Prediction of the stability of imipenem in intravenous mixtures.

abstract：:A series of 5-(4-aryl- or 4-arylcarbonylpiperazin-1-yl)-5-deoxy-1,4: 3,6-dianhydro-L-iditol 2-nitrates was prepared in order to obtain orally active, nitrate-type vasodilators with reduced side effects. Our drug design was based on a small reduction in the lipophilicity compared to that of 5-deoxy-5-[4-(3-phenylthiopr...

journal_title：Chemical & pharmaceutical bulletin

authors： Hayashi H,Ikeda J,Kubo K,Moriyama T,Karasawa A,Suzuki F

更新日期：1993-06-01 00:00:00

abstract：:Novel C(7)-derivatives of 1-cyclopropyl-6-fluoro-4-quinolone carboxylic acid (3a-o) have been synthesized and evaluated for in vitro antibacterial activity. Compounds 3e (3-aminocyclobutyl), 3g (1-aminocyclopropyl), 3m ((2-aminomethyl)vinyl), and 3o ((1-aminomethyl)vinyl) showed significant inhibitory activity, compar...

journal_title：Chemical & pharmaceutical bulletin

authors： Todo Y,Nitta J,Miyajima M,Fukuoka Y,Ikeda Y,Yamashiro Y,Saikawa I,Narita H

更新日期：1994-10-01 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 sensitive and selective spectrofluorimetric and spectrophotometric stability-indicating methods have been developed for the determination of some non-steroidal anti-inflammatory oxicam derivatives namely lornoxicam (Lx), tenoxicam (Tx) and meloxicam (Mx) after their complete alkaline hydrolysis. The methods are ba...

journal_title：Chemical & pharmaceutical bulletin

authors： Taha EA,Salama NN,Fattah Lel-S

更新日期：2006-05-01 00:00:00

abstract：:Protein nitration at tyrosine residues proceeds to form 3-nitrotyrosine; this product is today used as a biomarker of nitrative stress. We have developed an efficient method with which to identify nitrated peptides and to quantify protein nitration levels in different biological samples by a combination of the chemica...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsumoto H,Taguchi R,Kohda K

更新日期：2010-04-01 00:00:00

abstract：:With the aim of improving of the efficacy and decreasing the side effects of oxybutynin (1), N-[(tetrahydro-3- or 4-pyridyl)methyl]-, N-(4-piperidyl)-, and N-(3- or 4-piperidylalkyl)-2-hydroxyacetamides (3a-n, 4a-g) and the related carboxamides (3o-r, 4h-k, 13', 17) were synthesized and evaluated for inhibitory activi...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi K,Tsubaki K,Mizuno H,Take K,Okumura K,Terai T,Shiokawa Y

更新日期：1994-01-01 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：:The mechanism of the deprotonation of 2-butanone (1) with methoxide anion (2) was studied by ab initio molecular orbital (MO) methods. Calculations of the thermodynamic stabilities of each complex and the regioselectivity of the reaction were performed using a static isodensity surface polarized continuum model (IPCM)...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda H,Yukawa M,Niiya T

更新日期：2006-05-01 00:00:00

abstract：:The superoxide O2(·-) scavenging reaction of (+)-catechin (Cat), quercetin (Que), rutin, and α-tocopherol (α-TOH) as natural phenolic compounds is investigated on the basis of electrochemical and ESR spectral measurements with the aid of density functional theory (DFT) calculations. Reversibility of the O2/O2(·-) redo...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakayama T,Uno B

更新日期：2015-01-01 00:00:00

abstract：:We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazo...

journal_title：Chemical & pharmaceutical bulletin

authors： Suh JH,Yum EK,Cho YS

更新日期：2015-01-01 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：:From the ethanolic extract of the aerial parts of Globularia davisiana, a new iridoid glycoside, davisioside (1), was isolated. Davisioside (1) comprises a rare iridoid aglycone structure with a saturated double bond between C-3 and C-4. Nine known iridoid glycosides, asperuloside (2), alpinoside (3), geniposide (4), ...

journal_title：Chemical & pharmaceutical bulletin

authors： Caliş I,Kirmizibekmez H,Taşdemir D,Ireland CM

更新日期：2002-05-01 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：: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 cardenolide diglycoside (1) was isolated from Nerium oleander together with ten known cardenolide diglycosides 2-11. The structure of compound 1 was established on the basis of their spectroscopic data. The in vitro anti-inflammatory activity of compounds 1-11 was examined on the basis of inhibitory activity aga...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhao M,Bai L,Toki A,Hasegawa R,Sakai J,Hasegawa T,Ogura H,Kataoka T,Bai Y,Ando M,Hirose K,Ando M

更新日期：2011-01-01 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：: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：:Fourteen new bisnor- and norditerpene dilactones, makilactones E-R, having a 7alpha : 8alpha-epoxy-9,11-enolide substructure, were isolated from a methanolic extract of the root and the bark of Podocarpus macrophyllus D. DON (Podocarpaceae) with thirteen known bisnor- and norditerpenoids, and the structures of those n...

journal_title：Chemical & pharmaceutical bulletin

authors： Sato K,Inaba Y,Park HS,Akiyama T,Koyama T,Fukaya H,Aoyagi Y,Takeya K

更新日期：2009-07-01 00:00:00

abstract：:Pharmacokinetics of recombinant tissue-type plasminogen activator (rt-PA) produced in mouse C127 cells (t-PA(C127] and Chinese hamster ovary cells (t-PA(CHO] was investigated in chimpanzees. rt-PA was administered via a constant rate i.v. infusion for 60 min, and t-PA concentration and activity in plasma were measured...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanigawara Y,Hori R,Okumura K,Tsuji J,Shimizu N,Noma S,Suzuki J,Livingston DJ,Richards SM,Keyes LD

更新日期：1990-02-01 00:00:00

abstract：:The anti-anginal drug Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, is thought to modulate the metabolism during myocardial ischemia by activating pyruvate dehydrogenase activity to promote glucose oxidation. Ranolazine and its five principal metabolites: CVT-2512, CVT-2513, CVT-2514, CVT-2738 and CVT-4...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao Z,Gong S,Guan T,Li Y,Wu X,Sun H

更新日期：2009-11-01 00:00:00

abstract：:We developed a rapid and efficient analytical technique for cyclosporine A using HPLC on a column packed with 2-µm nonporous octadecylsilyl silica particles. Under optimized conditions, cyclosporine A was separated with high resolution from other cyclic peptides within 3 min, because the mass transfer resistance in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Kato K,Nanjo K,Goda Y

更新日期：2018-01-01 00:00:00

abstract：:Novel saponins that retain a free carboxyl group at the C-17 position and various sugars linked at the C-3 position of hederagenin aglycone were synthesized via stereospecific glycosylation. Since these natural products represented by Pulsatilla saponin D (PSD) were obtained in very small amounts, the total synthesis ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim M,Park Y,Chung WY,Park KK,Jung M

更新日期：2015-01-01 00:00:00

abstract：:Eight dermorphin (DM) analogs extended at the C-terminus, based on the sequence of prepro-DM deduced from the cDNA, were synthesized by a simultaneous solid-phase method in which a pair of peptides was synthesized in a single vessel. Six peptides (three pairs) were obtained in satisfactory yields (17-37%). In the opio...

journal_title：Chemical & pharmaceutical bulletin

authors： Ambo A,Sasaki Y,Suzuki K

更新日期：1994-04-01 00:00:00

abstract：:When 8-bromoadenosine was incubated with cysteine at pH 7.2 and 37°C, an exclusive product was generated. This product was identified as a cysteine substitution derivative of adenosine at the 8 position, 8-S-L-cysteinyladenosine. The reaction accelerated as pH increased from mildly acidic to basic conditions. The isol...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Ogishi A,Shinohara T,Suito S

更新日期：2018-01-01 00:00:00

abstract：:Intramolecular [2+2] cycloaddition of γ,δ-unsaturated ketenes derived from hex-5-enoyl chloride derivatives gave bicyclo[2.1.1]hexan-5-ones with complete regioselectivity. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hoshikawa T,Tanji K,Matsuo J,Ishibashi H

更新日期：2012-01-01 00:00:00

abstract：:Italian canned tomatoes contain the tomato glycosides esculeosides B-1 (1, 0.0052%) and B-2 (2, 0.0068%) without esculeoside A. Herein, the structure of esculeoside B-1 (1) is characterized to be 3-O-β-lycotetraosyl (5S,22R,23S,25S)-22,26-epimino-16β,23-epoxy-3β,23,27-trihydroxycholestane 27-O-β-D-glucopyranoside. We ...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Fujiwara Y,Ikeda T,Ono M,Murakami K,Zhou JR,Yokomizo K,Nohara T

更新日期：2013-01-01 00:00:00

abstract：:A series of new (5R,8R,10R)-ergoline derivatives was synthesized, and their antihypertensive and dopaminergic activities were tested in conscious spontaneously hypertensive rats and in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra. (5R,8R,10R)-6-Alkyl-8-ergolinemethanols, prepared from...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohno S,Adachi Y,Koumori M,Mizukoshi K,Nagasaka M,Ichihara K,Kato E

更新日期：1994-07-01 00:00:00

abstract：:α,β-Unsaturated amides were incorporated as viable dipolarophiles in a catalytic asymmetric 1,3-dipolar cycloaddition of azomethine imines. The use of a 7-azaindoline auxiliary was essential to acquire sufficient reactivity with excellent diastereoselectivity, likely due to the chelating activation of the amide by the...

journal_title：Chemical & pharmaceutical bulletin

authors： Li Z,Kumagai N,Shibasaki M

更新日期：2020-01-01 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

authors： Fujioka T,Sakurai A,Mihashi K,Kashiwada Y,Chen IS,Lee KH

更新日期：1997-01-01 00:00:00

abstract：:A new heptapeptide GAGPHGG (OC1) was isolated from Carapax trionycis which was a traditional Chinese medicine (TCM) used for treatment of hepatic diseases. The structure of OC1 was characterized by MS, NMR techniques, together with amino acid sequence analysis. The hepatoprotective activity of OC1 was evaluated in viv...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang P,Zhang Y,An Y,Xu K,Xu X,Fu C,Lin J,Xu S,Li Q,Lei H

更新日期：2013-01-01 00:00:00