben Salah H,Jarraya R,Martin MT,Veitch NC,Grayer RJ,Simmonds MS,Damak M

更新日期：2002-09-01 00:00:00

abstract：:Four acyclic diterpene glycosides were extracted from Habanero, the fruits of Capsicum chinense JACQ., which is known as one of the hottest peppers in existence. Two of these glycosides were identified as capsianoside XIII and capsianoside XV. The other two were new ones and were characterized as 3-O-beta-D-glucopyran...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee JH,El-Aasr M,Ikeda T,Oda K,Miyashita H,Yoshimitsu H,Okawa M,Kinjo J,Nohara T

更新日期：2009-07-01 00:00:00

abstract：:The purpose of this study was to predict the stability of imipenem in a mixed infusion. The hydrolysis of imipenem in aqueous solution was found to be accelerated by pH, and by increasing concentrations of sodium bisulfite (SBS) and L-cysteine. Equations were derived for the degradation rate constants (k(obs)) of pH, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Takasu Y,Shimizu K,Asahara K,Uchida T

更新日期：2013-01-01 00:00:00

abstract：:Two efficient and practical methods of synthesis of the C-10 substituent of DV-7751 (1), a novel quinolone carboxylic acid, were established. The first method utilizes an optical resolution of racemic 8-amino-6-benzyl-6-azaspiro[3.4]octane (13), while the second employs an enantioselective microbial reduction of 6-ben...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyadera A,Satoh K,Imura A

更新日期：2000-04-01 00:00:00

abstract：:A series of 5-(4-aryl- or 4-arylcarbonylpiperazin-1-yl)-5-deoxy-1,4: 3,6-dianhydro-L-iditol 2-nitrates was prepared in order to obtain orally active, nitrate-type vasodilators with reduced side effects. Our drug design was based on a small reduction in the lipophilicity compared to that of 5-deoxy-5-[4-(3-phenylthiopr...

journal_title：Chemical & pharmaceutical bulletin

authors： Hayashi H,Ikeda J,Kubo K,Moriyama T,Karasawa A,Suzuki F

更新日期：1993-06-01 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：:Two new iridoid glycosides, 7 beta,8 beta-epoxy-8 alpha-dihydrogeniposide (1) and 8-epiapodantheroside (2), were isolated, together with six known (3-8) and three artifact (9-11) iridoids, from the leaves of Gardenia jasminoides cv. fortuneana Hara. Their structures were established based on chemical and spectral data...

journal_title：Chemical & pharmaceutical bulletin

authors： Machida K,Takehara E,Kobayashi H,Kikuchi M

更新日期：2003-12-01 00:00:00

abstract：:Increase of lipophilicity of cationic doxorubicin (DOX) by its association with a fatty acid ion is of interest for pharmaceutical formulations and could have an impact on the drug delivery into cancer cells. On the basis of spectroscopic analysis of intrinsic DOX fluorescence, this study provides an experimental evid...

journal_title：Chemical & pharmaceutical bulletin

authors： Munnier E,Tewes F,Cohen-Jonathan S,Linassier C,Douziech-Eyrolles L,Marchais H,Soucé M,Hervé K,Dubois P,Chourpa I

更新日期：2007-07-01 00:00:00

abstract：:The density of hydroxyl radicals (·OH) produced in aqueous samples by exposure to X-ray or carbon-ion beams was investigated. The generation of ·OH was detected by the electron paramagnetic resonance (EPR) spin-trapping technique using 5,5-dimethyl-1-pyrroline-N-oxide (DMPO) as the spin-trapping agent. When the concen...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto K,Ueno M,Nakanishi I,Anzai K

更新日期：2015-01-01 00:00:00

abstract：:The anti-anginal drug Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, is thought to modulate the metabolism during myocardial ischemia by activating pyruvate dehydrogenase activity to promote glucose oxidation. Ranolazine and its five principal metabolites: CVT-2512, CVT-2513, CVT-2514, CVT-2738 and CVT-4...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao Z,Gong S,Guan T,Li Y,Wu X,Sun H

更新日期：2009-11-01 00:00:00

abstract：:This paper describes syntheses and doxorubicin-inclusion abilities of beta-cyclodextrin (CyD) derivatives with a hydroquinone alpha-glycoside residue attached at the primary side. The hydroquinone glycoside having an alpha-D-glucosidic or 2-acetamido-2-deoxy-alpha-D-glucosidic linkage became a useful component for pro...

journal_title：Chemical & pharmaceutical bulletin

authors： Oda Y,Miura M,Hattori K,Yamanoi T

更新日期：2009-01-01 00:00:00