Ab initio molecular orbital study of the reactivity of active alkyl groups. VII. Solvent effects on the formation of enolate isomers from 2-butanone with methoxide anion in methanol.

abstract：:Two series of new pyridines bearing thiazoline (3a--n) and thiazolidinone (5a--e) moieties were prepared via the cyclization of the corresponding substituted pyridyl thiourea (2a--g) with an appropriately substituted phenacyl bromide or chloroacetic acid, respectively. The antimicrobial activity was determined for rep...

journal_title：Chemical & pharmaceutical bulletin

authors： Hassan HY,el-Koussi NA,Farghaly ZS

更新日期：1998-05-01 00:00:00

abstract：:The admixture of a steroid ointment and a moisturizing cream is frequently prescribed to patients suffering from atopic dermatitis. For the mixing operation, a revolution/rotation-type hybrid mixer is widely used in pharmacy. The purpose of this study was to monitor the mixed state of the admixtures during the mixing ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokokawa M,Setoyama H,Okada K,Hayashi Y,Machida Y,Onuki Y,Obata Y

更新日期：2018-01-01 00:00:00

abstract：:To develop non-prodrugs of taxoids with satisfactory stability in vivo, high water-solubility, and potent antitumor activity, we prepared several 10-O-sec-aminoethyl docetaxel analogs (3) and evaluated their cytotoxicity against mouse leukemia and human tumor cell lines, microtubule disassembly-inhibitory activity, an...

journal_title：Chemical & pharmaceutical bulletin

authors： Uoto K,Takenoshita H,Yoshino T,Hirota Y,Ando S,Mitsui I,Terasawa H,Soga T

更新日期：1998-05-01 00:00:00

abstract：:A model based on solubility parameters is proposed to predict the solubility curves of antihelmintic drugs at several temperatures, including aqueous and non-aqueous mixtures. The solubility of the drugs was measured in ethanol-water and ethanol-ethyl acetate mixtures at 15-35 degrees C (mebendazole) and at 25 degrees...

journal_title：Chemical & pharmaceutical bulletin

authors： Bustamante P,Muela S,Escalera B,Peña A

更新日期：2010-05-01 00:00:00

abstract：:Phthalimidoacetyl isothiocyanate underwent addition-cyclization reactions with some nitrogen and carbon nucleophilic reagents. Simultaneous or subsequent cyclization of the obtained adducts gave target heterocyclic systems such as 1,2,4-triazoles, 1,3-diazines, 1,3-oxazines and thiourea attached to a phthalimido moiet...

journal_title：Chemical & pharmaceutical bulletin

authors： Hemdan MM,El-Sayed AA

更新日期：2016-01-01 00:00:00

abstract：:As part of our search for a dual inhibitor possessing both thromboxane A2 (TXA2) receptor antagonistic and TXA2 synthase inhibitory activities, some [[(benzenesulfonamido)alkyl]phenyl]alkanoic acid derivatives possessing a pyridyl or imidazolyl group were synthesized. Their TXA2 receptor antagonistic and TXA2 synthase...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai S,Ogawa N,Suzuki T,Kato K,Ohashi T,Yasuda S,Kato H

更新日期：1996-08-01 00:00:00

abstract：:Four new cycloart-7-ene triterpenol arabinosides, bugbanosides C-F, were isolated from the underground parts of Cimicifuga simplex Wormsk. (Ranunculaceae). The structures were elucidated as 12beta-acetoxy-3beta,15alpha,-24R,25-tetrahydroxy-16,23-dione-cycloart-7-ene 3-O-alpha-arabinopyranoside, 12beta-acetoxy-24R,25-e...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusano A,Shibano M,Tsukamoto D,Kusano G

更新日期：2001-04-01 00:00:00

abstract：:Heparan sulfate proteoglycan was extracted from bovine lens capsules by 0.45 M NaCl/2 M urea and purified using ion-exchange chromatography and gel filtration. The proteoglycan was found to consist of protein and carbohydrate in a ratio of 75 to 25. The estimated average molecular weight of the heparan sulfate proteog...

journal_title：Chemical & pharmaceutical bulletin

authors： Onodera S

更新日期：1991-04-01 00:00:00

abstract：:Liposome uptake by HepG2 human hepatoma cells was investigated in comparison with the uptake by J774 murine macrophage-like cells. HepG2 cells accumulated liposomes (egg yolk phosphatidylcholine (EPC)/Chol; 75/25, diameter 0.2 micron) at 37 degrees C comparably to J774 macrophage-like cells. Confocal microscopic obser...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishiwata H,Sato SB,Kobayashi S,Oku M,Vertut-Doï A,Miyajima K

更新日期：1998-12-01 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：:Bis[2-[(E)-2-octenoylamino]ethyl] disulfide (compd. I-3) inhibited collagen- and arachidonic acid-induced rat platelet aggregation, although not adenosine 5'-diphosphate (ADP)-induced rat platelet aggregation. Based on these results, we then investigated the inhibitory effect of compd. I-3 on thromboxane B2 formation ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimura T,Nakajima H,Tsujikawa K,Yasuda N,Haruyama M,Okabe M,Iwai M,Yokoyama K

更新日期：1989-03-01 00:00:00

abstract：:Tetrasubstituted (Z)-alkenes were readily prepared through the Horner-Wadsworth-Emmons reactions of methyl 2-[bis(2,2,2-trifluoroethyl)phosphono]propionate with aryl alkyl ketones by employing Sn(OSO(2)CF(3))(2) and N-ethylpiperidine. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sano S,Takehisa T,Ogawa S,Yokoyama K,Nagao Y

更新日期：2002-09-01 00:00:00

abstract：:A series of [2-(omega-phenylalkyl)phenoxy]alkylamines was synthesized and their 5-hydroxytryptamine2 (5-HT2) and/or dopamine2 (D2) receptor antagonistic activities were examined in vitro. [2-(4-Phenylbutyl)phenoxy]alkylamines showed strong inhibition of both 5-HT2 and D2 receptors. In particular, [2-(4-Phenylbutyl)phe...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka N,Goto R,Ito R,Hayakawa M,Ogawa T,Fujimoto K

更新日期：1998-04-01 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：:The reaction of the N-furfuryloxamic acid sodium salt (12) with 1,1'-oxalyldiimidazole (ODI) yielded the imidazolide (13) as an intermediate, and this directly reacted with 2-aminothiazole derivatives (14) or 2-aminobenzothiazole derivatives (15) under essentially neutral conditions to afford the N'-12-(substituted th...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa T,Tsutsui C

更新日期：2000-09-01 00:00:00

abstract：:ZnAB has the combined structure of N,N-bis(2-pyridylmethyl)ethylenediamine as a specific chelater for Zn(2+) and 1,3,5,7-tetramethyl-8-phenyl-boron dipyrromethene as a fluorophore. Complexation of ZnAB with Zn(2+) produces a remarkable enhancement of fluorescence intensity. ZnAB has the advantages of less sensitivity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koutaka H,Kosuge J,Fukasaku N,Hirano T,Kikuchi K,Urano Y,Kojima H,Nagano T

更新日期：2004-06-01 00:00:00

abstract：:The bitter and sweet forms of a plant species differing with alkaloid contents may provide a model system for investigation of alkaloid biosynthesis at a molecular level. The pattern and concentration of quinolizidine alkaloids were determined by capillary GC-MS in bitter and sweet plants of Lupinus angustifolius. Bit...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirai MY,Suzuki H,Yamazaki M,Saito K

更新日期：2000-10-01 00:00:00

abstract：:An efficient stereocontrolled total synthesis of (+)-biotin (1) has been achieved via the intermediacy of Roche's lactone 5 starting from cis-1,3-dibenzyl-2-imidazole-4,5-dicarboxylic acid (2). The bifunctional cinchona alkaloid-derived squaramide-promoted enantioselective alcoholysis was utilizing as a tool for the c...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen XX,Xiong F,Fu H,Liu ZQ,Chen FE

更新日期：2011-01-01 00:00:00

abstract：:Anhydrous theophylline was prepared by heating theophylline monohydrate at temperatures between 60 degrees C and 140 degrees C. The effects of dehydration temperatures on the moisture absorption and dissolution behavior of anhydrous theophylline were investigated in this study. The hydration rate of anhydrous theophyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2001-12-01 00:00:00

abstract：:Six new cyclic peptides, gypsophin A-F (1-6), were isolated from Gypsophila oldhamiana. Their structures were elucidated by extensive NMR and chemical degradation. Compound 3 exhibited moderate activity of antiplatelet aggregation in vitro. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang G,Luo JG,Yang MH,Wang XB,Kong LY

更新日期：2013-01-01 00:00:00

abstract：:Further isolation work on the water-soluble fraction of a MeOH extract of Tricalysia dubia afforded one new megastigmane gentiobioside, named tricalysionoside A (1), and three sulfates, named sulfatricalysines A-C (2-4). Extensive isolation work on the 1-BuOH-soluble fraction of a MeOH extract of T. dubia yielded sulf...

journal_title：Chemical & pharmaceutical bulletin

authors： Shitamoto J,Sugimoto S,Matsunami K,Otsuka H,Shinzato T,Takeda Y

更新日期：2011-01-01 00:00:00

abstract：:A facile stereoselective synthesis of (Z)- and (E)-allyl sulfides has been accomplished from Morita-Baylis-Hillman acetates in one-pot by treatment with benzene thiol in the presence of catalytic amounts of 15% aqueous NaOH and TBAI in DMSO at room temperature. The method has been applied for the synthesis of (Z)-3-(4...

journal_title：Chemical & pharmaceutical bulletin

authors： Das B,Chowdhury N,Damodar K,Banerjee J

更新日期：2007-08-01 00:00:00

abstract：:First, Raddeanin A, a cytotoxic oleanane-type triterpenoid saponin isolated from Anemone raddeana REGEL, was synthesized. Stepwise glycosylation was adopted in the synthesis from oleanolic acid, employing arabinosyl, glucosyl and rhamnosyl trichloroacetimidate as donors. The chemical structure of Raddeanin A was confi...

journal_title：Chemical & pharmaceutical bulletin

authors： Qian S,Chen QL,Guan JL,Wu Y,Wang ZY

更新日期：2014-01-01 00:00:00

abstract：:As the glycosyl constituents of Ficus pumila L. fruits (Moraceae), three new sesquiterpenoid glucosides, pumilasides A, B and C were isolated together with benzyl beta-D-glucopyranoside, (E)-2-methyl-2-butenyl beta-D-glucopyranoside and rutin. Their structures were characterized as (1S,4S,5R,6R,7S,10S)-1,4,6-trihydrox...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima J,Kimizuka K,Tanaka Y

更新日期：2000-01-01 00:00:00

abstract：:Chemical investigation on the stem of a Chinese mangrove plant Bruguiera sexangula var. rhynchopetala (Rhizophoraceae) resulted in the isolation and characterization of four new phenolic glycosides rhyncosides A-D (1-4), and two new lignan derivatives namely rhyncosides E-F (5-6), along with twelve known phenolic cons...

journal_title：Chemical & pharmaceutical bulletin

authors： Bao S,Ding Y,Deng Z,Proksch P,Lin W

更新日期：2007-08-01 00:00:00

abstract：:A series of 4-aza-5 alpha-androstane compounds with one or two aromatic moieties in the carbamoyl group at the C-17 position were synthesized and their inhibitory activities for rat and human prostatic testosterone 5 alpha-reductase were tested in vitro. Compounds with one aromatic moiety in the carbamoyl group showed...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurata H,Ishibashi K,Saito S,Hamada T,Horikoshi H,Furukawa Y,Kojima K

更新日期：1996-01-01 00:00:00

abstract：:Using CPG support linked with 5-deazaflavin, the 5-deazaflavin modified oligodeoxynucleotides at 3'-end(ODN-dF1) were synthesized. The thermal stability of the duplex of ODN-dF1 with its complement was higher than that of oligonucleotide linked to 5-deazaflavin at 5'-end internucleotide linkage. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura Y,Akiyama T,Bessho K,Yoneda F

更新日期：1993-07-01 00:00:00

abstract：:The constituents of the MeOH extract of Salvia miltiorhiza BUNGE, which showed strong aldose reductase (AR) inhibitory activity, were examined, and two new abietane-type diterpenoids, danshenol A (1) and danshenol B (2), were isolated together with six known ones: dihydrotanshimme I (3), cryptotanshinone (4), tanshino...

journal_title：Chemical & pharmaceutical bulletin

authors： Tezuka Y,Kasimu R,Basnet P,Namba T,Kadota S

更新日期：1997-08-01 00:00:00

abstract：:In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-(spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Kakefuda A,Nagaoka H,Yamamoto O,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:Jellies for oral administration are dosage forms that contain water, as stipulated in the Japanese Pharmacopeia, and heat is generally applied to the jellies during the manufacturing process. Therefore, it is difficult to formulate drugs that may be affected adversely by water and/or heat. To solve this problem, we tr...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakino Y,Hishikawa Y,Onodera R,Tahara K,Takeuchi H

更新日期：2017-01-01 00:00:00