Synthesis and evaluation of novel 2-oxo-1,2-dihydro-3-quinolinecarboxamide derivatives as serotonin 5-HT4 receptor agonists.

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：:Four new aromatic constituents, rhododendroketoside, (-)-sakuraresinoside, acernikol, and nikoenoside, were isolated from a Japanese folk medicine, the stem bark of Acer nikoense MAXIM. The structures of the new constituents were determined on the basis of chemical and physicochemical evidence. The principle cyclic di...

journal_title：Chemical & pharmaceutical bulletin

authors： Morikawa T,Tao J,Ueda K,Matsuda H,Yoshikawa M

更新日期：2003-01-01 00:00:00

abstract：:Direct beta-glucosidation between benzyl alcohol and D-glucose (5) using the immobilized beta-glucosidase from almonds with the synthetic prepolymer ENTP-4000 gave a benzyl beta-D-glucoside (1) in 53% yield. The coupling of the benzyl beta-D-glucopyranoside congener (8) derived from 1 with phenyl 2,3,4-tri-O-acetyl-1-...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawahara E,Fujii M,Kato K,Ida Y,Akita H

更新日期：2005-08-01 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

abstract：:Four new minor saponins, papyrioside LE-LH, were isolated from the leaves of Tetrapanax papyriferum, and their structures were determined on the basis of spectroscopic evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mutsuga M,Kojima K,Saracoglu I,Ogihara Y

更新日期：1997-03-01 00:00:00

abstract：:Four new neo-clerodane diterpenoid alkaloids, named scutebarbatines C-F (1-4), were isolated from the whole plants of Scutellaria barbata D. DON. Their structures were elucidated by spectral analyses (UV, IR, FAB-MS, 1D-NMR and 2D-NMR). In vitro, compounds 1-4 showed significant cytotoxic activities against three huma...

journal_title：Chemical & pharmaceutical bulletin

authors： Dai SJ,Chen M,Liu K,Jiang YT,Shen L

更新日期：2006-06-01 00:00:00

abstract：:Two new cycloartane glycosides, named aquilegiosides K and L, have been isolated from the dried underground parts of Aquilegia vulgaris. Their structures were determined by two dimensional (2D) NMR spectroscopic analysis and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshimitsu H,Nishida M,Nohara T

更新日期：2008-11-01 00:00:00

abstract：:(±)-8-Deisopropyladunctin B, the deisopropyl form of adunctin B, which was isolated from the leaves of Piper aduncum (Piperaceae) collected in Papua New Guinea, was synthesized in 0.77% overall yield in 17 steps from 5,7-dimethoxycoumarin-3-carboxylate. The key step was our original stereoconvergent skeleton transform...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomura S,Arimitsu K,Yamaguchi S,Kosuga Y,Kakimoto Y,Komai T,Hasegawa K,Nakanishi A,Miyoshi T,Iwasaki H,Ozeki M,Kawasaki I,Kurume A,Ohta S,Yamashita M

更新日期：2012-01-01 00:00:00

abstract：:Improvement of solubility for fullerene (C60) was studied by cogrinding with cycloamyloses using a ball mill in the solid state. Cycloamylose is a novel cyclic alpha-1,4-glucan produced from synthetic amylose by enzymatic reaction. Although sample solutions showed a pale yellow for the initial period of cogrinding wit...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukami T,Mugishima A,Suzuki T,Hidaka S,Endo T,Ueda H,Tomono K

更新日期：2004-08-01 00:00:00

abstract：:A new pentacyclic cucurbitane glucoside, named aoibaclyin (1) and a new triterpene (2) have been isolated from the EtOH extract of the fruits of Gymnopetalum integrifolium Kurz (Cucurbitaceae), together with three known compounds, bryoamaride (3), 25-O-acetylbryoamaride (4) and beta-sitosterol 3-O-beta-D-glucopyranosi...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekine T,Kurihara H,Waku M,Ikegami F,Ruangrungsi N

更新日期：2002-05-01 00:00:00

abstract：:Two new pyrrole oligoglycosides, plancipyrrosides A and B (1 and 2), were isolated from methanol extract of the Vietnamese starfish Acanthaster planci using various chromatographic procedures. Their structures were elucidated by spectroscopic methods including one and two dimensional (1D- and 2D)-NMR and Fourier trans...

journal_title：Chemical & pharmaceutical bulletin

authors： Vien LT,Hanh TT,Huong PT,Dang NH,Thanh NV,Lyakhova E,Cuong NX,Nam NH,Kiem PV,Kicha A,Minh CV

更新日期：2016-11-01 00:00:00

abstract：:Scale-up of wet granulation in a vertical high shear mixer was conducted. Pharmaceutical excipient powders composed of lactose, cornstarch and micro-crystallinecellulose, and hydroxypropylcellulose as a binder were mixed together and then granulated with purified water under various operating conditions and vessel sca...

journal_title：Chemical & pharmaceutical bulletin

authors： Watano S,Okamoto T,Sato Y,Osako Y

更新日期：2005-04-01 00:00:00

abstract：:When phenylalanine was irradiated at ultraviolet (UV) light, p-tyrosine, m-tyrosine and o-tyrosine were identified as hydroxylated products. From p-tyrosine and m-tyrosine, the formation of L-3,4-dihydroxyphenylalanine (DOPA) was observed. The hydroxylation of phenylalanine was prevented by radical scavengers, e.g., c...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishimitsu S,Fujimoto S,Ohara A

更新日期：1990-05-01 00:00:00

abstract：:Seven halogenated derivatives of delta 9-tetrahydrocannabinol (delta 9-THC, 1) substituted on the aromatic ring at the 2 and/or 4 position, 2 (4)-fluoro- (2), 2,4-difluoro- (3), 2-chloro- (4), 2-bromo- (5), 2,4-dibromo- (6), 2-iodo- (7) and 2,4-diiodo-delta 9-THC (8) were synthesized and pharmacological effects such a...

journal_title：Chemical & pharmaceutical bulletin

authors： Usami N,Kobana K,Yoshida H,Kimura T,Watanabe K,Yoshimura H,Yamamoto I

更新日期：1998-09-01 00:00:00

abstract：:From the air-dried roots of Glycyrrhiza uralensis Fischer collected in Xinjiang province, China ("Shinkyo-Kanzo" in Japanese), a new oleanene-type triterpene oligoglycoside named licorice-saponin L3 and a new chalcone oligoglycoside named isoliquiritin apioside were isolated together with glycyrrhizin, 18 alpha-glycyr...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa I,Hori K,Uchida E,Chen WZ,Yoshikawa M,Ren J

更新日期：1993-09-01 00:00:00

abstract：:The percutaneous penetration of R-(+)- and S-(-)-propranolol (PL) through rat excised skin was investigated in vitro. The flux of S-(-)-PL after application to normal skin was high compared with that of R-(+)-PL. On the other hand, in damaged rat skin, the flux of R-(+)-PL was almost equivalent to that of S-(-)-PL. It...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki K,Kaiho F,Inagaki A,Dohi M,Hazemoto N,Haga M,Hara H,Kato Y

更新日期：1992-04-01 00:00:00

abstract：:The analysis of genotoxic impurities (GTIs) in active pharmaceutical ingredients (APIs) is a challenging task. The target detection limit (DL) in an API is typically around 1 ppm (1 µg/g API). Therefore, a sensitive and selective analytical method is required for their analysis. 4-Chloro-1-butanol, an alkylating agent...

journal_title：Chemical & pharmaceutical bulletin

authors： Harigaya K,Yamada H,Yaku K,Nishi H,Haginaka J

更新日期：2014-01-01 00:00:00

abstract：:To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng XW,Huang N,Xu H,Yang WB,Yang LM,Qu H,Zheng YT

更新日期：2010-07-01 00:00:00

abstract：:Oral gel formulations are known as easy to administer drug products for patients who have problems taking drugs including those with conditions such as dysphagia. In addition, there are numerous commercially available oral gel products, most of which are immediate-release formulation that release their pharmaceutical ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hishikawa Y,Kakino Y,Tsukamoto H,Tahara K,Onodera R,Takeuchi H

更新日期：2016-01-01 00:00:00

abstract：:The effect of chromomycin A3 binding on the geometry of DNA duplex (plasmid pBR322) has been examined using topoisomerase I relaxation followed by gel electrophoresis. To determine the equilibrium constant of this drug-DNA binding-dissociation reaction in the same concentration range (ca. 10(-5) M) in the same buffer ...

journal_title：Chemical & pharmaceutical bulletin

authors： Utsuno K,Kojima K,Maeda Y,Tsuboi M

更新日期：1998-11-01 00:00:00

abstract：:Some (piperidinomethylene)bis(phosphonic acid) derivatives were prepared and their activity to inhibit a rise in serum calcium induced by parathyroid hormone in thyroparathyroidectomised rats was evaluated. Several (4-alkylidene-, 4,4-dialkyl-, or 4-alkyl-4-halopiperidinomethylene)bis(phosphonic acid) derivatives show...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimura M,Hayashida M,Nomiyama K,Ikegami S,Iida Y,Tamura M,Hiyama Y,Ohishi Y

更新日期：1993-11-01 00:00:00

abstract：:An improved chemical reaction protocol with short time and easy work-up was described here for 2-phenylbenzofuran derivatives. The final purified products, 2-phenylbenzofuran derivatives 5a-g and the intermediate diols 4a-g, were evaluated for their estrogen receptor (ER) binding affinity and selective activity in vit...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang P,Yang Y,Zheng X,Huang W,Ma Z,Shen Z

更新日期：2012-01-01 00:00:00

abstract：:Total synthetic studies on natural products with promising biological profiles, coupled with their intriguing structural features, are described. The target molecules dealt with in this article are five helianane-type sesquiterpenes (heliannuols A, D and K and heliespirones A and C) and three meroterpenes (breviones A...

journal_title：Chemical & pharmaceutical bulletin

authors： Shishido K

更新日期：2013-01-01 00:00:00

abstract：:Stereoisomers of thiol proteinase inhibitor (TPI) were synthesized by a conventional solution method. Among them, iNoc-D-Gln-Val-Val-Ala-Ala-pNA weakly inhibited the amidolytic activity of papain, although iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited papain activity fairly potently. However, the other five D-amino acid-cont...

journal_title：Chemical & pharmaceutical bulletin

authors： Iguchi S,Hirano K,Okamoto H,Okamoto Y,Okada Y

更新日期：1996-08-01 00:00:00

abstract：:Chemical investigation of the soft coral Sinularia leptoclados has afforded three new sesquiterpenoids, leptocladols A (1), B (2), and 1-epi-chabrolidione A (3). The relative structures of 1-3 were determined on the basis of extensive spectroscopic analysis. The relative configuration of 1 was further confirmed by a s...

journal_title：Chemical & pharmaceutical bulletin

authors： Su JH,Chiang MY,Wen ZH,Dai CF,Hsu CH,Sheu JH

更新日期：2010-02-01 00:00:00

abstract：:A series of 43 stilbene derivatives that showed cytotoxicity against human lung carcinoma (A549) was analyzed using comparative molecular field analysis (CoMFA) for defining the hypothetic pharmacophore model. The polyoxylated stilbenes were found to be active inhibitors of tubulin polymerization. Several cis-stilbene...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim S,Min SY,Lee SK,Cho WJ

更新日期：2003-05-01 00:00:00

abstract：:To find candidates with high antimicrobial and low hemolytic activities, many gramicidin S (GS) analogs of various ring sizes have been designed and synthesized. However, syntheses of antimicrobially active analogues of GS having a disordered symmetry structure from C(2) have almost never been reported, because the st...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamaki M,Takanashi K,Harada T,Fujinuma K,Shindo M,Kimura M,Uchida Y

更新日期：2011-01-01 00:00:00

abstract：:Arginine vasopressin (AVP) has a dual action mainly in the periphery, i.e., vasoconstriction and water reabsorption via V1A and V2 receptors; it may play a role in a number of diseases, including congestive heart failure (CHF), hypertension, renal disease, edema, and hyponatremia. We have attempted to develop a new se...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuhisa A,Taniguchi N,Koshio H,Yatsu T,Tanaka A

更新日期：2000-01-01 00:00:00

abstract：:To investigate the possible mechanism of the stimulatory effect of a hot water extract from Artemisia leaf (Artemisia princeps PANPANINI) (AFE) on the proliferation of endothelial cells, cells from bovine aorta were cultured for 72 h in RPMI1640 medium supplemented with 10% fetal calf serum in the presence of 5 microg...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaji T,Kaga K,Miezi N,Hayashi T,Ejiri N,Sakuragawa N

更新日期：1990-09-01 00:00:00

abstract：:Chemical examination of a Chinese soft coral Lobophytum pauciflorum resulted in the isolation of seven new biscembranoids, named lobophytones H-N (1-7). Their structures were determined by interpretation of 1D- and 2D-NMR (correlation spectroscopy (COSY), heteronuclear single quantum coherence (HSQC), heteronuclear mu...

journal_title：Chemical & pharmaceutical bulletin

authors： Yan P,Deng Z,van Ofwegen L,Proksch P,Lin W

更新日期：2010-12-01 00:00:00