Abstract：
:We synthesized some 4,4'- and 2,2'-dihydroxytriphenylmethane derivatives 3a--e and 4a--c by condensation of phenol 1 and aromatic aldehyde 2 in moderate to good yields (30--83%). Most of them showed significant antiviral activity against herpes simplex virus type 1 (anti-HSV-1 activity) in a plaque reduction assay. The most potent antiviral activity (EC(50)=0.79 microg/ml) was observed in the 4,4'-dihydroxytriphenylmethane derivative 3b. This compound 3b showed lower cytotoxicity (CC(50)=30.2 microg/ml), compared to that of the prototype 3a.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Mibu N,Yokomizo K,Uyeda M,Sumoto Kdoi
10.1248/cpb.53.1171subject
Has Abstractpub_date
2005-09-01 00:00:00pages
1171-4issue
9eissn
0009-2363issn
1347-5223pii
JST.JSTAGE/cpb/53.1171journal_volume
53pub_type
杂志文章abstract：:2-(5-Arylidene-4-oxo-3-phenyl-thiazolidin-2-ylidene)-3-oxo-propionitriles 4a-j were prepared via condensation of aromatic aldehydes with 4-thiazolidinones 3a,b. The latter was obtained via electrophilic attack of phenylisothiocyanate on 3-oxo-propionitriles 1a,b followed by reaction with chloroacetyl chloride under ba...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.c12-00498
更新日期：2012-01-01 00:00:00
abstract：:Detailed chemical studies on the cytotoxic fraction from the leaves of Dysoxylum cumingianum have resulted in the isolation of two new triterpene glucosides, cumingianosides P (18) and Q (19), with an apotirucallane-type skeleton. The structures of 18 and 19 were determined by spectral examinations, and by conversion ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.45.202
更新日期：1997-01-01 00:00:00
abstract：:We used near infrared (NIR) spectroscopy to evaluate the degree of mixing of blended dry syrup (DS) products whose particle sizes are not specified in the Revised 16th Edition of the Japanese Pharmacopoeia, and also evaluated the degree of mixing when powder products or fine granule products were added to DS products....
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.60.624
更新日期：2012-01-01 00:00:00
abstract：:From the ethyl acetate fraction of the stem bark of Camellia japonica, three new triterpenoids, 3beta-O-acetyl-16beta-hydroxy-12-oxoolean (6), 3beta-O-acetyl-16beta-hydroxy-11-oxoolean-12-ene (7), and 3beta-O-acetyl-16beta-hydroxyolean-12-ene (8), along with seven known compounds, 3alpha-hydroxy-1-oxofriedelan (1), fr...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.58.121
更新日期：2010-01-01 00:00:00
abstract：:The effect of propranolol (PPL), phenoxybenzamine (PBZ) or bicuculline (BCL) on the diazepam (DZP)-induced changes of pineal melatonin synthesis in male rats was examined in vivo and in vitro. Administration of PBZ did not affect the inhibitory action of DZP on pineal melatonin synthesis in vivo. A single injection of...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.39.2677
更新日期：1991-10-01 00:00:00
abstract：:Pyrrole-2,5-dicarboxylates were rapidly and selectively reduced to the corresponding mono-alcohol using 3 eq of diisobutylaluminum hydride at 0°C. Pyrrole-2,4-dicarboxylate showed the same reactivity; however, the selectivity decreased with pyrrole-3,4-dicarboxylate. When the nitrogen atom of the pyrrole-2,5-dicarboxy...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.c16-00122
更新日期：2016-01-01 00:00:00
abstract：:Doxazosin mesylate (DXM) sustained release pellets were prepared by an extrusion-spheronization and fluid-bed coating technique. The core pellets containing DXM were prepared by extrusion-spheronization technique, and coated by a fluid-bed coater to control the release of DXM. The factors affecting to properties of pe...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.c12-00767
更新日期：2013-01-01 00:00:00
abstract：:Stereoisomers of thiol proteinase inhibitor (TPI) were synthesized by a conventional solution method. Among them, iNoc-D-Gln-Val-Val-Ala-Ala-pNA weakly inhibited the amidolytic activity of papain, although iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited papain activity fairly potently. However, the other five D-amino acid-cont...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.44.1599
更新日期：1996-08-01 00:00:00
abstract：:This study examined the intestinal transport of five harman alkaloids using the Caco-2 cell monolayer as a model of the human intestinal mucosa. Transport parameters, permeability coefficients and percent transports, were calculated and compared under identical conditions with atenolol. Permeability coefficients were ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.52.394
更新日期：2004-04-01 00:00:00
abstract：:From the most polar fractions of Solidago virga-aurea L. (Compositae), 9 oleanane-type triterpene saponins named solidagosaponins XXI-XXIX (1-9) were isolated, together with a known saponin, virgaureasaponin 2 (10). These saponins are bisdesmosidic glycosides having two monosaccharides at C-3 and four or five monosacc...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.42.617
更新日期：1994-03-01 00:00:00
abstract：:A novel analytical method for the determination of pharmaceutical polymorphs was developed using terahertz spectroscopy. It was found out that each polymorph of a substance showed a specific terahertz absorption spectrum. In particular, analysis of the second derivative spectrum was enormously beneficial in the discri...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.58.76
更新日期：2010-01-01 00:00:00
abstract：:Four new ursane-type triterpenes, 3beta-acetoxy-11alpha-methoxy-12-ursene (1), 3beta-acetoxy-11alpha-ethoxy-12-ursene (2), 3beta-acetoxy-11alpha-hydroperoxy-12-ursene (3), 3beta-hydroxy-11alpha-hydroperoxy-12-ursene (4), and two new oleanane-type triterpenes, 3beta-acetoxy-11alpha-ethoxy-12-oleanene (5), 3beta-acetoxy...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.48.593
更新日期：2000-05-01 00:00:00
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journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.42.2309
更新日期：1994-11-01 00:00:00
abstract：:Sulfonic acid functionalized silica catalyzed the three-component reaction of aromatic amines, alpha,beta-unsaturated aldehydes and beta-keto esters forming the corresponding 1,4-dihydropyridines in short reaction times and in high yields. ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.56.366
更新日期：2008-03-01 00:00:00
abstract：:The latex of Euphorbia nivulia afforded three new ingol diterpenes, 3-acetyl-8-methoxyl-7-angolyl-12-hydroxylingol (7), 3,12-diacetyl-7-hydroxy-8-methoxylingol (8), and 3,12-diacetyl-7-angolyl-8-hydroxylingol (9) along with five known ingol diterpenes 2-6 and a known triterpene cyclonivulinol (1). Their structures wer...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.51.431
更新日期：2003-04-01 00:00:00
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journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.c20-00527
更新日期：2020-01-01 00:00:00
abstract：:Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.c16-00824
更新日期：2017-02-01 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
pub_type： 杂志文章
doi：10.1248/cpb.37.2103
更新日期：1989-08-01 00:00:00
abstract：:A series of 2-acyl-6-methoxy-3,3,14-trimethyl-3,14-dihydro-7H-benzo[b]pyrano[3,2-h]acridin-7-ones (4-6) was prepared by treatment of 6-methoxy-3,3,14-trimethyl-3,14-dihydro-7H-benzo[b]pyrano[3,2-h]acridin-7-one (3) with an excess of an appropriate acyl chloride in the presence of aluminum chloride. Treatment of (+/-)-...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.53.919
更新日期：2005-08-01 00:00:00
abstract：:A new toxic neoanisatin-derivative (1) was isolated from the pericarps of Illicium majus. The structure of this compound was elucidated by spectroscopic data, including the 2D COSY NMR technique. The toxicity of compound 1 is also described. ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.38.291
更新日期：1990-01-01 00:00:00
abstract：:The enzyme tyrosinase regulates melanogenesis and skin hyperpigmentation by converting L-3,4-dihydroxyphenylalanine (L-DOPA) into dopaquinone, a key step in the melanin biosynthesis. The present work deals with design and synthesis of various oxindole-based chalcones as monophenolase and diphenolase activity inhibitor...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.c17-00301
更新日期：2017-01-01 00:00:00
abstract：:Biological activity of thioaurones was not tested so far and the group constitute completely unexplored source of new molecules of pharmacological interest. We report synthesis and evaluation of cytotoxic activity of thioaurone derivatives bearing p-hydroquinone system in ring A. Their activity was found to depend str...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.54.350
更新日期：2006-03-01 00:00:00
abstract：:We have already reported unique compounds containing a N,O-spiro acetal structure as an orally active factor Xa (FXa) inhibitor. This time, we described a N,N-spiro acetal structure as an analogue of the N,O-spiro acetal structure for an orally active FXa inhibitor. The synthesis of these analogues could be achieved i...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.54.1535
更新日期：2006-11-01 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
pub_type： 杂志文章
doi：10.1248/cpb.53.620
更新日期：2005-06-01 00:00:00
abstract：:ZCVI₄-2 is a newly developed furoxan-based nitric oxide-releasing derivative of oleanolic acid. It exhibited strong cytotoxicity against human hepatocellular carcinoma (HCC) in vitro and significantly inhibited the growth of HCC tumors in vivo. However, its low aqueous solubility and toxicity due to the fast release o...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.59.734
更新日期：2011-01-01 00:00:00
abstract：:A series of 1,2,3,4-tetrahydroisoquinoline derivatives containing the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton were prepared and evaluated for their in vitro binding affinities to muscarinic receptors and for antagonism of bradycardia in vivo. Among them, compound 3f had the highest affinity for ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.47.672
更新日期：1999-05-01 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
pub_type： 杂志文章
doi：10.1248/cpb.48.1242
更新日期：2000-08-01 00:00:00
abstract：:Three new 15,16-seco-cycloartane glycosides, which were constructed by a C-C bond cleavage in the D ring, have been isolated from Cimicifuga Rhizome for the first time. Their structures were determined by the use of 2D NMR techniques and chemical evidence. ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.55.789
更新日期：2007-05-01 00:00:00
abstract：:Caragana tibetica KOM. (Fabaceae) is a medicinal plant that has been traditionally used in western part of China. In the course of our screening study on antioxidant activity of medicinal plants, the 70% acetone extract of the stems of C. tibetica was found to have a potent superoxide anion scavenging activity. Tibeti...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.53.1204
更新日期：2005-09-01 00:00:00
abstract：:A novel macrocyclic diterpene, jatrophenone, has been isolated from the whole plant of Jatropha gossypifolia. The structure of the compound was established by detailed studies of its one- and two-dimensional (1D and 2D) NMR spectra. The compound possesses significant antibacterial activity. ...
journal_title：Chemical & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/cpb.51.870
更新日期：2003-07-01 00:00:00
