N-Arylpiperazine-1-carboxamide derivatives: a novel series of orally active nonsteroidal androgen receptor antagonists.

abstract：:A new phenolic glycoside, 3,4,5-trimethoxyphenol-1-(6-xylopyranosyl)glucopyranoside, was isolated together with twenty known compounds identified as koaburaside, 3,4,5-trimethoxyphenol, 5,7-dihydroxychromone-7-neohesperidoside, naringin, neoeriocitrin, p-coumaric acid, vanillin, vanillic acid, coniferyl aldehyde, feru...

journal_title：Chemical & pharmaceutical bulletin

authors： Kosuge K,Mitsunaga K,Koike K,Ohmoto T

更新日期：1994-08-01 00:00:00

abstract：:A new polyhydroxy sterol ester, (25S)-5alpha-cholestane-3beta,6alpha,7alpha,8,15alpha,16beta-hexahydroxyl-26-O-14'Z-eicosenoate (1), together with seven known steroid derivatives (2-8), were isolated from the EtOH extract of the whole body of China Sea starfish Asterina pectinifera. The structure of 1 was determined b...

journal_title：Chemical & pharmaceutical bulletin

authors： Peng Y,Zheng J,Huang R,Wang Y,Xu T,Zhou X,Liu Q,Zeng F,Ju H,Yang X,Liu Y

更新日期：2010-06-01 00:00:00

abstract：:Chitosan-alginate polyelectrolyte complex (PEC) have been prepared in situ in beads and microspheres. This study examines the preparation of suitable chitosan-alginate coacervates for casting into homogeneous PEC films for potential applications in packaging, controlled release systems and wound dressings. Coacervatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yan X,Khor E,Lim LY

更新日期：2000-07-01 00:00:00

abstract：:Manidipine dihydrochloride or benidipine hydrochloride will change to hydrate form in part, when differential scanning calorimetric (DSC) measurement is carried out together with lactose monohydrate. This interaction was accelerated by compressing their mixture. It can be suggested that the interaction may cause by th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hosaka S,Sato M,Ozawa Y,Hamada C,Takahashi Y,Kitamori N

更新日期：2005-05-01 00:00:00

abstract：:Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lo...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

更新日期：2016-01-01 00:00:00

abstract：:To find novel PPAR ligands, we prepared several 3-{3 or 4-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}propanoic acid derivatives which were designed based on the structure of our previous PPARgamma ligand 1. In PPAR binding affinity assays, compound 4, which had an ethoxy group at the C-2 position of the propanoic acid o...

journal_title：Chemical & pharmaceutical bulletin

authors： Usui S,Fujieda H,Suzuki T,Yoshida N,Nakagawa H,Ogura M,Makishima M,Miyata N

更新日期：2007-07-01 00:00:00

abstract：:In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have...

journal_title：Chemical & pharmaceutical bulletin

authors： Yi W,Cao R,Chen Z,Yu L,Wen H,Yan Q,Ma L,Song H

更新日期：2010-05-01 00:00:00

abstract：:Polypropyleneglycol (PPG) was used as a dispersion medium for the preparation of microspheres (MS) consisting of starch, gelatin, whey protein or dextran. Aqueous solutions of the polymers were dispersed in PPG at various initial temperatures and then the systems were cooled to 0.5 degrees C to allow water in the disp...

journal_title：Chemical & pharmaceutical bulletin

authors： Seki T,Shinohara K,Kato N,Uchida M,Natsume H,Morimoto K,Juni K

更新日期：2007-03-01 00:00:00

abstract：:In continuation of our efforts to discover novel nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) as potentially "Safe NSAIDs," we report herein the design, synthesis and evaluation of 21 new NO-NSAIDs of commonly used NSAIDs such as aspirin, diclofenac, naproxen, flurbiprofen, ketoprofen, suli...

journal_title：Chemical & pharmaceutical bulletin

authors： Borhade N,Pathan AR,Halder S,Karwa M,Dhiman M,Pamidiboina V,Gund M,Deshattiwar JJ,Mali SV,Deshmukh NJ,Senthilkumar SP,Gaikwad P,Tipparam SG,Mudgal J,Dutta MC,Burhan AU,Thakre G,Sharma A,Deshpande S,Desai DC,Dubash

更新日期：2012-01-01 00:00:00

abstract：:A series of benzylamides of N-alkylated, N-acylated or free nine cyclic and one linear amino acids as potential anticonvulsants have been synthesized. The structures of the obtained compounds were designed on the basis of the previously determined structure and physicochemical properties/anticvonvulsant activity relat...

journal_title：Chemical & pharmaceutical bulletin

authors： Paruszewski R,Strupińska M,Stables JP,Swiader M,Czuczwar S,Kleinrok Z,Turski W

更新日期：2001-05-01 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：:Six new dammarane-type triterpene diglycosides with a hydroperoxide group, floralginsenosides A, B, C, D, E, and F, were isolated from ginseng flower, the flower buds of Panax ginseng C. A. MEYER, together with seven known dammarane-type triterpene oligoglycosides. The structures of new floralginsenosides were elucida...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Sugimoto S,Nakamura S,Matsuda H

更新日期：2007-04-01 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：:Mucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the t...

journal_title：Chemical & pharmaceutical bulletin

authors： Ruiz-Caro R,Gago-Guillan M,Otero-Espinar FJ,Veiga MD

更新日期：2012-01-01 00:00:00

abstract：:Increase of lipophilicity of cationic doxorubicin (DOX) by its association with a fatty acid ion is of interest for pharmaceutical formulations and could have an impact on the drug delivery into cancer cells. On the basis of spectroscopic analysis of intrinsic DOX fluorescence, this study provides an experimental evid...

journal_title：Chemical & pharmaceutical bulletin

authors： Munnier E,Tewes F,Cohen-Jonathan S,Linassier C,Douziech-Eyrolles L,Marchais H,Soucé M,Hervé K,Dubois P,Chourpa I

更新日期：2007-07-01 00:00:00

abstract：:One new guaiane-type sesquiterpene glycoside, 2'-O-E-caffeoyl-8alpha-hydroxy-11alpha,13-dihydro-3beta-O-beta-D-glucozaluzanin C (1), was isolated from the whole herb of Ainsliaea fragrans (Compositae), together with five known sesquiterpene lactones: 8alpha-hydroxy-11alpha,13-dihydro-3beta-O-beta-D-glucozaluzanin C (2...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang H,Wu T,Yan M,Liu G,Li P,Zhang XQ,Ye WC,Zhang LY

更新日期：2009-06-01 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：: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：:We recently proposed a new hydrogen-accepting parameter, S(HA), for monosubstituted (di)azines on the basis of the heat of formation calculated by the conductor-like screening model (COSMO) method. In this work, S(HA) values for monosubstituted thiophenes and furans were calculated and the results were applied to the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamagami C,Tachikawa H

更新日期：2003-10-01 00:00:00

abstract：:A new flavonol, morin-3-O-alpha-rhamnopyranoside (1), along with four known flavonols, kaempferol 3-O-alpha-rhamnopyranoside (2), kaempferol 3-O-beta-glucopyranoside (3), quercetin 3-O-alpha-rhamnopyranoside (4) and (+)-catechin (5), were isolated from the methanolic extract of Muehlenbeckia platyclada. The structures...

journal_title：Chemical & pharmaceutical bulletin

authors： Yen CT,Hsieh PW,Hwang TL,Lan YH,Chang FR,Wu YC

更新日期：2009-03-01 00:00:00

abstract：:Microcrystalline cellulose (MCC) granules were prepared by wet granulation using a high-shear mixer. Physical characteristics of the granules were investigated using near IR spectrometry, thermogravimetry and isothermal water vapor adsorption. Near IR spectra of dried MCC granules prepared for various granulation time...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Kikuchi H,Yonemochi E,Terada K,Yamamoto K

更新日期：2001-04-01 00:00:00

abstract：:Using a microcalorimetric method, we have measured the heat production in states 3 and 4 respiration of a mitochondrial preparation from rat heart ventricle. Adenosine triphosphate production in state 3 respiration was also determined for the same preparation after heat production was measured. In Tris-buffered soluti...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamura K,Hayatsu H,Watanabe I,Nakano T,Sugawara Y,Nishii Y

更新日期：1989-11-01 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：:Improvement of solubility for fullerene (C60) was studied by cogrinding with cycloamyloses using a ball mill in the solid state. Cycloamylose is a novel cyclic alpha-1,4-glucan produced from synthetic amylose by enzymatic reaction. Although sample solutions showed a pale yellow for the initial period of cogrinding wit...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukami T,Mugishima A,Suzuki T,Hidaka S,Endo T,Ueda H,Tomono K

更新日期：2004-08-01 00:00:00

abstract：:Soluble (SSG, beta-1,3-D-glucan obtained from the culture filtrates of a fungus, Sclerotinia sclerotiorum IFO 9395) and particulate (zymosan) beta-glucans were oxidized by sodium hypochlorite (NaClO), and the oxidized products were analyzed by gel filtration and ion-exchange chromatographies and by limulus G-test to s...

journal_title：Chemical & pharmaceutical bulletin

authors： Miura NN,Ohno N,Adachi Y,Yadomae T

更新日期：1996-11-01 00:00:00

abstract：:Beauveriolides I and III, which are naturally occurring cyclodepsipeptides, have been reported to bind to sterol O-acyltransferase (SOAT), inhibiting its ability to synthesize cholesteryl esters. To facilitate an analysis of the binding site(s) of these compounds, we designed beauveriolide analogues 1a-d wherein the L...

journal_title：Chemical & pharmaceutical bulletin

authors： Masuda Y,Aoyama K,Yoshida M,Kobayashi K,Ohshiro T,Tomoda H,Doi T

更新日期：2016-07-01 00:00:00

abstract：:Analogs related to 1 alpha,25-dihydroxy-2 beta-(3-hydroxypropoxy)vitamin D3 (ED-71) (4), oxa-type and carba-type analogs of vitamin D3 bearing substituents at the 2 beta-position of 1 alpha,25-dihydroxyvitamin D3 (1), were synthesized from the alpha-epoxides (6 and 13). Three analogs, ED-71 (4) and two carba-type anal...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono Y,Watanabe H,Shiraishi A,Takeda S,Higuchi Y,Sato K,Tsugawa N,Okano T,Kobayashi T,Kubodera N

更新日期：1997-10-01 00:00:00

abstract：:A highly sensitive spectrophotometric determination of human serum albumin (HSA) with 3',4',5',6'-tetrachlorogallein (T.Cl.Gall)-Mo(VI) complex in a Triton X-100 + polyvinyl alcohol micellar medium is proposed. This method can be used to determine up to ca. 150 micrograms/10 ml of HSA from the optical absorbance at 64...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujita Y,Mori I,Ikuta K,Nakahashi Y,Kato K,Nakanishi T

更新日期：1989-09-01 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：:The full structures of the two steroidal saponins from Narthecium asiaticum MAXIM. We previously identified as toxic substances by monitoring the toxicity in guinea pigs were phytochemically reinvestigation on the aerial parts of the plant. The desired toxic saponins (6,7) were isolated together with two known lignan ...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue T,Mimaki Y,Sashida Y,Kobayashi M

更新日期：1995-07-01 00:00:00