QSPR prediction of aqueous solubility of drug-like organic compounds.

abstract：:Alkaline sucrose density gradient and agarose gel electrophoresis methods were used to observe lambda deoxyribonucleic acid (DNA) strand breaks by the reaction system of reduced glutathione (GSH) with alloxan in the presence of Fe(3+)-ethylenediaminetetraacetic acid (EDTA). When DNA was incubated in the reaction syste...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai K,Haga K,Ogiso T

更新日期：1992-08-01 00:00:00

abstract：:We have attempted to prepare micronized drug particles and to maintain the micronized state long-term in order to improve the solubility of a practically insoluble drug, griseofulvin (GF). GF nanoparticles (GFNPs) prepared by high-pressure homogenization were micronized to about 45 nm (mean particle size). GFNPs were ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kamiya S,Nozawa Y,Miyagishima A,Kurita T,Sadzuka Y,Sonobe T

更新日期：2006-02-01 00:00:00

abstract：:Separation of twelve sympathomimetic amines and related compounds by micellar electrokinetic chromatography (MEKC) with UV absorbance detection is described. These amines were well separated within 25 min using 50 mM sodium tetraborate solution containing 15 mM sodium dodecylsulfate (SDS) of pH 9.3 as a running soluti...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroda N,Sato D,Ohyama K,Wada M,Nakahara Y,Nakashima K

更新日期：2001-07-01 00:00:00

abstract：:The compound tentatively named TL-1 was isolated from Talaromyces luteus as a metabolite having monoamine oxidase (MAO) inhibitory potency. TL-1 showed mixed-type inhibition of MAO in mouse liver when kynuramine was used as a substrate, and the IC50 was 6.6 microM. The inhibition constants (Ki) for MAO-A and -B in mou...

journal_title：Chemical & pharmaceutical bulletin

authors： Satoh Y,Yamazaki M

更新日期：1989-01-01 00:00:00

abstract：:Clotrimazole (CT)-containing proliposomes were prepared by penetrating an ethanol solution of CT and Egg phosphatidylcholine (PC) into microporous sorbitol particles, followed by vacuum evaporation of the solvent. As a result, CT proliposomes with free-flowing flowability were obtained. On contact with water, the prol...

journal_title：Chemical & pharmaceutical bulletin

authors： Ning MY,Guo YZ,Pan HZ,Yu HM,Gu ZW

更新日期：2005-06-01 00:00:00

abstract：:From the MeOH extract of the aerial part of Vietnamese Orthosiphon stamineus, five new isopimarane-type diterpenes [orthosiphols F-J (1-5)] and two new diterpenes [staminols A (6) and B (7)] with a novel carbon-framework, to which we proposed the name "staminane", and three new highly-oxygenated staminane-type diterpe...

journal_title：Chemical & pharmaceutical bulletin

authors： Tezuka Y,Stampoulis P,Banskota AH,Awale S,Tran KQ,Saiki I,Kadota S

更新日期：2000-11-01 00:00:00

abstract：:An uncommon, previously unreported p-quinone-lignan compound called justicidone (4-(1,3-benzodioxol-5-yl)-6-methoxynaphtho[2,3-c]furan-1,5,8(3H)-trione) (2), along with the known savinin (1) were isolated from Justicia hyssopifolia (Acanthaceae). Their structures were determined by spectroscopic methods. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Andrés Pérez J,Boluda C,López H,Manuel Trujillo J

更新日期：2004-01-01 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：:A new synthetic method for chiral oxazolidinone derivatives, therapeutic agents for treating urinary disturbance, is described. The condensed compound obtained from chiral 1-amino-3-phenyl-2-propanol and 1-phenyl-3-morpholino-1-propanone was reduced with Me4NBH(OAc)3 to give the intermediate, 1-(3-morpholino-1-phenylp...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida S,Yamamoto M,Mochizuki N,Nohira H

更新日期：1999-08-01 00:00:00

abstract：:Chiral building block syntheses of promising drugs were achieved using two types of catalytic stereoselective cyanosilylations of aldehydes promoted by Lewis acid-Lewis base bifunctional catalysts 1 and 2 as the key steps (diastereoselective cyanosilylation of amino aldehyde and enantioselective cyanosilylation). In t...

journal_title：Chemical & pharmaceutical bulletin

authors： Nogami H,Kanai M,Shibasaki M

更新日期：2003-06-01 00:00:00

abstract：:A novel series of quinoline azodyes (5-(4'-derivatives phenyldiazo)-8-hydroxy-7-quinolinecarboxaldehyde)) (HL1-HL5) has been prepared and characterized by elemental analyses, 1H-NMR and IR spectra. The IR spectral data indicate that the compounds can exist in two resonance structures. Proton-ligand dissociation consta...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Sonbati AZ,El-Bindary AA,Shoair AGF,Younes RM

更新日期：2001-10-01 00:00:00

abstract：:Novel hybrid L-ascorbic acid (vitamin C) derivatives with other biologically active substances, 5-hydroxy-2-hydroxymethyl-beta-pyrone (kojic acid) and alpha-tocopherol (vitamin E), linked at the C-2 or C-3 hydroxyl group were synthesized, and their thermal stability and inhibitory effects on tyrosinase activity, activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morisaki K,Ozaki S

更新日期：1996-09-01 00:00:00

abstract：:N-(2-Dimethylaminoethyl)carboxamide (1a-d), 2-dimethylaminoethyl alkyl ether (2a, b), and 2-dimethylaminoethyl 2-hydroxy-2-phenethyl ether (3a-c) and its amino and methylene analogues (3d, 4) have been screened for antiamnestic and antihypoxic activities in mice. A clear reversing effect on electroconvulsive shock-ind...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono S,Yamafuji T,Chaki H,Todo Y,Maekawa M,Kitamura K,Tai M,Narita H

更新日期：1995-09-01 00:00:00

abstract：:Virulence (vir) gene expression of Agrobacterium tumefaciens is activated by plant phenolic compounds such as alpha-hydroxyacetosyringone (HOAS), acetosyringone (AS), methyl syringate, coniferyl alcohol and sinapyl alcohol. Inositol was found to be a potentiating factor of vir-inducing activity, which enhanced the vir...

journal_title：Chemical & pharmaceutical bulletin

authors： Song YN,Shibuya M,Ebizuka Y,Sankawa U

更新日期：1991-10-01 00:00:00

abstract：:A method for scale-up of a lubricant mixing process in a V-type blender was proposed. Magnesium stearate was used for the lubricant, and the lubricant mixing experiment was conducted using three scales of V-type blenders (1.45, 21 and 130 L) under the same fill level and Froude (Fr) number. However, the properties of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Horibe M,Sonoda R,Watano S

更新日期：2018-01-01 00:00:00

abstract：:An efficient synthesis of the antiviral and antioxidative chromene (1) was achieved. A small amount of chromene 1 could be derived from plastoquinones 2 and 3, the major constituents of the brown alga, Sargassum micracanthum. By the following synthetic scheme involving its application, many kinds of analogs can be syn...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori J,Iwashima M,Takeuchi M,Saito H

更新日期：2006-03-01 00:00:00

abstract：:Remote loading of insulin and bovine serum albumin (BSA) into neutral or positively-charged liposomes by incubation under a transmembrane pH gradient or non-pH gradient was investigated. Trapping efficiencies in several incubation conditions were compared with those of the conventional reverse-phase evaporation vesicl...

journal_title：Chemical & pharmaceutical bulletin

authors： Hwang SH,Maitani Y,Takayama K,Nagai T

更新日期：2000-03-01 00:00:00

abstract：:Hyaluronate-hydroxyethyl acrylate blend gel (HA-PHEA) were prepared to modify the brittleness of hyaluronate gel (HA) and the characteristics of HA-PHEA gel were compared with those of HA and polyhydroxyethyl acrylate (PHEA) gels. These gels were high in water content and transparent. HA-PHEA gel was improved in visco...

journal_title：Chemical & pharmaceutical bulletin

authors： Jin Y,Yamanaka J,Sato S,Miyata I,Yomota C,Yonese M

更新日期：2002-10-01 00:00:00

abstract：:The interaction of halofantrine with phosphatidylcholine and phosphatidylethanolamine bilayers has been investigated by differential scanning calorimetry. Halofantrine caused a broadening of the gel to liquid crystalline phase transition endotherm of the phosphatidylcholines. A decrease in the transition temperature T...

journal_title：Chemical & pharmaceutical bulletin

authors： Lim LY,Go ML

更新日期：1999-06-01 00:00:00

abstract：:A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted-1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydr...

journal_title：Chemical & pharmaceutical bulletin

authors： Megally Abdo NY,Kamel MM

更新日期：2015-01-01 00:00:00

abstract：:Two new cangorosin A type triterpene dimers, which composed of two triterpene units jointed by two ether linkages between the A and B rings, were isolated from the Brazilian medicinal plant "xuxuá" (Maytenus chuchuhuasca). Structures of new isolates, xuxuasins A (1) and B (2), were established based on several spectro...

journal_title：Chemical & pharmaceutical bulletin

authors： Shirota O,Sekita S,Satake M,Morita H,Takeya K,Itokawa H

更新日期：2004-09-01 00:00:00

abstract：:Three new hydrolyzable tannins, euphormisins M1, M2, and M3, were isolated from Euphorbia humifusa WILLD., and respectively characterized as 1,3,6-tri-O-galloyl-4-O- brevifolincarboxyl-beta-D-glucose (19), an oxidative metabolite (23) of geraniin, and 1,3,6-tri-O-galloyl-alpha-D-glucose (18), by spectroscopic and chem...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Amakura Y,Liu YZ,Okuda T

更新日期：1994-09-01 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：:Improved synthesis of the trans-3,5-disubstituted pyrrolidin-3-ylthio side-chain of the novel carbapenem 1 was achieved via stereoselective reduction of the 1-aryl-1-butanone derivative 5 and successive intramolecular cyclization of the resulting chiral alcohol 6. The 1-aryl-1-butanone derivative 5 was obtained by a c...

journal_title：Chemical & pharmaceutical bulletin

authors： Hashihayata T,Sakoh H,Goto Y,Hirose M,Sakuraba S,Imamura H,Sugimoto Y,Yamada K,Morishima H

更新日期：2001-11-01 00:00:00

abstract：:From Puerariae Radix, the root of Pueraria lobata (Leguminosae), six new oleanene-type triterpene glycosides, called kudzusaponins A1 (1), A2 (2), Ar (3), SA4 (5), and SB1 (6) were isolated together with kudzusaponin A3 (7), soyasaponins SA3 (8), and I (9). The structures of 1-6 were determined to be 3-O-alpha-L-rhamn...

journal_title：Chemical & pharmaceutical bulletin

authors： Arao T,Kinjo J,Nohara T,Isobe R

更新日期：1997-02-01 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：:A series of imidazo[1,2-alpha]pyridinyl-2-oxobenzoxazolidines (4a-i), -3-oxo-2H-1,4-benzoxazines (5a-q), their thio-analogues (4j-p and 5r-t) and 5,6,7,8-tetrahydroimidazo[1,2-alpha]pyridinyl derivatives (8 and 9) were synthesized and tested for anti-stress ulcer activity in rats. Several compounds were found to be mo...

journal_title：Chemical & pharmaceutical bulletin

authors： Katsura Y,Nishino S,Takasugi H

更新日期：1991-11-01 00:00:00

abstract：:A facile stereoselective synthesis of (Z)- and (E)-allyl sulfides has been accomplished from Morita-Baylis-Hillman acetates in one-pot by treatment with benzene thiol in the presence of catalytic amounts of 15% aqueous NaOH and TBAI in DMSO at room temperature. The method has been applied for the synthesis of (Z)-3-(4...

journal_title：Chemical & pharmaceutical bulletin

authors： Das B,Chowdhury N,Damodar K,Banerjee J

更新日期：2007-08-01 00:00:00

abstract：:It is well known that high-pressure carbon dioxide (CO2) lowers the glass transition temperature (Tg) of polymers. We therefore investigated whether Tg depression of high-pressure CO2 results in interparticle bridging of a polymer and the tablet characteristics that makes the manufacture of an orally disintegrating ta...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi M,Shinozuka D,Kondo H,Sako K,Otake K

更新日期：2018-01-01 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