Formal (3+3) cycloaddition of silyl enol ethers catalyzed by trifric imide: domino Michael addition-claisen condensation accompanied with isomerization of silyl enol ethers.

abstract：:beta-Cyclododecyl aspartate was prepared and its application to peptide synthesis was examined. Derivatives of beta-cyclododecyl aspartate are more likely to crystallize and should be useful for peptide synthesis. The cyclododecyl ester was much stable to bases than the benzyl ester and rather more stable than the cyc...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawasaki K,Murakami T,Koshino K,Namikawa M,Maeda M,Hama T,Mayumi T

更新日期：1994-04-01 00:00:00

abstract：:A series of novel potentially platelet aggregation-inhibiting 1,4-benzoxazine-3(4H)-one derivatives was designed and synthesized through Smiles rearrangement, reduction and acetylation reactions. The antiaggregatory activities of the target molecules on arterial blood samples from rabbits, expressed by IC₅₀ values (μM...

journal_title：Chemical & pharmaceutical bulletin

authors： Liu C,Tan JL,Xiao SY,Liao JF,Zou GR,Ai XX,Chen JB,Xiang Y,Yang Q,Zuo H

更新日期：2014-01-01 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：:A nondestructive, efficient, and rapid method for quantitative analysis of two bioactive components (salidroside and p-tyrosol) in Rhodiola crenulata, a traditional Tibetan medicine, by Fourier transform near-infrared (FT-NIR) spectroscopy was developed. Near-infrared diffuse reflectance spectra in the range of 4000 t...

journal_title：Chemical & pharmaceutical bulletin

authors： Li T,He X

更新日期：2016-01-01 00:00:00

abstract：:When 8-bromoadenosine was incubated with cysteine at pH 7.2 and 37°C, an exclusive product was generated. This product was identified as a cysteine substitution derivative of adenosine at the 8 position, 8-S-L-cysteinyladenosine. The reaction accelerated as pH increased from mildly acidic to basic conditions. The isol...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Ogishi A,Shinohara T,Suito S

更新日期：2018-01-01 00:00:00

abstract：:Stereocontrolled syntheses of model compounds related to a major antigenic epitope against antibupleurum 2IIc/PG-1-IgG from antiulcer pectic polysaccharide are described. A trisaccharide derivative (13) was prepared as a precursor and a novel and simple approach for the rational design of a glycocluster and glycodendr...

journal_title：Chemical & pharmaceutical bulletin

authors： Jin Y,Hada N,Oka J,Kanie O,Daikoku S,Kanie Y,Yamada H,Takeda T

更新日期：2006-04-01 00:00:00

abstract：:Oiling-out is a unique phenomenon that the liquid phase is separated into two parts during crystallization. The emergence of new liquid phase changes the environment where crystals nucleate and grow, we call "mother phase," because target material and impurities become distributed to each phase according to their own ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Takiyama H

更新日期：2020-01-01 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：:Biodegradable pasty-type copolyesters with a relatively low molecular weight of 4500 were synthesized by direct copolycondensation of epsilon-caprolactone (CL) and delta-valerolactone (VL) in the absence of catalysts to evaluate in vivo capabilities of the polymer for implantable controlled release devices in drug del...

journal_title：Chemical & pharmaceutical bulletin

authors： Imasaka K,Yoshida M,Fukuzaki H,Asano M,Kumakura M,Mashimo T,Yamanaka H,Nagai T

更新日期：1991-08-01 00:00:00

abstract：:Two novel tropoloisoquinoline alkaloids, Pareirubrines A and B, have been isolated as antileukemic substances from Cissampelos pareira (Menispermaceae), together with the same skeleton alkaloids, grandirubrine and isoimerubrine. Their structures were elucidated by nuclear magnetic resonance (NMR) studies, and their so...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Matsumoto K,Takeya K,Itokawa H,Iitaka Y

更新日期：1993-08-01 00:00:00

abstract：:Three new norlanostane-type triterpene glycosides, scillanostasides A, B, and C, and two new lanostane-type triterpene glycosides, scillanostasides D and E, were isolated from the bulbs of Scilla scilloides Druce (Liliaceae) along with one known norlanostane-type triterpene heptaglycoside, scillascilloside G-1. Their ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Toyohisa D,Morishita T,Horita H,Yasuda S,Nishida Y,Tanaka T,Okawa M,Kinjo J,Yoshimitsu H,Nohara T

更新日期：2011-01-01 00:00:00

abstract：:20(S)-Camptothecin derivatives having nitro, amino, chloro, bromo, hydroxyl and methoxyl groups in the A-ring were synthesized. B-Ring hydrogenated camptothecin (2a) was converted into 10-hydroxycamptothecin (6e) by treatment with lead tetraacetate in trifluoroacetic acid. 10-Substituted derivatives (6) were obtained ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sawada S,Matsuoka S,Nokata K,Nagata H,Furuta T,Yokokura T,Miyasaka T

更新日期：1991-12-01 00:00:00

abstract：:The crystal of bovine trypsin complexed with a potent inhibitor, 4-[4-(N,N- dimethylcarbamoylmethoxycarbonylmethyl)phenoxycarbonylphenyl ]guanidinium (FOY-305) in the novel orthorhombic from with a low molecular packing density was studied by the X-ray diffraction method. Using synchrotron radiation, the intensity dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto O,Taga T,Matsushima M,Higashi T,Machida K

更新日期：1990-08-01 00:00:00

abstract：:A one-pot conversion of allyl alcohols into selenochroman derivatives was achieved by treatment with a phenyl trimethylsilyl selenide (TMSSePh)-AIBr3 reagent system. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe H,Yamasaki A,Koshiba N,Takeuchi Y,Harayama T

更新日期：2001-09-01 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

abstract：:Poorly water-soluble drugs N-5159, griseofulvin (GFV), glibenclamide (GBM) and nifedipine (NFP) were ground in a dry process with polyvinylpyrrolidone (PVP) and sodium dodecyl sulfate (SDS). Different crystallinity behavior of each drug during grinding was shown in the ternary Drug/PVP/SDS system. However, when each t...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh K,Pongpeerapat A,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2003-02-01 00:00:00

abstract：:An examination was made on the effect of fumaric acid on an experimental systemic candidiasis. Male ICR mice were innoculated into the tail veins with 10(6) yeast cells of Candida albicans and treated with daily intraperitoneal injections of fumaric acid at the dose of 40 mg/kg/d. The results indicated that the admini...

journal_title：Chemical & pharmaceutical bulletin

authors： Akao M,Kuroda K

更新日期：1991-11-01 00:00:00

abstract：:Thermodynamic studies were carried out to evaluate the binding of theophylline on adenosine deaminase (ADA) in 50 mM sodium phosphate buffer pH 7.5, at 300 K, using isothermal titration calorimetry (ITC). A simple method for determination of binding isotherm in the drug--ADA interaction was applied using ITC data. ADA...

journal_title：Chemical & pharmaceutical bulletin

authors： Saboury AA,Bagheri S,Ataie G,Amanlou M,Moosavi-Movahedi AA,Hakimelahi GH,Cristalli G,Namaki S

更新日期：2004-10-01 00:00:00

abstract：:The complexation of Zn(II) with glycyl-L-histidylglycine and its deuterated derivatives, glycyl-d2-L-histidylglycine and glycyl-L-histidylglycine-d2, was studied by proton nuclear magnetic resonance spectroscopy over the pD range, from 3.4 to 11.0, at 25 degrees C. Addition of Zn(II) to the peptide made the resonances...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda J,Hanaki A,Yoshida N,Nakajima T

更新日期：1995-12-01 00:00:00

abstract：:Two new acylated flavonol glycosides, named amurenosides A and B, together with quercetin 3-(2,6-di-O-alpha-rhamnopyranosyl-beta-galactopyranoside), have been isolated from the whole plant of Vicia amurensis. Their structures were elucidated as quercetin 3-O-alpha-L-(3-feruloylrhamnopyranosyl)(1-->6)-[alpha-L-rhamnopy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kang SS,Chang YS,Kim JS

更新日期：2000-08-01 00:00:00

abstract：:Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developed a synthesis based on the photocyclization of tertiary ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aragon PJ,Yapi AD,Pinguet F,Chezal JM,Teulade JC,Blache Y

更新日期：2007-09-01 00:00:00

abstract：:Synthesis and pharmacological evaluation of novel thienopyridazinones and related compounds are described. A thiophene ring was found to be able to replace the benzene ring of a phthalazinone without loss of biological activities. This observation supports our hypothesis that the benzene ring plays an important role i...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Maruyama N,Koga T,Kamei K,Akima M,Kuroki T,Hamana M,Ohi N

更新日期：1995-02-01 00:00:00

abstract：:Chemical and pharmacological studies of Panax vietnamensis (Vietnamese ginseng; VG) have been reported since its discovery in 1973. However, the content of each saponin in different parts of VG has not been reported. In this study, 17 ginsenosides in the different underground parts of P. vietnamensis were analyzed by ...

journal_title：Chemical & pharmaceutical bulletin

authors： Le TH,Lee GJ,Vu HK,Kwon SW,Nguyen NK,Park JH,Nguyen MD

更新日期：2015-01-01 00:00:00

abstract：:Hot aqueous extracts of 134 Chinese crude drugs were subjected to screening for inhibitory activity on K+ contracture of guinea pig taenia coli, and significant activity was observed in 17 crude drugs. Chemical investigations of two crude drugs, Kakko and Ubai, which originate from Pogostemon cablin and Prunus mume, r...

journal_title：Chemical & pharmaceutical bulletin

authors： Ichikawa K,Kinoshita T,Sankawa U

更新日期：1989-02-01 00:00:00

abstract：:We developed a rapid and efficient analytical technique for cyclosporine A using HPLC on a column packed with 2-µm nonporous octadecylsilyl silica particles. Under optimized conditions, cyclosporine A was separated with high resolution from other cyclic peptides within 3 min, because the mass transfer resistance in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Kato K,Nanjo K,Goda Y

更新日期：2018-01-01 00:00:00

abstract：:We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Hirono S

更新日期：2019-01-01 00:00:00

abstract：:The release properties of phenylpropanolamine hydrochloride (PPA) from ethylcellulose (EC) matrix granules prepared by an extrusion granulation method were examined. The release process could be divided into two parts; the first and second stages were analyzed by applying square-root time law and cube-root law equatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukui A,Fujii R,Yonezawa Y,Sunada H

更新日期：2004-03-01 00:00:00

abstract：:We investigated the distribution and fate of liposomes after their intravenous injection into a mouse. Liposomes were composed of dimyristoylphosphatidylcholine, cholesterol and dicetylphosphate (7:2:1, molar ratio) with or without lactosylceramide. They were characterized as small unilamellar vesicles, approximately ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshioka S,Banno Y,Okano Y,Ohki K,Mizukami Y

更新日期：1992-04-01 00:00:00

abstract：:A full account is given of the first chemical synthesis of the antitumor antibiotic guanine 7-oxide (5) and its 9-substituted derivatives (24a--k and 26). Coupling of appropriate primary amines (17a--e, g--k) with phenacyl bromide (16) produced, after treatment with HCl, the corresponding N-substituted phenacylamine h...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawa K,Nishii M,Inagaki J,Nohara F,Saito T,Itaya T,Fujii T

更新日期：1992-02-01 00:00:00

abstract：:Freshwater cyanobacteria produce lethal toxins such as microcystins and anatoxins. During the purification of microcystins in bloom samples we found that a toxic cyanobacterium produced not only microcystins but also other types-peptides in early 1990. Since then we have isolated approximately thirty peptides from fre...

journal_title：Chemical & pharmaceutical bulletin

authors： Harada K

更新日期：2004-08-01 00:00:00