Convenient one-pot synthesis of 2-oxazolines from carboxylic acids.

abstract：:The effects of storage on the crystallization, dissolution and absorption of tolbutamide from amorphous tolbutamide-2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) complex were investigated, in comparison with those of polyvinylpyrrolidone (PVP) solid dispersion. The amorphous solid complex of tolbutamide with HP-beta...

journal_title：Chemical & pharmaceutical bulletin

authors： Kimura K,Hirayama F,Arima H,Uekama K

更新日期：2000-05-01 00:00:00

abstract：:Seven halogenated derivatives of delta 9-tetrahydrocannabinol (delta 9-THC, 1) substituted on the aromatic ring at the 2 and/or 4 position, 2 (4)-fluoro- (2), 2,4-difluoro- (3), 2-chloro- (4), 2-bromo- (5), 2,4-dibromo- (6), 2-iodo- (7) and 2,4-diiodo-delta 9-THC (8) were synthesized and pharmacological effects such a...

journal_title：Chemical & pharmaceutical bulletin

authors： Usami N,Kobana K,Yoshida H,Kimura T,Watanabe K,Yoshimura H,Yamamoto I

更新日期：1998-09-01 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

authors： Yang CS,Hashimoto M,Baba N,Takahashi M,Kaneto H,Kawano N,Kouno I

更新日期：1990-01-01 00:00:00

abstract：:One novel sesquiterpene with new skeleton, (6S)-2-methyl-6-(4-hydroxyphenyl-3-methyl)-2-hepten-4-one (1), two new bisabolane sesquiterpenes, (6S)-2-methyl-6-(4-hydroxyphenyl)-2-hepten-4-one (2), (6S)-2-methyl-6-(4-formylphenyl)-2-hepten-4-one (3), and two calebin derivatives, 4''-(4'''-hydroxyphenyl-3'''-methoxy)-2''-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng Y,Qiu F,Takahashi K,Liang J,Qu G,Yao X

更新日期：2007-06-01 00:00:00

abstract：:Nitroxyl (HNO), a one-electron-reduced form of nitric oxide, has various biological activities, including a cardioprotective effect. Here, we first synthesized another, more hydrophilic photocontrollable HNO donor (3), which can release HNO in a spatially and temporally controlled manner, and then examined the propert...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuo K,Nakagawa H,Adachi Y,Kameda E,Aizawa K,Tsumoto H,Suzuki T,Miyata N

更新日期：2012-01-01 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：:N-1 and N-2 substituted pyrazolo[4,5-g]pyrido[1,2-a]benzimidazoles were prepared regioselectively, and cytotoxicities evaluated in vitro against K562 and HL60 cells. All compounds displayed weaker activity than doxorubicin against sensitive lines, but showed the same activity against resistant cell lines (multidrug re...

journal_title：Chemical & pharmaceutical bulletin

authors： Dupuy M,Pinguet F,Blache Y,Chavignon O,Teulade JC,Chapat JP

更新日期：1998-11-01 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：:A novel lead compound, N-(3-[4-(4-fluorobenzoyl)piperidin-1-yl]propyl)-1-methyl-5-oxo-N-phenylpyrrolidine-3-carboxamide (1), was identified as a CCR5 antagonist by high-throughput screening using [(125)I]RANTES and CCR5-expressing CHO cells. The IC(50) value of 1 was 1.9 microM. In an effort to improve the binding aff...

journal_title：Chemical & pharmaceutical bulletin

authors： Imamura S,Ishihara Y,Hattori T,Kurasawa O,Matsushita Y,Sugihara Y,Kanzaki N,Iizawa Y,Baba M,Hashiguchi S

更新日期：2004-01-01 00:00:00

abstract：:A new fluorinated analog of vitamin D2, 24-epi-26,26,26,27,27,27-hexafluoro- 1 alpha,25-dihydroxyvitamin D2, was efficiently synthesized starting from (R)-4-isopropyl-3-propionyl-2- oxazolidinone with high stereochemical control. In all four physiological test systems, the fluorinate vitamin D2 analog was found to be ...

journal_title：Chemical & pharmaceutical bulletin

authors： Iseki K,Oishi S,Namba H,Taguchi T,Kobayashi Y

更新日期：1995-11-01 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：:Values of inhibition constants, Ki, and concentrations required for 50% inhibition, IC50, for a collection of structurally diverse competitive inhibitors of calf spleen purine nucleoside phosphorylase have been determined employing inosine as substrate. These values have been employed to create predictive quantitative...

journal_title：Chemical & pharmaceutical bulletin

authors： Andricopulo AD,Yunes RA

更新日期：2001-01-01 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

authors： Miyase T,Inose Y,Ueno A

更新日期：1994-03-01 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

abstract：:A new monomethylated ganglioside, DSG-A (3), was obtained, together with four known gangliosides, compounds (1, 2, 4, 5), from the lipid fraction of the chloroform/methanol extract of the ovary of the sea urchin Diadema setosum. The structures of the new ganglioside was determined on the basis of chemical and spectros...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada K,Tanabe K,Miyamoto T,Kusumoto T,Inagaki M,Higuchi R

更新日期：2008-05-01 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：:Enantioselective fluorinating agents, (R)- and (S)-,N-fluoro-3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (BNBT-F, 2) are readily prepared in 3 steps from racemic 3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (5) via optical resolution and fluorination. These agents m...

journal_title：Chemical & pharmaceutical bulletin

authors： Shibata N,Liu Z,Takeuchi Y

更新日期：2000-12-01 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

abstract：:Panaxacol (1) and dihydropanaxacol (2), cytotoxic polyacetylenes isolated from the callus of Panax ginseng, were synthesized starting from D-(-)-diethyl tartrate. The absolute configuration of 1 was determined to be 9R, 10R and the absolute configuration at C-3 of 2 was tentatively assigned as 3S by the application of...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujimoto Y,Satoh M,Takeuchi N,Kirisawa M

更新日期：1990-06-01 00:00:00

abstract：:We have developed a novel organometallic catalysis and applied it to drug discovery. Two new catalysts were found, ruthenium hydride with a nitrogen-containing heterocyclic carbene (A) and an organopalladium catalyst supported on a sulfur-terminated semiconductor, gallium arsenide (001) (B). Both catalysts are environ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arisawa M

更新日期：2007-08-01 00:00:00

abstract：:We have developed a competitive enzyme immunoassay for a drug, which was a newly synthesized anti-ulcer agent, using an enzyme immunoassay. The polyclonal anti-drug antibody coupled to biotin, peroxidase labeled drug derivatives as a tracer, and a small column of Sepharose 4B covalently bound to avidin were used in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Okumura T,Asano T,Adachi T,Hirano K

更新日期：1991-07-01 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：:The pharmacokinetic profiles of the hypoglycemic agent, acetohexamide (AH) and its major active metabolite, hydroxyhexamide (HH) were studied in three species of laboratory animals after intraperitoneal (ipl) administration in comparison with those after intravenous (iv) administration of AH and of the preformed metab...

journal_title：Chemical & pharmaceutical bulletin

authors： Asada S,Nagamine S,Nakae H

更新日期：1989-03-01 00:00:00

abstract：:The structures of new neo-lignans, isoamericanol A (1) and americanol A (2) isolated from the seeds of Phytolacca americana have been elucidated on the basis of spectroscopic data and then confirmed by chemical correlation with the previously known isoamericanin A (3) and americanin A (4). Isoamericanol A, americanol ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Hasegawa T,Toda M,Kodama M,Okazaki H

更新日期：1992-01-01 00:00:00

abstract：:Eight new myriocin analogs, 2-epi-myriocin, Z-14-deoxomyriocin, and nor-deoxomyriocins, and a known myriocin derivative, 14-deoxomyriocin, were synthesized from 2-deoxy-D-glucose via common intermediates in previous myriocin and Z-myriocin syntheses. The immunosuppressive activities of new myriocin analogs and Z-myrio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Yokokawa Y,Okuno Y,Yagi N,Murakami N

更新日期：1994-12-01 00:00:00

abstract：:Enantiomerically pure (1S,3S)- and (1S,3R)-1-amino-3-(hydroxymethyl)cyclopentanes have been efficiently synthesized from L-aspartic acid. The title compounds are isosteres of ribose and may be used to construct nucleoside analogs with important antiviral and antineoplastic activities as demonstrated by a concise total...

journal_title：Chemical & pharmaceutical bulletin

authors： Rapoport H,Chen Y,Mohareb RM,Ahn JH,Sim TB,Ho JZ

更新日期：2003-10-01 00:00:00

abstract：:A new extension of the Hildebrand solubility approach which describes drug solubility in solvent mixtures showing multiple solubility peaks, the chameleonic effect, is proposed. The experimental solubilities of oxolinic acid were measured at 25 degrees C in solvent mixtures of ethanol-water and ethanol-ethyl acetate. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Jouyban-Gharamaleki A,Romero S,Bustamante P,Clark BJ

更新日期：2000-02-01 00:00:00

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

authors： Hanna MM,George RF

更新日期：2012-01-01 00:00:00

abstract：:The metabolites of clentiazem in the urine or bile of rats and dogs were investigated. Fifteen basic, 6 acidic, 2 neutral and 4 conjugated metabolites were isolated. In the present paper, fourteen reference compounds as shown in Charts 1, 2 and 3 were synthesized to identify the structures of the metabolites in proced...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue H,Nakamura S,Otsuka H,Gaino M,Harada T,Matsuki K,Takeda M

更新日期：1994-01-01 00:00:00

abstract：:Bromination of 17-O-acetyltestosterone (17beta-acetoxyandrost-4-en-3-one) (1) was performed with 1, 5, and 10 eq of Br2 in AcOH-Et2O at room temperature. In all cases 2alpha,6beta- (2) and 2alpha,6beta-dibromo-17beta-acetoxyandrost-4-en-3-one (3) were obtained, although the yields were dependent upon the conditions us...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimizu T,Tobari A,Koyanagi J,Kawase M,Saito S

更新日期：2001-01-01 00:00:00