Effect of polymer excipients on the enzyme activity of lyophilized bilirubin oxidase and beta-galactosidase formulations.

abstract：:We studied a method of estimating the number of contacts in a solid dosage form using thermal analysis. Ibuprofen (IB) and Ethenzamide (ET) were used as model actives. IB and ET were granulated and sieved with each other. We prepared mixtures of IB and ET using different diameter granules. The number of contacts betwe...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoki S,Mizutani T,Danjo K

更新日期：2000-01-01 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：:Chalcone (3) has been synthesized as a new chalcone derivative bearing benzofuran moiety at 1 position. Such chalcone was used as a model dielectrophile applied to react with some nucleophiles such as 5-amino pyrazoles, 5-amino-1,2,4-triazole, 2-aminobenzimidazole, and 6-uraciles under Michael reaction conditions and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nassar E,El-Badry YA,El Kazaz H

更新日期：2016-01-01 00:00:00

abstract：:The reaction of the N-furfuryloxamic acid sodium salt (12) with 1,1'-oxalyldiimidazole (ODI) yielded the imidazolide (13) as an intermediate, and this directly reacted with 2-aminothiazole derivatives (14) or 2-aminobenzothiazole derivatives (15) under essentially neutral conditions to afford the N'-12-(substituted th...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa T,Tsutsui C

更新日期：2000-09-01 00:00:00

abstract：:Fibrinogen-related peptides, monomeric cyclic peptides through a disulfide bond [cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-NH2), cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-Gly-NH2), cyclo(H-Cys-Arg-Gly-Asp-Cys-NH2) and cyclo(H-Cys-Arg-Gly-Asp-Cys-Gly-NH2)], were prepared by the solid phase method with disulfide bond formation on the solid...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakiuchi M,Izuno Y,Maeda M,Ueda K,Fujiwara K,Kunitada S,Kawasaki K

更新日期：1996-05-01 00:00:00

abstract：:A series of 2-(4-methylphenyl)benzothiazoles was synthesized and evaluated using an adjuvant-induced arthritic rat model. This class of desired compounds affecting the immune response was found using hemagglutination assay. 4-Acetoxy-2-(4-methylphenyl)benzothiazole (7m), KB-2683, was most potent in the adjuvant-induce...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori N,Tsukamoto G,Imamura A,Ohashi M,Saito T,Yoshino K

更新日期：1992-09-01 00:00:00

abstract：:Chemical reactivity descriptors and lipophilicyty (log P) were evaluated via semi-empirical method for the quantum calculation of molecular electronic structure (PM3) in order to clarify the structure-cytotoxic activity relationships of disubstutited thioureas. Analysed compounds were obtained by the linkage of 2-amin...

journal_title：Chemical & pharmaceutical bulletin

authors： Filipowska A,Filipowski W,Tkacz E,Nowicka G,Struga M

更新日期：2016-01-01 00:00:00

abstract：:A series of phthiobuzone analogs, prepared from potassium phthalimide or phthalandione, have been evaluated for their antiviral activities. Among the candidates, compounds 5j and 5k, which contain the substituted 4-halogenated phenyl ring at N-4',4'' position, show more potent antiviral activity than phthiobuzone agai...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang YJ,Zhao JH,Pan XD,Zhang PC

更新日期：2010-02-01 00:00:00

abstract：:A variety of 5,4'-disubstituted flavones, which are anticipated to be androgen receptor antagonists to treat diseases mediated by the androgen receptor, were synthesized. It was found that an intramolecular ipso-substitution reaction via cesium enolate using 2-fluoro-6-hydroxyacetophenone and various benzoyl chlorides...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsugi M,Takeda M,Takahashi A,Tazaki T,Tamura H,Shioiri T

更新日期：2010-08-01 00:00:00

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：: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：:Polyamines, especially spermine, inhibit N-methyl-D-aspartate (NMDA) receptors as open channel blockers. Two types of water-soluble NMDA receptor antagonist, ACCn (1) and TGCn (2), with a 1,4,7,10-tetraazacyclododecane cyclic polyamine group, were synthesized and the effects of both compounds on NMDA receptors were st...

journal_title：Chemical & pharmaceutical bulletin

authors： Masuko T,Metori K,Kizawa Y,Kusama T,Miyake M

更新日期：2005-04-01 00:00:00

abstract：:A new oleanan-type triterpene and three new cincholic acid glycosides were isolated from Peruvian "Una de Gato" (Cat's claw, plant of origin: Uncaria tomentosa), a traditional herbal medicine in Peru. Their structures were determined by spectroscopic analysis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima M,Hashimoto K,Sandoval M,Aimi N,Takayama H

更新日期：2004-10-01 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：:With the aim of improving of the efficacy and decreasing the side effects of oxybutynin (1), N-[(tetrahydro-3- or 4-pyridyl)methyl]-, N-(4-piperidyl)-, and N-(3- or 4-piperidylalkyl)-2-hydroxyacetamides (3a-n, 4a-g) and the related carboxamides (3o-r, 4h-k, 13', 17) were synthesized and evaluated for inhibitory activi...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi K,Tsubaki K,Mizuno H,Take K,Okumura K,Terai T,Shiokawa Y

更新日期：1994-01-01 00:00:00

abstract：:16 alpha-Hydroxyandrost-4-ene-3,17,19-trione (10) was synthesized from the 16 alpha-hydroxy-6 beta,19-epoxy-17-one 3 via protection of the 16 alpha-hydroxy function as its tert-butyldimethylsilyl ether or acetate. Reductive cleavage of the epoxy ring of the silyl ether 4 or the acetate 5 with zinc dust gave the 19-alc...

journal_title：Chemical & pharmaceutical bulletin

authors： Numazawa M,Hoshi K,Konno T,Nagaoka M

更新日期：1990-07-01 00:00:00

abstract：:Three new cycloartane triterpene glycosides, soulieosides A (1), B (2), and C (3), were isolated from the rhizomes of Souliea vaginata, and their structures were elucidated on the basis of extensive NMR experiments and chemical methods. Soulieosides A-C were assigned as 25-O-acetylcimigenol-3-O-beta-D-(2-acetyl)xylopy...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou L,Yang J,Zou J,Tu G

更新日期：2004-05-01 00:00:00

abstract：:Three new phenolic glycosides, named oplopanphesides A-C (1-3), have been isolated from the root barks of Oplopanax horridus. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR techniques. These phenolic glycosides possess a novel feature in their sugar moieties that ...

journal_title：Chemical & pharmaceutical bulletin

authors： Huang WH,Zhang QW,Meng LZ,Yuan CS,Wang CZ,Li SP

更新日期：2011-01-01 00:00:00

abstract：:Our aim is to test the characteristics and expression activity in brain capillary endothelial cells (BCECs) of DNA-loaded nanoparticles before and after the modification with Antennapedia peptide (Antp). Chitosan (CH), polyethylenimine (PEI) and polyamidoamine (PAMAM) were chosen to prepare the nanoparticles; Lipofect...

journal_title：Chemical & pharmaceutical bulletin

authors： Huang R,Yang W,Jiang C,Pei Y

更新日期：2006-09-01 00:00:00

abstract：:2,2,-Disubstituted norbornenes (1, 2), 2,2-Disubstituted norbornane (3), 2,2,3-trisubstituted norbornenes (4, 5), oxanorbornenes (6) and azanorbornenes (7) were synthesized by the Diels-Alder reaction using alpha, beta-dehydroamino acids as a key step, and their antiulcer activities were examined. The oxazolidine deri...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamazaki H,Horikawa H,Nishitani T,Iwasaki T,Nosaka K,Tamaki H

更新日期：1992-01-01 00:00:00

abstract：:Toxicarioside D (1), a new cardenolide, along with 10 other known ones, was isolated from the stem of Antiaris toxicaria LESCH. by bioassay-guided fractionation. Their structures were determined on the basis of spectroscopic analysis. All the reported compounds effectively inhibited the growth of various cancer cell l...

journal_title：Chemical & pharmaceutical bulletin

authors： Jiang MM,Dai Y,Gao H,Zhang X,Wang GH,He JY,Hu QY,Zeng JZ,Zhang XK,Yao XS

更新日期：2008-07-01 00:00:00

abstract：:A series of joro spider toxins, novel polyamines sharing a common moiety of 2,4-dihydroxyphenylacetyl cadaverine, have been identified using various bioassays, such as inhibition of a glutamatergic transmission and insecticidal activity. In this paper, we tried to chemically find still unknown polyamine toxins in the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiba T,Akizawa T,Matsukawa M,Pan-Hou H,Yoshioka M

更新日期：1994-09-01 00:00:00

abstract：:A series of N-azabicycloalkyl-1-alkyl-2-oxo-1,2-dihydro-3-quinolinecarboxamides were synthesized and tested for serotonin 5-HT4 receptor-stimulating effects in the regulation of electrically-evoked contraction in guinea pig muscle. Among them, N-azabicycloalkyl-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide (8c,...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki M,Ohuchi Y,Asanuma H,Kaneko T,Yokomori S,Ito C,Isobe Y,Muramatsu M

更新日期：2000-12-01 00:00:00

abstract：:Three new spirostanol glycosides (1-3) and a new furostanol glycoside (4), together with two known spirostanol glycosides (5 and 6) were isolated from the whole plants of Agave utahensis (Agavaceae). The structures of the new compounds were determined by spectroscopic analysis and the results of hydrolytic cleavage. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokosuka A,Mimaki Y

更新日期：2007-01-01 00:00:00

abstract：:A gas chromatography-selected ion monitoring procedure with chemical ionization is described for the determination of bromovalerylurea (BVU) in human plasma. BVU was extracted with ether after addition of 2-bromo-2-methylpropylurea as an internal standard. The lower limit of BVU quantification by this method was 2 ng/...

journal_title：Chemical & pharmaceutical bulletin

authors： Kokatsu J,Yomoda R,Suwa T

更新日期：1992-06-01 00:00:00

abstract：:The fluorometric thiobarbituric acid (TBA) assay of blood plasma was performed under various conditions in order to assess whether the assay reflects lipid peroxidation. The TBA-reactivity of malonaldehyde was not dependent on the pH values of the reaction and was little affected by tert-butyl hydroperoxide (tert-BuOO...

journal_title：Chemical & pharmaceutical bulletin

authors： Kojima T,Kikugawa K,Kosugi H

更新日期：1990-12-01 00:00:00

abstract：:A practical protocol to obtain accurate heat capacity values of pharmaceutical compounds using modulated-temperature differential scanning calorimetry was established. Three pharmaceutical compounds, acetaminophen, indomethacin, and tri-O-methyl-β-cyclodextrin were used as model compounds. Powder samples did not produ...

journal_title：Chemical & pharmaceutical bulletin

authors： Harada T,Kawakami K,Yoshihashi Y,Yonemochi E,Terada K,Moriyama H

更新日期：2013-01-01 00:00:00

abstract：:Three new fasciculol esters, fasciculic acids A (1), B (2) and C (3), having potent calmodulin antagonistic activity were isolated from the toxic mushroom Naematoloma fasciculare (Fr.) Karst. Their structures were elucidated on the basis of spectral and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi A,Kusano G,Ohta T,Ohizumi Y,Nozoe S

更新日期：1989-12-01 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：:Arginine-vasopressin (AVP) was acylated with various acyl azides (2a-j) in pH 9.1 buffer to give AVP derivatives (11a-j) modified at the tyrosine side chain with a carbohydrate via a spacer arm. Glycoconjugates of AVP modified at the N-terminal amide (12a-e) were also synthesized from AVP and carboxylic acids (3a-e) u...

journal_title：Chemical & pharmaceutical bulletin

authors： Susaki H,Suzuki K,Ikeda M,Yamada H,Watanabe HK

更新日期：1998-10-01 00:00:00