(2+2) cycloaddition reaction of alkyl enol ethers with acrylates by in situ generated silyl triflic imide catalyst.

abstract：:A series of benzylidene 2-aminoimidazolones derivatives were synthesized. Most compounds displayed strong inhibitory activity on the proliferation of human HepG2 cells in vitro. The active compounds were further evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against five human ca...

journal_title：Chemical & pharmaceutical bulletin

authors： Ling Y,Wang ZQ,Xiao YA,Zhu C,Shen L,Wang XM,Hui Y,Wang XY

更新日期：2013-01-01 00:00:00

abstract：:Eight new myriocin analogs, 2-epi-myriocin, Z-14-deoxomyriocin, and nor-deoxomyriocins, and a known myriocin derivative, 14-deoxomyriocin, were synthesized from 2-deoxy-D-glucose via common intermediates in previous myriocin and Z-myriocin syntheses. The immunosuppressive activities of new myriocin analogs and Z-myrio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Yokokawa Y,Okuno Y,Yagi N,Murakami N

更新日期：1994-12-01 00:00:00

abstract：:Zerumbone is a multifunctional compound which shows various biological activities, such as antitumor activity, anti-inflammatory activity, antiulcer activity, etc. However, to use Zerumbone as functional foods or medicines, its pharmaceutical properties such as solubility should be improved. In the present study, we p...

journal_title：Chemical & pharmaceutical bulletin

authors： Hassan MM,Mohammed AFA,Elamin KM,Devkota HP,Ohno Y,Motoyama K,Higashi T,Imai T

更新日期：2020-01-01 00:00:00

abstract：:In order to confirm the proposed structures of two metabolites 3 and 4 of the gastroprokinetic agent mosapride [4-amino-5-chloro-2-ethoxy-N-([4-(4-fluorobenzyl)-2-morpholinyl] methyl)benzamide, 2], the compounds were synthesized and their biological activity was examined. The structures of the metabolites were confirm...

journal_title：Chemical & pharmaceutical bulletin

authors： Kato S,Morie T,Yoshida N

更新日期：1995-04-01 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：:The intercalation reaction of diclofenac sodium (DFS) with layered inorganic compounds, gamma-titanium phosphate (gamma-TiP), proton type titanium oxide (H-TiO2) and sodium type synthetic mica (Na-TSM), was examined on. The direct reaction of DFS in ethanol-water mixed solvent resulted in the large amount accommodatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Tajima T,Suzuki N,Watanabe Y,Kanzaki Y

更新日期：2005-11-01 00:00:00

abstract：:A new pregnane glycoside, a dibenzylbutyrolactone lignan, 5-hydroxymatairesinol dimethyl ether, and three new flavonoids, including one 8-methylflavan-3-ol, and two 8-methylflavones, together with five known flavonoids and two known alkaloids were isolated from the rhizomes of Tupistra chinensis. The structures of all...

journal_title：Chemical & pharmaceutical bulletin

authors： Pan WB,Wei LM,Wei LL,Wu YC

更新日期：2006-07-01 00:00:00

abstract：:The synthesis of optically active acyclic analogues of 3'-azido-3'-deoxythymidine, which lack only the 2'-CH2 of the sugar, is described. The synthesis of some nucleoside analogues that contain the N-acetyl-D-neuraminic acid moiety is also described. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Murata M,Achiwa K

更新日期：1990-03-01 00:00:00

abstract：:The latex of Euphorbia nivulia afforded three new ingol diterpenes, 3-acetyl-8-methoxyl-7-angolyl-12-hydroxylingol (7), 3,12-diacetyl-7-hydroxy-8-methoxylingol (8), and 3,12-diacetyl-7-angolyl-8-hydroxylingol (9) along with five known ingol diterpenes 2-6 and a known triterpene cyclonivulinol (1). Their structures wer...

journal_title：Chemical & pharmaceutical bulletin

authors： Ravikanth V,Lakshmi Niranjan Reddy V,Vijender Reddy A,Ravinder K,Prabhakar Rao T,Siva Ram T,Anand Kumar K,Prakesh Vamanarao D,Venkateswarlu Y

更新日期：2003-04-01 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 binding of carprofen (CP) to human serum albumin (HSA) and bovine serum albumin (BSA) was compared using equilibrium dialysis method. The affinity of CP for the primary binding site was BSA > HSA. However, the number of primary binding sites (n1) was 1.94 on HSA, considerably greater than that on BSA (0.79). The d...

journal_title：Chemical & pharmaceutical bulletin

authors： Kohita H,Matsushita Y,Moriguchi I

更新日期：1994-04-01 00:00:00

abstract：:2- or 3-Substituted 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclohepten-8- ylcarbonyl)-4-(3,4,5-trimethoxybenzoyl)- and 4-(3,4,5-trimethoxybenzyl)piperazines (2a-s, 3a, b) were prepared and evaluated for antagonistic activities against platelet-activating factor (PAF)-induced platelet aggregation and blood pressure reduc...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukushi H,Mabuchi H,Terashita Z,Nishikawa K,Sugihara H

更新日期：1994-03-01 00:00:00

abstract：:Cornusiin A (1), cornusiin B (2) and cornusiin C (3), new dimeric, monomeric and trimeric hydrolyzable tannins, were isolated from the fruits of Cornus officinalis (Cornaceae). Their structures, including the orientation of the valoneoyl group in 1 and 3, were established on the basis of chemical and spectroscopic dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Hatano T,Ogawa N,Kira R,Yasuhara T,Okuda T

更新日期：1989-08-01 00:00:00

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：:The synthesis of acetomycin and related analogs was investigated. Acetomycin was synthesized from diethyl allyl(methyl)malonate in 6.5% yield over 18 steps. The total number of steps was improved compared to our previous synthesis; i.e., four steps shorter, and the total yield was 4.5% greater than the previous synthe...

journal_title：Chemical & pharmaceutical bulletin

authors： Uenishi J,Kobayashi N,Komine S,Okadai T,Yonemitsu O,Sasaki T,Yamada Y

更新日期：1999-04-01 00:00:00

abstract：:The regioselective intramolecular 1,3-dipolar cycloaddition of the phenylsulfonylallene-nitrone derivatives has been developed. This reaction showed that the distal double bond of the allene exclusively reacted with the nitrone group to produce the bicyclic isoxazolidine derivatives regardless of the substitution patt...

journal_title：Chemical & pharmaceutical bulletin

authors： Inagaki F,Kobayashi H,Mukai C

更新日期：2012-01-01 00:00:00

abstract：:Orally disintegrating tablets (ODTs) are useful for improving benefits for patients of various ages. Masking the unpleasant taste of a drug is an important factor in the compliance of patients who take ODTs. We evaluated the taste acceptability effects of various taste-masking methods on bitter famotidine ODTs as a cl...

journal_title：Chemical & pharmaceutical bulletin

authors： Sugiura T,Uchida S,Namiki N

更新日期：2012-01-01 00:00:00

abstract：:Different green synthesis of alkyl esters of acyclovir (acyclovir prodrugs) is described. Hexanoic, decanoic, dodecanoic and tetradecanoic acyclovir esters were synthesized reacting acyclovir and the respective acid anhydride in dimethyl sulfoxide (DMSO), in solvents from renewable sources and without solvent (T=30 °C...

journal_title：Chemical & pharmaceutical bulletin

authors： de Regil-Hernández R,Martínez-Lagos F,Rodríguez-Bayón A,Sinisterra JV

更新日期：2011-01-01 00:00:00

abstract：:The interaction of a newly developed Helicobacter pylori eradicating agent (TG44, 4-methylbenzyl-4'-[trans-4-(guanidinomethyl)cyclohexylcarbonyloxy]biphenyl-4-carboxlylate monohydrochloride) with beta-cyclodextrin (beta-CyD) in aqueous solution and in solid state was studied to gain insight into the high in-vivo H. py...

journal_title：Chemical & pharmaceutical bulletin

authors： Anzai K,Mizoguchi J,Yanagi T,Hirayama F,Arima H,Uekama K

更新日期：2007-10-01 00:00:00

abstract：:New abietane-type diterpenes, 15-acetoxy-7-oxodehydroabietic acid (1), picealactones A (2), B (3), and C (4), together with the known 7-oxodehydroabietic acid (5) were isolated and identified from the heartwood of Picea morrisonicola. The structures of 1-4 were determined on the basis of spectral data explanation. Com...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Yeh MH,Lin HC

更新日期：2004-07-01 00:00:00

abstract：:A new series of highly potent angiotensin-converting enzyme (ACE) inhibitors, 1-(N2-substituted L-lysyl-gamma-D-glutamyl)octahydro-1H-indole-2-carboxylic acids, was synthesized; various acyl groups were introduced at the alpha-amino group of the N-terminal P1 Lys. The effect of the N2-acyl groups on in vitro inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Sawayama T,Tsukamoto M,Sasagawa T,Nishimura K,Deguchi T,Takeyama K,Hosoki K

更新日期：1990-01-01 00:00:00

abstract：:The objective of present work was to enhance the solubility and bioavailability of poorly aqueous soluble drug Irbesartan (IBS). The solid dispersions were prepared by spray drying method using low viscosity grade HPMC E5LV. Prepared solid dispersions were characterized by dissolution study, fourier transform infrared...

journal_title：Chemical & pharmaceutical bulletin

authors： Boghra RJ,Kothawade PC,Belgamwar VS,Nerkar PP,Tekade AR,Surana SJ

更新日期：2011-01-01 00:00:00

abstract：:Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we ...

journal_title：Chemical & pharmaceutical bulletin

authors： Dohi M,Momose W,Yamashita K,Hakomori T,Sato S,Noguchi S,Terada K

更新日期：2017-02-01 00:00:00

abstract：:N-9-Fluorenylmethoxycarbonyl-Se-4-methoxybenzylselenocysteine++ + [Fmoc-Sec(MBzl)-OH] was synthesized from selenocystine and successfully applied to Fmoc-based solid-phase peptide synthesis. The stability and the deprotection conditions of the Se-MBzl group were examined. The diselenide bond of a peptide was directly ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koide T,Itoh H,Otaka A,Yasui H,Kuroda M,Esaki N,Soda K,Fujii N

更新日期：1993-03-01 00:00:00

abstract：:A quantitative structure property relationship (QSPR) study was performed to develop a model that relates the structures of 150 drug organic compounds to their aqueous solubility (log S(w)). Molecular descriptors derived solely from 3D structure were used to represent molecular structures. A subset of the calculated d...

journal_title：Chemical & pharmaceutical bulletin

authors： Ghasemi J,Saaidpour S

更新日期：2007-04-01 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：:The structures of the ternary palladium(II) complexes of the formulations [Pd(Gly)(bpy)](+)Cl(-).4H(2)O (Gly=glycine; bpy=2,2'-bipyridine) (1), [Pd(Gly)(phen)](+)Cl(-).4H(2)O (2) (phen=1,10-phenanthroline) and {[Pd(Gly)(bpa)](+)Cl(-)}(2).6H(2)O (3) (bpa=2,2'-bipyridylamine) were determined. All complexes are positivel...

journal_title：Chemical & pharmaceutical bulletin

authors： Yodoshi M,Okabe N

更新日期：2008-07-01 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：:Targeted protein degradation by small molecules is an emerging modality with significant potential for drug discovery. We previously developed chimeric molecules, termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which induce the ubiquitylation and proteasomal de...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohoka N,Ujikawa O,Shimokawa K,Sameshima T,Shibata N,Hattori T,Nara H,Cho N,Naito M

更新日期：2019-03-01 00:00:00

abstract：:This paper discusses a process for making a novel granular detergent with an interspersion particle comprising an anionic surfactant and a polymeric polycarboxalate. This process contains three steps to develop the interspersion particles with anionic surfactant and polymeric ploycarboxalate. The first step was to for...

journal_title：Chemical & pharmaceutical bulletin

authors： Ebihara F,Watano S

更新日期：2003-06-01 00:00:00