Synthesis of BMS-309403-related compounds, including [¹⁴C]BMS-309403, a radioligand for adipocyte fatty acid binding protein.

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

abstract：:Rapid and precise compositional analysis of copoly (DL-lactic/glycolic acid) (PLGA) was performed by pyrolysis-gas chromatography/mass spectrometry (Py-GC/MS) combined with one-step hydrolysis and methylation in the presence of tetramethylammonium hydroxide (TMAH). Pyrolysis of PLGA with TMAH gave two characteristic p...

journal_title：Chemical & pharmaceutical bulletin

authors： Urakami K,Higashi A,Umemoto K,Godo M,Watanabe C,Hashimoto K

更新日期：2001-02-01 00:00:00

abstract：:Novel hybrid L-ascorbic acid (vitamin C) derivatives with other biologically active substances, 5-hydroxy-2-hydroxymethyl-beta-pyrone (kojic acid) and alpha-tocopherol (vitamin E), linked at the C-2 or C-3 hydroxyl group were synthesized, and their thermal stability and inhibitory effects on tyrosinase activity, activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morisaki K,Ozaki S

更新日期：1996-09-01 00:00:00

abstract：:Simple one-pot methods for preparation of 2-oxazolines have been developed using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM). Treatment of a mixture of carboxylic acids and 2-haloethylammonium salts with DMT-MM in methanol followed by refluxing in the presence of KOH gives oxazolines. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Takechi Y,Kimura N,Tanaka H,Kunishima M

更新日期：2008-12-01 00:00:00

abstract：:The effects of excipients on the protein stability during lyophilization as well as the storage stability of lyophilized bilirubin oxidase (BO) and beta-galactosidase (GA) formulations were studied using four polymer excipients: dextran, polyvinylalcohol (PVA), poly(acrylic acid) (PAA), and alpha, beta-poly(N-hydroxye...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshioka S,Aso Y,Kojima S,Tanimoto T

更新日期：2000-02-01 00:00:00

abstract：:From the herb of Luffa acutangula ROXB. (Cucurbitaceae), seven oleanane-type triterpene saponins, acutosides A--G, were isolated and their structures were determined. Acutoside A is oleanolic acid 3-O-beta-D-glucopyranosyl-(1----2)-beta-D-glucopyranoside. Acutosides B, D, E, F and G have a common prosapogenin structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagao T,Tanaka R,Iwase Y,Hanazono H,Okabe H

更新日期：1991-03-01 00:00:00

abstract：:Seventeen saponins isolated from the root of Pulsatilla koreana were examined for their in vitro cytotoxic activity against the human solid cancer cell lines, A-549, SK-OV-3, SK-MEL-2, and HCT15, using the SRB assay method, and their in vivo antitumor activity using BDF1 mice bearing Lewis lung carcinoma (LLC). The sa...

journal_title：Chemical & pharmaceutical bulletin

authors： Bang SC,Lee JH,Song GY,Kim DH,Yoon MY,Ahn BZ

更新日期：2005-11-01 00:00:00

abstract：:Three new natural sesquiterpene coumarins, isofeterin (1), lehmannolol (3), sinkianone (4), and one known compound, lehmannolone (2), were isolated from the roots of Ferula teterrima and Ferula sinkiangensis. Their chemical structures were established on the basis of spectroscopic analysis, including X-ray crystallogr...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang JR,An Z,Li ZH,Jing S,Qina HL

更新日期：2006-11-01 00:00:00

abstract：:Four new dibenzocyclooctadiene lignan glucosides, schisandrosides A-D (1-4), as well as two known rare nortriterpenoids, micrandilactone C (5) and propindilactone Q (6), were isolated from the roots of Schisandra chinensis BAILLON (Schisandraceae). The structure of compounds 1-4 were elucidated by physical and spectro...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim HM,Ryu B,Lee JS,Choi JH,Jang DS

更新日期：2015-01-01 00:00:00

abstract：:Total syntheses of structurally and biologically intriguing natural products relying on new synthetic methodologies are described. This article features cinchona alkaloid-catalyzed asymmetric Morita-Baylis-Hillman reactions, heterocycle syntheses based on rhodium-catalyzed C-H amination and indium-catalyzed Conia-ene ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hatakeyama S

更新日期：2014-01-01 00:00:00

abstract：:A series of dibenzofurans were efficiently and conveniently synthesized via one-pot consecutive C(sp(2))-O bond formation reaction (SNAr) in the presence of anhydrous K(2)CO(3), followed by C(sp(2))-C(sp(2)) bond formation reaction (intramolecular palladium-catalyzed aryl-aryl coupling reaction) between aryl halides a...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu H,Fan LL

更新日期：2008-10-01 00:00:00

abstract：:To experimentally clarify a possible stereostructure-activity relationship proposed for H2-receptor antagonists, three 5-aminophenylimidazoles (1, 2 and 3), in which respective amino groups are located on the ortho, meta and para positions of the benzene ring, were synthesized and examined for their conformational cha...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida T,In Y,Inoue M,Kurihara T,Moriomoto K,Morisaka K,Shibata K

更新日期：1990-07-01 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：:Two sesterterpenes, deoxymanoalide (1) and deoxysecomanoalide (2), were isolated from the nudibranch Chromodoris willani collected in Okinawa and their structures determined on the basis of spectroscopic data and chemical conversions. The mollusk feeds on a sponge containing manoalide (3) and secomanoalide (4) and is ...

journal_title：Chemical & pharmaceutical bulletin

authors： Uddin MH,Otsuka M,Muroi T,Ono A,Hanif N,Matsuda S,Higa T,Tanaka J

更新日期：2009-08-01 00:00:00

abstract：:We have examined the lipid peroxide levels in aclacinomycin (ACM)-treated mice by using adriamycin (ADR) as a comparative drug. There was no increase in the lipid peroxide level of the heart at either 3h or 4d after ACM administration (15 mg/kg, i.p.), although the level in the heart of ADR-treated mice was elevated t...

journal_title：Chemical & pharmaceutical bulletin

authors： Sazuka Y,Yoshikawa K,Tanizawa H,Takino Y

更新日期：1989-12-01 00:00:00

abstract：:New fatty polyenic (linoleic, linolenic, arachidonic, linoelaidic) mono esters of erythromycin A have been synthesized by using various reagents such as acyl chloride, carboxylic acid anhydride, and mixed carbonic anhydride. These different ways of activating the fatty acid allowed a regioselectivity of esterification...

journal_title：Chemical & pharmaceutical bulletin

authors： Philippe M,Campos A,Sebag H,Rougier A,Dupuis D,Saint-Leger D,Vanlerberghe G

更新日期：1990-06-01 00:00:00

abstract：:We previously reported 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide 2 as on orally available monoacylglycerol acyltransferase 2 (MGAT2) inhibitor which exhibited an in vivo efficacy at an oral dose of 100 mg/kg in a mouse oral lipid tolerance test. Further optimizatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Busujima T,Tanaka H,Iwakiri K,Shirasaki Y,Munetomo E,Saito M,Masuko A,Kitano K,Io F,Kato K,Kamigaso S,Nozoe A,Sato N

更新日期：2016-01-01 00:00:00

abstract：:The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydr...

journal_title：Chemical & pharmaceutical bulletin

authors： Giammona G,Giannola LI,Carlisi B,Bajardi ML

更新日期：1989-08-01 00:00:00

abstract：:A novel method for thermodynamic stability studies of polymorphic drug substances has been developed. In order to estimate the transition temperature for an enantiotropic polymorphic pair, a formula for calculating the temperature at which the solubilities of each polymorph become equal has been derived with heat of s...

journal_title：Chemical & pharmaceutical bulletin

authors： Urakami K,Shono Y,Higashi A,Umemoto K,Godo M

更新日期：2002-02-01 00:00:00

abstract：:The purpose of this study was to predict the stability of meropenem in a mixed infusion. The hydrolysis of meropenem in aqueous solution was found to be accelerated by pH, and by increasing concentrations of sodium bisulfite (SBS) and L-cysteine. Equations were derived for the degradation rate constants (kobs) of pH, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takasu Y,Yoshida M,Tange M,Asahara K,Uchida T

更新日期：2015-01-01 00:00:00

abstract：:Targeted protein degradation by small molecules is an emerging modality with significant potential for drug discovery. We previously developed chimeric molecules, termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which induce the ubiquitylation and proteasomal de...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohoka N,Ujikawa O,Shimokawa K,Sameshima T,Shibata N,Hattori T,Nara H,Cho N,Naito M

更新日期：2019-03-01 00:00:00

abstract：:A rapid, sensitive, and specific analytical method for the determination of 1-hydroxyethylidene-1,1-diphosphonic acid (HEDP) on uncooked foods after treatment with a peracetic acid-based sanitizer (PAS) was developed. The method involves simple sample preparation steps and analysis using ion chromatography (IC) couple...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki I,Kubota H,Ohtsuki T,Tatebe C,Tada A,Yano T,Akiyama H,Sato K

更新日期：2016-01-01 00:00:00

abstract：:Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi S,Kojima T,Hashimoto K,Saito B,Sumi H,Ishikawa T,Ikeda Y

更新日期：2015-01-01 00:00:00

abstract：:The oxidative behaviour of, a hypnotic drug, zolpidem was studied at glassy carbon electrode in Britton-Robinson buffer over the pH range 2.0-11.0 using cyclic, linear sweep and differential pulse voltammetry. Oxidation of the drug was effected in a single irreversible, diffusion-controlled step. Using differential pu...

journal_title：Chemical & pharmaceutical bulletin

authors： Radi AE,Bekhiet G,Wahdan T

更新日期：2004-09-01 00:00:00

abstract：:Toxicarioside D (1), a new cardenolide, along with 10 other known ones, was isolated from the stem of Antiaris toxicaria LESCH. by bioassay-guided fractionation. Their structures were determined on the basis of spectroscopic analysis. All the reported compounds effectively inhibited the growth of various cancer cell l...

journal_title：Chemical & pharmaceutical bulletin

authors： Jiang MM,Dai Y,Gao H,Zhang X,Wang GH,He JY,Hu QY,Zeng JZ,Zhang XK,Yao XS

更新日期：2008-07-01 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：:Bioassay-directed fractionation of the extract of the cyanobacterium P. tenue led to the isolation of the three classes of glycolipids, viz., monogalactosyl diacylglycerol (MGDG), digalactosyl diacylglycerol (DGDG), and sulfoquinovosyl diacylglycerol (SQDG) as anti-tumor-promoters. In comparing the anti-tumor-promotin...

journal_title：Chemical & pharmaceutical bulletin

authors： Shirahashi H,Murakami N,Watanabe M,Nagatsu A,Sakakibara J,Tokuda H,Nishino H,Iwashima A

更新日期：1993-09-01 00:00:00

abstract：:Three new oleanane-type saponins, giganteosides L (1), M (2) and N (3) along with eight known ones were isolated from the roots of Cephalaria gigantea. Their structures were established as 3-O-[beta-D-galactopyranosyl-(1-->2)-beta-D-glucuronopyranosyl]-28-O-[beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl]-oleanol...

journal_title：Chemical & pharmaceutical bulletin

authors： Tabatadze N,Elias R,Faure R,Gerkens P,De Pauw-Gillet MC,Kemertelidze E,Chea A,Ollivier E

更新日期：2007-01-01 00:00:00

abstract：:From Puerariae Radix, the root of Pueraria lobata (Leguminosae), six new oleanene-type triterpene glycosides, called kudzusaponins A1 (1), A2 (2), Ar (3), SA4 (5), and SB1 (6) were isolated together with kudzusaponin A3 (7), soyasaponins SA3 (8), and I (9). The structures of 1-6 were determined to be 3-O-alpha-L-rhamn...

journal_title：Chemical & pharmaceutical bulletin

authors： Arao T,Kinjo J,Nohara T,Isobe R

更新日期：1997-02-01 00:00:00

abstract：:Polycomb repressive complex 2 (PRC2) is an attractive drug target for anti-cancer treatment. Among the three core subunits (EZH2, EED and SUZ12) of PRC2, EZH2 is the catalytic subunit that methylates histone H3 lysine 27 (H3K27), while EED is the regulatory subunit. Besides the small-molecule inhibitors of EZH2, those...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhu K,Du D,Yang R,Tao H,Zhang H

更新日期：2020-01-01 00:00:00