Synthesis and evaluation of pyrrolin-2-one compounds, a series of plasminogen activator inhibitor-1 inhibitors.

abstract：:Four new compounds 1-4 were obtained from an oxidative coupling reaction of (E)-isorhapontigenin using FeCl(3) as oxidant. Their structures and stereochemistry were determined on the basis of spectroscopic evidence [UV, IR, MS, (1)H-, (13)C-NMR, NOE and 2D NMR], and their possible formation mechanisms were also discus...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao CS,Zhou LX,Lin M

更新日期：2004-02-01 00:00:00

abstract：:Novel 4,5,6,7-tetrahydrothieno[3,2-c]pyridines, 1-thienyl-1,2,3,4-tetrahydroisoquinolines and related compounds, in which the benzene rings of (+)-1 (FR115427) were replaced with heteroaromatic rings such as thiophene, furan, benzothiophene and indole, were synthesized and evaluated for anticonvulsant activity against...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohkubo M,Kuno A,Katsuta K,Ueda Y,Shirakawa K,Nakanishi H,Kinoshita T,Takasugi H

更新日期：1996-04-01 00:00:00

abstract：:Chemical investigation of the soft coral Sinularia leptoclados has afforded three new sesquiterpenoids, leptocladols A (1), B (2), and 1-epi-chabrolidione A (3). The relative structures of 1-3 were determined on the basis of extensive spectroscopic analysis. The relative configuration of 1 was further confirmed by a s...

journal_title：Chemical & pharmaceutical bulletin

authors： Su JH,Chiang MY,Wen ZH,Dai CF,Hsu CH,Sheu JH

更新日期：2010-02-01 00:00:00

abstract：:Alkylidenemalonates were readily dimerized in the presence of SmI2 to give 2,3-disubstituted 1,1,4,4-butanetetracarboxylates as mixtures of meso and racemic isomers in moderate to good yields. The structure of the less polar isomer of tetraethyl 2,3-diphenyl-1,1,4,4-butanetetracarboxylate was determined by X-ray cryst...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita M,Okuyama K,Kawasaki I,Nakamura S,Nagamine R,Tsujita T,Ohta S

更新日期：2000-11-01 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：:The gamma subunit of enolase (gamma-enolase) was purified from the brain tissues of cow, dog, goat, pig, rabbit, and rat. The purification was achieved in only three steps: ammonium sulfate-precipitation, DE 53 cellulose ion-exchange chromatography, and polyacrylamide gel electrophoresis (PAGE) in a preparative mode. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoki T,Tanaka T,Watabe H

更新日期：1992-05-01 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

authors： Zhang J,Gao Y,Su F,Gong Z,Zhang Y

更新日期：2011-01-01 00:00:00

abstract：:Atranorin, lichexanthone, and the (+)-usnic, diffractaic, divaricatic, perlatolic, psoromic, protocetraric, and norstictic acids isolated from the lichens Parmotrema dilatatum (VAIN.) HALE, Usnea subcavata MOTYKA, Usnea sp., Ramalina sp., Cladina confusa (SANT.) FOLMM. & AHTI, Dirinaria aspera HÄSÄNEN, and Parmotrema ...

journal_title：Chemical & pharmaceutical bulletin

authors： Brandão LF,Alcantara GB,Matos Mde F,Bogo D,Freitas Ddos S,Oyama NM,Honda NK

更新日期：2013-01-01 00:00:00

abstract：:A new sesquiterpene 2,9-humuladien-6-ol-8-one (1) was isolated from methanol extract of Zingiber aromaticum, along with 15 known compounds. The structures of the isolated compounds were elucidated on the basis of spectroscopic analyses. The isolated compounds were tested for their inhibitory activity on the metabolism...

journal_title：Chemical & pharmaceutical bulletin

authors： Subehan,Usia T,Kadota S,Tezuka Y

更新日期：2005-03-01 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：:Two new naphthopyrones, cassiasides B2 (1) and C2 (2), were isolated from the seeds (Cassiae Semen) of Cassia obtusifolia L. The structures of the two new compounds 1 and 2 were established as rubrofusarin 6-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-glucopyranosyl-(1-->3)-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-gluc...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitanaka S,Nakayama T,Shibano T,Ohkoshi E,Takido M

更新日期：1998-10-01 00:00:00

abstract：:Binding sites of polyphenolic compounds on human serum albumin (HSA) were investigated using induced Cotton effects on the circular dichroism (CD) spectra. Polyphenolic compounds used in this study are known to be metabolites from tannins and their related polyphenols in food and medicinal plants. The present investig...

journal_title：Chemical & pharmaceutical bulletin

authors： Nozaki A,Kimura T,Ito H,Hatano T

更新日期：2009-09-01 00:00:00

abstract：:In this study we report the synthesis and pharmacological evaluation of four new progesterone derivatives; 17alpha-hydroxy-16beta-methylpregna-4,6-diene-3,20-dione 12, 17alpha-cyclopropylcarbonyloxy-16beta-methylpregna-4,6-diene-3,20-dione 13, 17alpha-cyclobutylcarbonyloxy-16beta-methylpregna-4,6-diene-3,20-dione 14, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ramírez E,Cabeza M,Bratoeff E,Heuze I,Pérez V,Valdez D,Ochoa M,Teran N,Jimenez G,Ramírez T

更新日期：2005-12-01 00:00:00

abstract：:The effect of the surface layering time of lactose carrier particles on the dry powder inhalation properties of salbutamol sulfate was investigated. Lactose carrier particles were layered with vegetable magnesium stearate by physical mixing. In the present study, drug/carrier powder mixtures were designed consisting o...

journal_title：Chemical & pharmaceutical bulletin

authors： Iida K,Hayakawa Y,Okamoto H,Danjo K,Luenberger H

更新日期：2004-03-01 00:00:00

abstract：:In our series of studies on potassium channel openers, several thienylcyanoguanidine derivatives were synthesized and evaluated for smooth muscle relaxation activity in vitro. Among the newly synthesized compounds, N-cyano-N'-(5-cyano-3-thienyl)-N"-tert-pentylguanidine (4b) and N-(5-bromo-3-thienyl)-N'-cyano-N"-tert-p...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshiizumi K,Ikeda S,Nishimura N,Yoshino K

更新日期：1997-12-01 00:00:00

abstract：:Chemical investigations on the sea whip gorgonian coral Junceella juncea have led to the isolation of five new 8-hydroxybriarane diterpenoids, junceols D-H (1-5). The structures of briaranes 1-5 were determined on the basis of spectroscopic methods and the methylenecyclohexane rings were found to exist in boat form in...

journal_title：Chemical & pharmaceutical bulletin

authors： Sung PJ,Pai CH,Hwang TL,Fan TY,Su JH,Chen JJ,Fang LS,Wang WH,Sheu JH

更新日期：2008-09-01 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：:Design of compounds having good anti-tubercular activity is gaining much importance in the field of tuberculosis research due to reemergence of antibiotic resistance strains. In this paper quantitative structure activity relationships (QSAR) were developed on chalcones, chalcone-like compounds, flavones and flavanones...

journal_title：Chemical & pharmaceutical bulletin

authors： Sivakumar PM,Geetha Babu SK,Mukesh D

更新日期：2007-01-01 00:00:00

abstract：:Peptide mimics derived from the first extracellular loop of CCR5 bearing non-peptide spacers in place of Ala-Ala-Ala sequence in the peptide moiety were synthesized, and the effects of these compounds on the inhibition against HIV-1 were examined. Compound 2b having m-aminophenoxyacetic acid derivative as a non-peptid...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda K,Ishii Y,Konishi K,Sato M,Tanaka K

更新日期：2004-12-01 00:00:00

abstract：:The percutaneous penetration of R-(+)- and S-(-)-propranolol (PL) through rat excised skin was investigated in vitro. The flux of S-(-)-PL after application to normal skin was high compared with that of R-(+)-PL. On the other hand, in damaged rat skin, the flux of R-(+)-PL was almost equivalent to that of S-(-)-PL. It...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki K,Kaiho F,Inagaki A,Dohi M,Hazemoto N,Haga M,Hara H,Kato Y

更新日期：1992-04-01 00:00:00

abstract：:Hyosgerin, a new optically active coumarinolignan, has been isolated and characterized along with three other coumarinolignans, venkatasin, cleomiscosin A and cleomiscosin B, from the seeds of Hyoscyamus niger L. The structure was determined on the basis of spectroscopic analysis and chemical conversion. The optical p...

journal_title：Chemical & pharmaceutical bulletin

authors： Sajeli B,Sahai M,Suessmuth R,Asai T,Hara N,Fujimoto Y

更新日期：2006-04-01 00:00:00

abstract：:In the course of an exploratory investigation of antitumor-promoting catechins, 3-O-acyl-(+)-catechins of varying carbon lengths from C(4) to C(18) were assessed for inhibitory effects on the activation of the Epstein-Barr virus early antigen. Like 3-O-acyl-(-)-epigallocatechins, the (+)-catechin derivatives showed pr...

journal_title：Chemical & pharmaceutical bulletin

authors： Uesato S,Taniuchi K,Kumagai A,Nagaoka Y,Seto R,Hara Y,Tokuda H,Nishino H

更新日期：2003-12-01 00:00:00

abstract：:We synthesized the racemates of the five presumed metabolites (1b-f) of (S)-(--)-N-tert-butyl-4,4-diphenyl-2-cyclopentenylamine hydrochloride (FK584, S(--)-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate their inhibitory a...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi K,Miyao Y,Yamano K,Yamamoto T,Terai T,Kusunoki T,Tsubaki K,Shiokawa Y

更新日期：1996-06-01 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：:The synthesis and structure-activity relationships of a series of new azabicycloalkanes as 5-HT3 (serotonin-3) receptor antagonists are described. Our study on the azabicycloalkaneacetamide derivatives showed that 2,3-dihydroindole as the aromatic ring moiety afforded potent 5-HT3 receptor antagonist activity, as judg...

journal_title：Chemical & pharmaceutical bulletin

authors： Kato M,Ito K,Nishino S,Yamakuni H,Takasugi H

更新日期：1995-08-01 00:00:00

abstract：:The effect of metal ions on transcription of the ada gene of Escherichia coli which is promoted by Ada protein in the presence of methylated deoxyribonucleic acid (DNA) was examined in a reconstituted system. Their effect on the O6-methylguanine-DNA methyltransferase (MGTase) activity of Ada protein was also examined....

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi K,Suzuki M,Sekiguchi M,Kawazoe Y

更新日期：1992-09-01 00:00:00

abstract：:Novel cyclic sulfoxides, such as 2-octyl, 2-dodecyl and 2-hexadecyltetrahydrothiophene-1-oxide were prepared by the alkylation of tetrahydrothiophene-1-oxide. Additionally, 2-methyl, 2-ethyl and 2-propyl-5-dodecyltetrahydro-thiophene-1-oxide were conducted by further alkylation. Their enhancing activity on the penetra...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoyagi T,Yamamura M,Matsui K,Nagase Y

更新日期：1992-07-01 00:00:00

abstract：:The structural conversion of the prion protein (PrP) from the normal cellular isoform (PrP(C)) to the posttranslationally modified form (PrP(Sc)) is thought to relate to Cu²⁺ binding to histidine (H) residues. Traditionally, the binding of metals to PrP has been investigated by monitoring the conformational conversion...

journal_title：Chemical & pharmaceutical bulletin

authors： Kojima A,Mabuchi Y,Konishi M,Okihara R,Nagano M,Akizawa T

更新日期：2011-01-01 00:00:00

abstract：:Nuclear factor-κB (NF-κB) is an inducible transcription factor activated by a variety of cytokines, and promotes the transcription of genes involved in cancer, inflammation, autoimmune disease, and viral infection, among others. Because of its involvement in numerous disease processes, considerable research has focuse...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanemaru Y,Momiki Y,Matsuura S,Horikawa T,Gohda J,Inoue J,Okamoto Y,Fujita M,Otsuka M

更新日期：2011-01-01 00:00:00

abstract：:The synthesis and biological evaluation of [2-Valine-A] insulin ([Val2-A]insulin) is reported. In this insulin, the isoleucine residue in position A2, invariant in the majority of mammalian insulins, is substituted by valine. The same substitution, along with four others, occurs naturally in the insulin produced by th...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohta N,Burke GT,Katsoyannis PG

更新日期：1989-03-01 00:00:00