The practical synthesis of a uterine relaxant, bis(2-[[(2S)-2-([(2R)-2-hydroxy-2-[4-hydroxy-3-(2-hydroxyethyl)-phenyl]ethyl]amino)-1,2,3,4-tetrahydronaphthalen-7-yl]oxy]-N,N-dimethylacetamide) sulfate (KUR-1246).

abstract：:Four new triterpenoid saponins (1-4) were isolated from the rhizome of Ardisia gigantifolia STAPF. The structures of new saponins were established as 3beta-o-alpha-L-rhamnopyranosyl-(1-->3)-[beta-D-xylopyranosyl-(1-->2)]-beta-D-glucopyranosyl-(1-->4)-[beta-D-glucopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl-16alpha-hyd...

journal_title：Chemical & pharmaceutical bulletin

authors： Mu LH,Gong QQ,Zhao HX,Liu P

更新日期：2010-09-01 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：:6-Amino-6-deoxyfumagillol (5) was synthesized by reductive amination of 6-oxo-6-deoxyfumagillol (4), which was obtained by oxidation of fumagillol (2). The reduction proceeded stereoselectively by the equatorial attack of hydride and 5 was found to have the same stereochemistry as that of 2. Several derivatives of 5 w...

journal_title：Chemical & pharmaceutical bulletin

authors： Marui S,Kishimoto S

更新日期：1992-03-01 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：:Oxidation of 2- and 3-hydroxycarbazoles with Frémy's salt gave the corresponding ortho-carbazolequinones. These molecules react as carbodienophiles in Diels-Alder reaction with 1-acetoxy-1,3-butadiene and 1,3-cyclopentadiene to provide the novel benzocarbazolequinone structures 15, 16, 18 and 19. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Compain-Batissou M,Latreche D,Gentili J,Walchshofer N,Bouaziz Z

更新日期：2004-09-01 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：:A series of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6,7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishikawa H,Tabusa F,Miyamoto H,Kano M,Ueda H,Tamaoka H,Nakagawa K

更新日期：1989-08-01 00:00:00

abstract：:Tumor necrosis factor (TNF), a cytokine produced in macrophages, also acts as an endogenous pyrogen (EP). To investigate whether TNF has a role in the fever induced by Nocardia rubra cell wall skeleton (N-CWS), the relationship between fever and TNF production was studied in guinea pigs. N-CWS injected i.v. to guinea ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohara K,Hirano Y,Ishida H,Mori J,Tensho A

更新日期：1989-10-01 00:00:00

abstract：:Possible utility of hydroxyalkylated beta-cyclodextrin (beta-CyD) derivatives as parenteral drug carriers was investigated, using nimodipine, a dihydropyridine derivative with calcium antagonistic action, as a model drug. The aqueous solubility of nimodipine increased linearly with increase in the concentration of hyd...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida A,Yamamoto M,Itoh T,Irie T,Hirayama F,Uekama K

更新日期：1990-01-01 00:00:00

abstract：:Three aromatic compounds (2-4) possessing a carbomethoxyl group or a dimethoxyphthaloyl group, prepared by the Diels-Alder reaction of the cardiac glycoside, proscillaridin (1), with dimethyl acetylenedicarboxylate and methyl propiolate, were transformed into alcohols, carboxylic acids and amides. The biological activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanase T,Murakami N,Nagai S,Ueda T,Sakakibara J,Ando H,Hotta Y,Takeya K

更新日期：1992-02-01 00:00:00

abstract：:Stomatitis induced by radiation therapy or cancer chemotherapy is a factor in sleep disorders and/or eating disorders, markedly decreasing patient quality of life. In recent years, disintegrating oral films that are easy to handle have been developed; therefore, we focused on the formulation of these films. We prepare...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawano Y,Sasatsu M,Mizutani A,Hirose K,Hanawa T,Onishi H

更新日期：2016-06-01 00:00:00

abstract：:Seventeen saponins isolated from the root of Pulsatilla koreana were examined for their in vitro cytotoxic activity against the human solid cancer cell lines, A-549, SK-OV-3, SK-MEL-2, and HCT15, using the SRB assay method, and their in vivo antitumor activity using BDF1 mice bearing Lewis lung carcinoma (LLC). The sa...

journal_title：Chemical & pharmaceutical bulletin

authors： Bang SC,Lee JH,Song GY,Kim DH,Yoon MY,Ahn BZ

更新日期：2005-11-01 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：:A new cycloartane bisdesmoside and two new trinorcycloartane glycosides, along with four known cycloartane compounds, were isolated from the rhizomes of Cimicifuga dahurica (Ranunculaceae). The structures of the new compounds were elucidated as 3-O-alpha-L-arabinopyranosyl cimigenol 15-O-beta-D-glucopyranoside, 24-hyd...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang QW,Ye WC,Hsiao WW,Zhao SX,Che CT

更新日期：2001-11-01 00:00:00

abstract：:The metabolites of clentiazem in the urine or bile of rats and dogs were investigated. Fifteen basic, 6 acidic, 2 neutral and 4 conjugated metabolites were isolated. In the present paper, fourteen reference compounds as shown in Charts 1, 2 and 3 were synthesized to identify the structures of the metabolites in proced...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue H,Nakamura S,Otsuka H,Gaino M,Harada T,Matsuki K,Takeda M

更新日期：1994-01-01 00:00:00

abstract：:Two new C(21) steroidal glycosides, tenacissoside L (1), tenacissoside M (2), were isolated from the stems of Marsdenia tenacissima (ROXB.) WIGHT et ARN. Their structures were elucidated, respectively, by means of chemical and spectral data, including ESI-MS, HR-ESI-MS, 1D-NMR and 2D-NMR. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang S,Lai YH,Tian B,Yang L

更新日期：2006-05-01 00:00:00

abstract：:Characteristics of the secondary structure of neocarzinostatin apoprotein (apo-NCS) were examined by various means. Gaussian analysis of the Fourier-transform infrared (FT-IR) curve and curve-fitting of the circular dichroism (CD) spectrum for apo-NCS revealed that this peptide was abundant in beta-structures. In the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Saito K,Sato Y,Edo K,Akiyama-Murai Y,Koide Y,Ishida N,Mizugaki M

更新日期：1989-11-01 00:00:00

abstract：:(+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4, 5-tetrahydro-8H-pyrido[4',3':4,5]thieno[3,2-f]triazolo[4,3-a] [1,4]diazepine (E6123) is a very potent platelet-activating factor (PAF) receptor antagonist and shows potent anti-PAF activities at the microgram level in a variety of animal models. In ord...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazawa S,Okano K,Kawahara T,Machida Y,Yamatsu I

更新日期：1992-03-01 00:00:00

abstract：:A new isoflavone, 4'-gamma,gamma-dimethylallyloxy-5,7,2',5'-tetramethoxyisoflavone, brandisianin A (1), was isolated from the leaves of Millettia brandisiana, along with one synthetically known isoflavone, 7,4'-di-O-prenylgenistein (2) and twelve known compounds. The structures were elucidated on the basis of extensiv...

journal_title：Chemical & pharmaceutical bulletin

authors： Pancharoen O,Athipornchai A,Panthong A,Taylor WC

更新日期：2008-06-01 00:00:00

abstract：:A new heptapeptide GAGPHGG (OC1) was isolated from Carapax trionycis which was a traditional Chinese medicine (TCM) used for treatment of hepatic diseases. The structure of OC1 was characterized by MS, NMR techniques, together with amino acid sequence analysis. The hepatoprotective activity of OC1 was evaluated in viv...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang P,Zhang Y,An Y,Xu K,Xu X,Fu C,Lin J,Xu S,Li Q,Lei H

更新日期：2013-01-01 00:00:00

abstract：:Nitroxyl (HNO), a one-electron-reduced form of nitric oxide, has various biological activities, including a cardioprotective effect. Here, we first synthesized another, more hydrophilic photocontrollable HNO donor (3), which can release HNO in a spatially and temporally controlled manner, and then examined the propert...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuo K,Nakagawa H,Adachi Y,Kameda E,Aizawa K,Tsumoto H,Suzuki T,Miyata N

更新日期：2012-01-01 00:00:00

abstract：:Two new iridoids, named patridoid I (1) and patridoid II (2), were isolated from the whole plant of Patrinia saniculaefolia (Valerianaceae), together with the known one, nardostachin (3). The structures of compounds 1 and 2 were established on the basis of spectroscopic methods, including two dimensional (2D NMR) and ...

journal_title：Chemical & pharmaceutical bulletin

authors： An RB,Min BS,Na MK,Chang HW,Son KH,Kim HP,Lee HK,Bae K,Kang SS

更新日期：2003-05-01 00:00:00

abstract：:Water-soluble porphyrins containing four platinum(II) complexes per molecule, [5alpha,10beta,15alpha,20beta-tetrakis(2-trans-(alpha,beta,alpha,beta-trans-Pt) and cis-(alpha,beta,alpha,beta-cis-Pt) [PtCl(NH(3))(2)]N-2-aminophenylporphyrin)], were synthesized and characterized. The binding of synthetic nucleotide polyme...

journal_title：Chemical & pharmaceutical bulletin

authors： Munakata H,Imai H,Nakagawa S,Osada A,Uemori Y

更新日期：2003-05-01 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：:The resistance to crushing after a self-setting bioactive calcium phosphate cement, consisting of various particle sizes of tetracalcium phosphate (TECP), dicalcium phosphate dihydrate (DCPD) and hydroxyapatite (HAP), had hardened was tested after setting at 37 degrees C, 100% RH. X-ray diffraction suggested that the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otsuka M,Matsuda Y,Suwa Y,Fox JL,Higuchi WI

更新日期：1993-11-01 00:00:00

abstract：:In the conventional method of mixer blending extraction, the yields of the tomato-saponin, esculeoside A, in the mini and middy tomatoes were found to be 0.043% and 0.046%, respectively. In order to improve the yields, we attempted a more efficient extraction using shock waves. The yields of esculeoside A were 0.0987%...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Takemoto A,Maehara H,Ohno M,Murakami Y,Itoh S,Nohara T

更新日期：2011-01-01 00:00:00

abstract：:[D-Leu8]Dynorphin(1--8)-NH2 analogs, in which each peptide bond was systematically replaced with a psi(CH2NH) peptide bond, were synthesized by the solid-phase method. The psi(CH2NH) bond was introduced by the Boc-amino acid aldehyde/NaCNBH3 method on a solid support. In the syntheses of the analogs, undesirable doubl...

journal_title：Chemical & pharmaceutical bulletin

authors： Ambo A,Adachi T,Sasaki Y

更新日期：1995-09-01 00:00:00

abstract：:A moisturizing cream mixed with a steroid ointment is frequently prescribed to patients suffering from atopic dermatitis. However, there is a concern that the mixing operation causes destabilization. The present study was performed to investigate the stability of such preparations closely using magnetic resonance imag...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Funatani C,Yamamoto Y,Fukami T,Koide T,Hayashi Y,Takayama K

更新日期：2017-01-01 00:00:00

abstract：:Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurashima H,Uchida S,Kashiwagura Y,Tanaka S,Namiki N

更新日期：2020-01-01 00:00:00

abstract：:A new method has been developed for the umpolung α-heteroarylation of ketones via an N-alkoxyenamine. The treatment of ketones with tris(heteroaryl)aluminum reagents in the presence of isoxazolidine gave the corresponding α-heteroarylated ketones in moderate to good yields. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyoshi T,Takeda N,Fukami M,Sato S,Ueda M,Miyata O

更新日期：2014-01-01 00:00:00