4-Sulfenyl-2-carbamoyl-4-isoxazolin-3-ones: biological isostere to 4-chloro-2-carbamoyl-4-isoxazolin-3-ones.

abstract：:Squalene-2,3-epoxide: lanosterol cyclase was purified from rat liver in five steps as a soluble and homogeneous protein. The purified enzyme showed a single band on SDS-polyacrylamide gel electrophoresis with a molecular weight of 75 kD. In its native state it behaved as a homo-dimer. The isoelectric point of 5.5 and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusano M,Abe I,Sankawa U,Ebizuka Y

更新日期：1991-01-01 00:00:00

abstract：:The reaction of lauroyl isothiocyanate and 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile was used to synthesize the title compound 2. Compound 2 could serve as the main building block in the synthesis of many target heterocyclic systems. Various fused pyrimidines were synthesized in the reactions of compo...

journal_title：Chemical & pharmaceutical bulletin

authors： Hemdan MM,Abd El-Mawgoude HK

更新日期：2015-01-01 00:00:00

abstract：:In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) value...

journal_title：Chemical & pharmaceutical bulletin

authors： Pinna GA,Loriga G,Murineddu G,Grella G,Mura M,Vargiu L,Murgioni C,La Colla P

更新日期：2001-11-01 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：:Dryocrassyl formate, sitostanyl formate, and 12alpha-hydroxyfern-9(11)-ene were isolated from the fresh fronds of Cyathea podophylla. Their structures were elucidated by spectroscopic techniques and synthesis. Ten known triterpenoids, three derivatives of phytol, a stanol, and beta-tocopherol were also identified from...

journal_title：Chemical & pharmaceutical bulletin

authors： Arai Y,Hattori T,Hamaguchi N,Masuda K,Takano A,Shiojima K

更新日期：2003-11-01 00:00:00

abstract：:Licorice is one of the ancient and most frequently applied herbs for its diverse phytochemicals. At present, wild resources of licorice have rapidly declined with increasing demand and the proportion of cultivated products in the market is quickly growing. However, the different level in chemical composition between t...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang C,Cai Z,Shi J,Chen S,Tan M,Chen J,Chen L,Zou L,Chen C,Liu Z,Liu X

更新日期：2019-01-01 00:00:00

abstract：:The title compounds, together with 3-vinylindolizine-1-carbonitriles (4-56%), were prepared in 1-18% yields from the S-alkylation of pyridinium 1-[3-ethoxycarbonyl-1-[cyanomethylthio(thiocarbonyl)]]all ylides with alkyl halides, followed by treatment of the resulting pyridinium salts with a base and then a dehydrogena...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakehi A,Ito S,Hirata K,Zuo P

更新日期：2000-06-01 00:00:00

abstract：:Isoliquiritigenin, glabridin, licoarylcoumarin and licoricidin were identified as strong inhibitors of adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase in waste materials which were obtained during the industrial extraction of glycyrrhizin from licorice roots. The structure-activity relationships of 12 fl...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusano A,Nikaido T,Kuge T,Ohmoto T,Delle Monache G,Botta B,Botta M,Saitoh T

更新日期：1991-04-01 00:00:00

abstract：:From the methanolic extract of Indonesian Orthosiphon stamineus, nine new highly-oxygenated isopimarane-type diterpenes [7-O-deacetylorthosiphol B (1), 6-hydroxyorthosiphol B (2), 3-O-deacetylorthosiphol I (3), 2-O-deacetylorthosiphol J (4), siphonols A-E (5-9)] have been isolated together with nine known diterpenes [...

journal_title：Chemical & pharmaceutical bulletin

authors： Awale S,Tezuka Y,Banskota AH,Adnyana IK,Kadota S

更新日期：2003-03-01 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：:A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The "in vitro" antibacterial activity of these compounds and their corresponding alpha-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobi...

journal_title：Chemical & pharmaceutical bulletin

authors： Rival Y,Grassy G,Michel G

更新日期：1992-05-01 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：: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：:Two novel tropoloisoquinoline alkaloids, Pareirubrines A and B, have been isolated as antileukemic substances from Cissampelos pareira (Menispermaceae), together with the same skeleton alkaloids, grandirubrine and isoimerubrine. Their structures were elucidated by nuclear magnetic resonance (NMR) studies, and their so...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Matsumoto K,Takeya K,Itokawa H,Iitaka Y

更新日期：1993-08-01 00:00:00

abstract：:From Jatropha cilliata M. Arg., a Peruvian medicinal plant, isoorientin and orientin were isolated as anxiolytic components by using the isolation guide of anti-conflict effect in mice. Several related flavonoids were also tested for this effect. Another bioassay-guided isolation using the acetic acid-induced writhing...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuyama E,Okamoto Y,Yamazaki M,Satake M

更新日期：1996-02-01 00:00:00

abstract：:To evaluate the usability of silk protein (sericin, SC) as a sustained-release material, the physicochemical properties of SC and the release profiles of model drugs from SC gel, sponge and film were studied. Heat aids the dissolution of SC. The molecular weight of SC tended to decrease as the heating temperature and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishida A,Yamada M,Kanazawa T,Takashima Y,Ouchi K,Okada H

更新日期：2010-11-01 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

authors： Khan SI,Abourashed EA,Khan IA,Walker LA

更新日期：2004-04-01 00:00:00

abstract：:From the water extract of Brazilian Tabebuia avellanedae, two new iridoids (1, 2) and a new phenylethanoid glycoside (3) have been isolated together with twelve known compounds (4-15). Their structures were determined based on the spectroscopic data. The isolated compounds inhibited nitric oxide (NO) production in lip...

journal_title：Chemical & pharmaceutical bulletin

authors： Awale S,Kawakami T,Tezuka Y,Ueda JY,Tanaka K,Kadota S

更新日期：2005-06-01 00:00:00

abstract：:Four new neo-clerodane diterpenoid alkaloids, named scutebarbatines C-F (1-4), were isolated from the whole plants of Scutellaria barbata D. DON. Their structures were elucidated by spectral analyses (UV, IR, FAB-MS, 1D-NMR and 2D-NMR). In vitro, compounds 1-4 showed significant cytotoxic activities against three huma...

journal_title：Chemical & pharmaceutical bulletin

authors： Dai SJ,Chen M,Liu K,Jiang YT,Shen L

更新日期：2006-06-01 00:00:00

abstract：:2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor γ (PPARγ) and PPARα agonist activities and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otake K,Azukizawa S,Takahashi K,Fukui M,Shibabayashi M,Kamemoto H,Kasai M,Shirahase H

更新日期：2011-01-01 00:00:00

abstract：:A series of phthiobuzone analogs, prepared from potassium phthalimide or phthalandione, have been evaluated for their antiviral activities. Among the candidates, compounds 5j and 5k, which contain the substituted 4-halogenated phenyl ring at N-4',4'' position, show more potent antiviral activity than phthiobuzone agai...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang YJ,Zhao JH,Pan XD,Zhang PC

更新日期：2010-02-01 00:00:00

abstract：:Increase of lipophilicity of cationic doxorubicin (DOX) by its association with a fatty acid ion is of interest for pharmaceutical formulations and could have an impact on the drug delivery into cancer cells. On the basis of spectroscopic analysis of intrinsic DOX fluorescence, this study provides an experimental evid...

journal_title：Chemical & pharmaceutical bulletin

authors： Munnier E,Tewes F,Cohen-Jonathan S,Linassier C,Douziech-Eyrolles L,Marchais H,Soucé M,Hervé K,Dubois P,Chourpa I

更新日期：2007-07-01 00:00:00

abstract：:The objective of this investigation was to clarify the influence of water-soluble polymers on the dissolution behavior of nifedipine from solid dispersions with combined carriers. All the solid dispersions of nifedipine were prepared by the fusion method using nicotinamide and 4 different water-soluble polymers, hydro...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki H,Sunada H

更新日期：1998-03-01 00:00:00

abstract：:Two new C(21) steroidal glycosides, tenacissoside L (1), tenacissoside M (2), were isolated from the stems of Marsdenia tenacissima (ROXB.) WIGHT et ARN. Their structures were elucidated, respectively, by means of chemical and spectral data, including ESI-MS, HR-ESI-MS, 1D-NMR and 2D-NMR. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang S,Lai YH,Tian B,Yang L

更新日期：2006-05-01 00:00:00

abstract：:Novel 1,2,3,4-tetrahydroisoquinoline derivatives bearing directly a cyclic amine at the 2-position were prepared and examined for their bradycardic activities in isolated right atria and in anesthetized rats. The structure-activity relationships (SAR) study revealed that the 2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinol...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakefuda A,Watanabe T,Taguchi Y,Masuda N,Tanaka A,Yanagisawa I

更新日期：2003-04-01 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：:A series of 8-methoxy or 8-methylquinolones bearing novel 3-aminooctahydrocyclopenta[c]pyrrole derivatives at the C-7 position was synthesized, and the pharmacological, physicochemical, and toxicological properties of the individual compounds were evaluated. Novel 8-methylquinolone 7, which includes a 3-amino-7-fluoro...

journal_title：Chemical & pharmaceutical bulletin

authors： Komoriya S,Odagiri T,Inagaki H,Nagamochi M,Miyauchi R,Yoshida KI,Kitamura T,Takahashi H

更新日期：2019-01-01 00:00:00

abstract：:Fe2+-dependent lipid peroxidation in phosphatidylcholine (PC) liposomes, assessed by thiobarbituric acid-reactive substances (TBARS) production, was stimulated in the presence of Fe3+ in a concentration-dependent manner. The rates of nitroblue tetrazolium (NBT) reduction and Fe2+ oxidation (Fe2+ disappearance and Fe3+...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohyashiki T,Kadoya A,Kushida K

更新日期：2002-02-01 00:00:00

abstract：:Six polyphenolic acids (1-6), including the three new compounds citriodolic acids A, B, and C (1-3), were isolated from the leaves of Eucalyptus citriodora. Their structures were elucidated by spectroscopic methods including one dimensional (1D)- and 2D-NMR, high-resolution electrospray ionization (HR-ESI)-MS, and cir...

journal_title：Chemical & pharmaceutical bulletin

authors： Lin SQ,Zhou ZL,Yin WQ

更新日期：2016-11-01 00:00:00

abstract：:Chemical reactivity descriptors and lipophilicyty (log P) were evaluated via semi-empirical method for the quantum calculation of molecular electronic structure (PM3) in order to clarify the structure-cytotoxic activity relationships of disubstutited thioureas. Analysed compounds were obtained by the linkage of 2-amin...

journal_title：Chemical & pharmaceutical bulletin

authors： Filipowska A,Filipowski W,Tkacz E,Nowicka G,Struga M

更新日期：2016-01-01 00:00:00