Antirheumatic agents. I. Novel methotrexate derivatives bearing an indoline moiety.

abstract：:Thioglycosides are available donors in glycosylation due to the stability of the anomeric C-S bond under general reaction conditions of protection and deprotection, and offer orthogonality in their activation. We report now that the hypervalent iodine effectively induced glycosylation reaction of thioglycosides with v...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajimoto T,Morimoto K,Ogawa R,Dohi T,Kita Y

更新日期：2016-01-01 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：: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：:From the water extract of Brazilian Tabebuia avellanedae, two new iridoids (1, 2) and a new phenylethanoid glycoside (3) have been isolated together with twelve known compounds (4-15). Their structures were determined based on the spectroscopic data. The isolated compounds inhibited nitric oxide (NO) production in lip...

journal_title：Chemical & pharmaceutical bulletin

authors： Awale S,Kawakami T,Tezuka Y,Ueda JY,Tanaka K,Kadota S

更新日期：2005-06-01 00:00:00

abstract：:The competitive inclusion complexations in the ternary phenacetin/competitors/beta-cyclodextrin (beta-CyD) systems were investigated by the solubility method, where m-bromobenzoic acid (m-BBA) and o-toluic acid (o-TA) were used as competitors. The solubility changes of the drug and competitors as a function of beta-Cy...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono N,Hirayama F,Arima H,Uekama K

更新日期：2001-01-01 00:00:00

abstract：:Interaction between Mn2+ ion and the two forms of DNA duplex (supercoiled and linearized pUC119 DNA) in solution has been examined by isothermal titration calorimetry. Although DNA condensation reaction heat was observed at 323 K, this was not the case at 298 K. DNA condensation was entropically driven and supercoiled...

journal_title：Chemical & pharmaceutical bulletin

authors： Utsuno K

更新日期：2008-03-01 00:00:00

abstract：:Total syntheses of structurally and biologically intriguing natural products relying on new synthetic methodologies are described. This article features cinchona alkaloid-catalyzed asymmetric Morita-Baylis-Hillman reactions, heterocycle syntheses based on rhodium-catalyzed C-H amination and indium-catalyzed Conia-ene ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hatakeyama S

更新日期：2014-01-01 00:00:00

abstract：:From the most polar fractions of Solidago virga-aurea L. (Compositae), 9 oleanane-type triterpene saponins named solidagosaponins XXI-XXIX (1-9) were isolated, together with a known saponin, virgaureasaponin 2 (10). These saponins are bisdesmosidic glycosides having two monosaccharides at C-3 and four or five monosacc...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyase T,Inose Y,Ueno A

更新日期：1994-03-01 00:00:00

abstract：:Four new compounds 1-4 were obtained from an oxidative coupling reaction of (E)-isorhapontigenin using FeCl(3) as oxidant. Their structures and stereochemistry were determined on the basis of spectroscopic evidence [UV, IR, MS, (1)H-, (13)C-NMR, NOE and 2D NMR], and their possible formation mechanisms were also discus...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao CS,Zhou LX,Lin M

更新日期：2004-02-01 00:00:00

abstract：:We describe here (2+2) cycloaddition reaction of alkyl enol ethers with acrylates catalyzed by triethylsilyl triflic imide (Et3SiNTf2), which was in situ generated from triethylsilane and triflic imide. The reaction efficiently provides substituted cyclobutanes bearing alkoxy function in a stereoselective manner. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takasu K,Miyakawa Y,Ihara M,Tokuyama H

更新日期：2008-08-01 00:00:00

abstract：:Five new components, named multiforisins A, B, C, D, and E, with immunosuppressive activity were isolated from an Ascomycete, Gelasinospora multiforis. Multiforisin A, the main immunosuppressive principle of this fungus, was deduced to be 5-formyl-3-(hydroxymethyl)-4-methoxy-6-(1E-propenyl)-alpha-pyrone. Multiforisins...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujimoto H,Satoh Y,Nakayama M,Takayama T,Yamazaki M

更新日期：1995-04-01 00:00:00

abstract：:The analgesic components were isolated from a Bornean medicinal plant, Tabernaemontana pauciflora Blume (syn. Ervatamia blumeana Mark gr.), and the major components were identified as coronaridine and 3-(2-oxopropyl)coronaridine. Four minor components were estimated to be 5R- and 5S-(2-oxopropyl)coronaridine, 3-(2-oxo...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuyama E,Gao LH,Yamazaki M

更新日期：1992-08-01 00:00:00

abstract：:Nonenzymatically glycated human serum albumin was incubated with ferric ion at 37 degrees C in 0.2 M phosphate buffer, pH 7.4, up to 30 days. In the incubation mixture, amino acids, tyrosine and phenylalanine, were detected, suggesting site specific cleavage of glycated human serum albumin. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai T,Takanashi M,Tsuchiya S

更新日期：1992-06-01 00:00:00

abstract：:We discovered that the reactivity of some conjugated and electron-deficient hydrocarbons was quite different in the presence of transition metal catalysts. In this review we report our development and applications of the highly selective palladium and nickel-catalyzed cycloaddition reactions of unsaturated hydrocarbon...

journal_title：Chemical & pharmaceutical bulletin

authors： Saito S

更新日期：2005-09-01 00:00:00

abstract：:Intramolecular [2+2] cycloaddition of γ,δ-unsaturated ketenes derived from hex-5-enoyl chloride derivatives gave bicyclo[2.1.1]hexan-5-ones with complete regioselectivity. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hoshikawa T,Tanji K,Matsuo J,Ishibashi H

更新日期：2012-01-01 00:00:00

abstract：:The biomimetic oxidation of curcumin, a main turmeric pigment with hydrogen peroxide catalyzed by different 5,10,15,20-tetraarylporphyrinatoiron(III) chlorides [TAPFe(III)Cl] in dichloromethane has been studied to give a C-C coupled curcumin dimer in 40-70% yield. The structure of the dimer has been elucidated by (1)H...

journal_title：Chemical & pharmaceutical bulletin

authors： Chauhan SM,Kandadai AS,Jain N,Kumar A

更新日期：2003-11-01 00:00:00

abstract：:We designed and synthesized a new class of peptidomimetic human immunodeficiency virus protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl isostere as the active moiety. From a structure-activity relatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimoto T,Hattori N,Takaku H,Kisanuki S,Fukazawa T,Terashima K,Kato R,Nojima S,Misawa S,Ueno T,Imai J,Enomoto H,Tanaka S,Sakikawa H,Shintani M,Hayashi H,Kiso Y

更新日期：2000-09-01 00:00:00

abstract：:The biotransformation of 2α,5α,10β-triacetoxy-14-oxo-taxa-4(20),11-diene (1) by cultured Gingko cells afforded four products. Their structures were identified on the basis of analyses of the chemical and spectroscopic (IR, MS, ¹H- and ¹³C-NMR) data. Among them, 2, 3 and 5 were three new compounds, and 4 displayed pote...

journal_title：Chemical & pharmaceutical bulletin

authors： Xie D,Zhang Y,Zou J,Yin D,Chen X,Dai J

更新日期：2011-01-01 00:00:00

abstract：:Polymorphic behaviours of paracetamol and propyphenazone and interaction between these two compounds were investigated using differential scanning calorimetry (DSC), X-ray powder diffraction and Fourier transform-infrared (FT-IR)-spectroscopy. Binary mixtures containing various ratios of the compounds were prepared as...

journal_title：Chemical & pharmaceutical bulletin

authors： Zalac S,Khan MZ,Gabelica V,Tudja M,Mestrović E,Romih M

更新日期：1999-03-01 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：:The effect of propranolol (PPL), phenoxybenzamine (PBZ) or bicuculline (BCL) on the diazepam (DZP)-induced changes of pineal melatonin synthesis in male rats was examined in vivo and in vitro. Administration of PBZ did not affect the inhibitory action of DZP on pineal melatonin synthesis in vivo. A single injection of...

journal_title：Chemical & pharmaceutical bulletin

authors： Wakabayashi H,Shimada K,Satoh T

更新日期：1991-10-01 00:00:00

abstract：:Chemical investigation of the seeds of Adonis aestivalis has led to the isolation of a new cardenolide (3β,5α,14β,17β-tetrahydroxycard-20,22-enolide) (1), two new glycosides (2, 3) of 1, and a new strophanthidin hexaglycoside (4), together with a known compound, strophanthidin 3-O-β-D-glucopyranoside (5). The structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubo S,Kuroda M,Matsuo Y,Masatani D,Sakagami H,Mimaki Y

更新日期：2012-01-01 00:00:00

abstract：:A novel fucan sulfate (Hor-1) was isolated from the hot water extract of an edible brown alga, Sargassum horneri (Turner) C. Agardh. The fucan sulfate was revealed to have sugar linkage types, sulfate content and uronic acid content different from those of sodium hornan (Na-HOR), another fucan sulfate isolated from th...

journal_title：Chemical & pharmaceutical bulletin

authors： Preeprame S,Hayashi K,Lee JB,Sankawa U,Hayashi T

更新日期：2001-04-01 00:00:00

abstract：:A novel C-methylated biflavone, taiwanhomoflavone-B (1), together with known compounds, 7,4',7"-tri-O-methylamentoflavone, 6-C-methylnaringenin and apigenin-7-O-beta-glucoside were isolated from an ethanolic extract of Cephalotaxus wilsoniana. The structure of 1 was elucidated on the basis of spectroscopic analysis. T...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Hwang SY,Yang Kuo LM,Lee YL,Li SY,Shen YC

更新日期：2002-12-01 00:00:00

abstract：:N-1 and N-2 substituted pyrazolo[4,5-g]pyrido[1,2-a]benzimidazoles were prepared regioselectively, and cytotoxicities evaluated in vitro against K562 and HL60 cells. All compounds displayed weaker activity than doxorubicin against sensitive lines, but showed the same activity against resistant cell lines (multidrug re...

journal_title：Chemical & pharmaceutical bulletin

authors： Dupuy M,Pinguet F,Blache Y,Chavignon O,Teulade JC,Chapat JP

更新日期：1998-11-01 00:00:00

abstract：:The tandem action of serine protease (alpha-chymotrypsin or subtilisin BPN') and Aspergillus genus aminoacylase on racemic N-acetyl-alpha-aminoalkanedioic acid alpha,omega-diester produced L-alpha-aminoalkanedioic acid omega-ester in good yield and high optical purity. L-alpha-Aminosuberic acid omega-ester thus obtain...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishino N,Arai T,Ueno Y,Ohba M

更新日期：1996-01-01 00:00:00

abstract：:A new cyclic tetrapeptide (1), along with known congeners (2, 3), was isolated from the fungus Phoma sp. derived from the giant jellyfish Nemopilema nomurai. The absolute configuration of 1 was determined using the modified Mosher's method and Marfey's method. Compound 1 displayed a weak suppressive effect on the prod...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim EL,Li JL,Xiao B,Hong J,Yoo ES,Yoon WD,Jung JH

更新日期：2012-01-01 00:00:00

abstract：:A simple method to synthesize (+/-)-2-O-(4-coumaroyl)-3-(4-hydroxyphenyl)lactic acid (1), a key intermediate in rosmarinic acid biosynthesis in higher plant cells, was established by condensation of protected 4-coumaric acid and (+/-)-3-(4-hydroxyphenyl)lactic acid followed by deprotection. A stable supply of 1 thus a...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuno M,Nagatsu A,Ogihara Y,Mizukami H

更新日期：2001-12-01 00:00:00

abstract：:Six novel acyclic sulfides, named garlicnins L-1-L-4 (1-4), E (5), and F (6), were isolated from the acetone extracts, with the ability to suppress M2 macrophage activation, of the bulbs of garlic (Allium sativum L.), and their chemical structures were characterized. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nohara T,Fujiwara Y,Ikeda T,Yamaguchi K,Manabe H,Murakami K,Ono M,Nakano D,Kinjo J

更新日期：2014-01-01 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