Studies on orally active cephalosporin esters. III. Effect of the 3-substituent on the chemical stability of pivaloyloxymethyl esters in phosphate buffer solution.

abstract：:A new lanostane-type triterpene, 29-hydroxypolyporenic acid C (8), was isolated from the dried sclerotia of Poria cocos together with eight other known compounds pachymic acid (1), dehydropachymic acid (2), 3-acetyloxy-16alpha-hydroxytrametenolic acid (3), polyporenic acid C (4), 3-epi-dehydropachymic acid (5), 3-epi-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou L,Zhang Y,Gapter LA,Ling H,Agarwal R,Ng KY

更新日期：2008-10-01 00:00:00

abstract：:A chemical investigation of Jaspis sp., the marine sponge collected from the South China Sea led to the isolation of six new isomalabaricane-type compounds, jaspolides A-F (1-6). The structures of those compounds were elucidated by extensive spectroscopic methods. The structure-types of 1 to 6 could be classified into...

journal_title：Chemical & pharmaceutical bulletin

authors： Tang S,Pei Y,Fu H,Deng Z,Li J,Proksch P,Lin W

更新日期：2006-01-01 00:00:00

abstract：:The structures of the ternary palladium(II) complexes of the formulations [Pd(Gly)(bpy)](+)Cl(-).4H(2)O (Gly=glycine; bpy=2,2'-bipyridine) (1), [Pd(Gly)(phen)](+)Cl(-).4H(2)O (2) (phen=1,10-phenanthroline) and {[Pd(Gly)(bpa)](+)Cl(-)}(2).6H(2)O (3) (bpa=2,2'-bipyridylamine) were determined. All complexes are positivel...

journal_title：Chemical & pharmaceutical bulletin

authors： Yodoshi M,Okabe N

更新日期：2008-07-01 00:00:00

abstract：:A new series of highly potent angiotensin-converting enzyme (ACE) inhibitors, 1-(N2-substituted L-lysyl-gamma-D-glutamyl)octahydro-1H-indole-2-carboxylic acids, was synthesized; various acyl groups were introduced at the alpha-amino group of the N-terminal P1 Lys. The effect of the N2-acyl groups on in vitro inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Sawayama T,Tsukamoto M,Sasagawa T,Nishimura K,Deguchi T,Takeyama K,Hosoki K

更新日期：1990-01-01 00:00:00

abstract：:A chemical investigation on a South China Sea gorgonian, Menella sp. resulted in the isolation and elucidation of menellin A (1), a highly oxygenated racemate with C(8) skeleton, and a polyhydroxylated steroid, menellsteroid C (2), along with eight known compounds (3-10). The structures of the new compounds were eluci...

journal_title：Chemical & pharmaceutical bulletin

authors： Chai XY,Sun JF,Tang LY,Yang XW,Li YQ,Huang H,Zhou XF,Yang B,Liu Y

更新日期：2010-10-01 00:00:00

abstract：:Microcrystalline cellulose (MCC) granules were prepared by wet granulation using a high-shear mixer. Physical characteristics of the granules were investigated using near IR spectrometry, thermogravimetry and isothermal water vapor adsorption. Near IR spectra of dried MCC granules prepared for various granulation time...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Kikuchi H,Yonemochi E,Terada K,Yamamoto K

更新日期：2001-04-01 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：:In the course of our chemotaxonomic study of the liverworts growing in Madagascar, mastigophoric acid methyl ester, along with eleven known compounds were isolated from Mastigophora diclados. Isolated metabolites showed that the Malagasy Mastigophora is more related to the samples from Borneo and Japan than to the Tai...

journal_title：Chemical & pharmaceutical bulletin

authors： Harinantenaina L,Asakawa Y

更新日期：2004-11-01 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：: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：: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：:A catalytic amount of tin(IV) chloride catalyzed formal [4+2] cycloaddition reaction of di-tert-butyl 2-ethoxycyclobutane-1,1-carboxylate with ketones or aldehydes to give diethyl 6-ethoxydihydro-2H-pyran-3,3(4H)-dicarboxylates, whereas two equivalents of trimethylsilyl triflate promoted tandem [4+2] cycloaddition and...

journal_title：Chemical & pharmaceutical bulletin

authors： Okado R,Nowaki A,Matsuo J,Ishibashi H

更新日期：2012-01-01 00:00:00

abstract：:Three dihydrobenzofuran derivatives 11, 19, 22, a Pummerer's ketone 20 and a dimeric phenylpropanoid 24 were synthesized by oxidative coupling reaction of methyl (E)-3-(4-hydroxy-2-methoxyphenyl)propenoate 10, which was prepared from umbelliferone. The major product 11 was converted into its acetate 21 and schizotenui...

journal_title：Chemical & pharmaceutical bulletin

authors： Maeda S,Masuda H,Tokoroyama T

更新日期：1994-12-01 00:00:00

abstract：:The permeability of nalmefene hydrochloride (NH) across different regions of ovine nasal mucosa was investigated in vitro. Five different regions of ovine nasal mucosa (superior turbinate mucosa, middle turbinate mucosa, inferior turbinate mucosa, posterior septum mucosa, and anterior septum mucosa) were studied. The ...

journal_title：Chemical & pharmaceutical bulletin

authors： Du G,Gao Y,Nie S,Pan W

更新日期：2006-12-01 00:00:00

abstract：:The structural conversion of the prion protein (PrP) from the normal cellular isoform (PrP(C)) to the posttranslationally modified form (PrP(Sc)) is thought to relate to Cu²⁺ binding to histidine (H) residues. Traditionally, the binding of metals to PrP has been investigated by monitoring the conformational conversion...

journal_title：Chemical & pharmaceutical bulletin

authors： Kojima A,Mabuchi Y,Konishi M,Okihara R,Nagano M,Akizawa T

更新日期：2011-01-01 00:00:00

abstract：:To improve the oral bioavailability of a dermorphin tetrapeptide analog, N(alpha)-1-iminoethyl-Tyr-D-MetO-Phe-MebetaAla-OH (III), which has a potent analgesic activity after oral administration, various derivatives were synthesized to increase lipophilicity by esterification of the C-terminal carboxyl group and/or acy...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawa T,Araki M,Miyamae T,Okayama T,Hagiwara M,Sakurada S,Morikawa T

更新日期：2003-07-01 00:00:00

abstract：:Many aminodihydroquinoline compounds have been studied to determine their cytotoxicity to cancer cells. However, anti-cancer stem cells (CSCs) activity of aminodihydroquinoline has not been tested in spite that CSC is believed to do an important roles in chemotherapy resistance and recurrence. The CSC selective target...

journal_title：Chemical & pharmaceutical bulletin

authors： Park H,Yu Y,Kim H,Lee E,Lee H,Jeon R,Kim WY

更新日期：2017-04-01 00:00:00

abstract：:To find novel PPAR ligands, we prepared several 3-{3 or 4-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}propanoic acid derivatives which were designed based on the structure of our previous PPARgamma ligand 1. In PPAR binding affinity assays, compound 4, which had an ethoxy group at the C-2 position of the propanoic acid o...

journal_title：Chemical & pharmaceutical bulletin

authors： Usui S,Fujieda H,Suzuki T,Yoshida N,Nakagawa H,Ogura M,Makishima M,Miyata N

更新日期：2007-07-01 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：:The synthetic route for a uterine relaxant, bis(2-[[(2S)-2-([(2R)-2-hydroxy-2-[4-hydroxy-3-(2-hydroxyethyl)-phenyl]ethyl]amino)-1,2,3,4-tetrahydronaphthalen-7-yl]oxy]-N,N-dimethylacetamide) sulfate (KUR-1246), was established by the coupling of optically active components, the bromohydrin 14 and the amine 24. We now d...

journal_title：Chemical & pharmaceutical bulletin

authors： Yanagi T,Kikuchi K,Takeuchi H,Ishikawa T,Nishimura T,Yamamoto I

更新日期：2001-08-01 00:00:00

abstract：:The enzyme tyrosinase regulates melanogenesis and skin hyperpigmentation by converting L-3,4-dihydroxyphenylalanine (L-DOPA) into dopaquinone, a key step in the melanin biosynthesis. The present work deals with design and synthesis of various oxindole-based chalcones as monophenolase and diphenolase activity inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Suthar SK,Bansal S,Narkhede N,Guleria M,Alex AT,Joseph A

更新日期：2017-01-01 00:00:00

abstract：:In the course of our search for bioactive metabolites from marine organisms, new hexylitaconic acid derivatives (1-4), along with (3S)-hexylitaconic acid (5), were isolated from a sponge-derived fungus Penicillium sp. Based on the NMR and MS data, the structures of compounds 1-4 were defined as α,β-dicarboxylic acid d...

journal_title：Chemical & pharmaceutical bulletin

authors： Li JL,Zhang P,Lee YM,Hong J,Yoo ES,Bae KS,Jung JH

更新日期：2011-01-01 00:00:00

abstract：:The differences in biological activities among polychlorinated dibenzo-p-dioxins (dioxins) are strongly dependent on the substitution pattern of chlorine at various positions on the parent dibenzo-p-dioxin molecule. The absolute hardness, eta, of dioxins shows a good correlation with the potency of biological activity...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi S,Sameshima K,Ishii Y,Tanaka A

更新日期：1995-10-01 00:00:00

abstract：:We have developed a new method to modify the C-4 position of 10-deacetylbaccatin III (5) using the C-4 acetoxy anion of the 13-keto derivative (7) and various alkyl halides. The method developed herein should be very useful for the preparation of C-4 modified taxoid analogs. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Uoto K,Takenoshita H,Ishiyama T,Terasawa H,Soga T

更新日期：1997-12-01 00:00:00

abstract：:It is well-known that baicalin-berberine complex (1) precipitates in the water decoction of numerous Chinese Medicinal formulae containing Radix Scutellariae and Rhizoma Coptidis or Cortex Phellodendri. In the current study, ionic interaction between the carboxylate ion of baicalin and the quaternary ammonium ion of b...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang JR,Tanaka T,Zhang H,Kouno I,Jiang ZH

更新日期：2012-01-01 00:00:00

abstract：:Three new cardiac glycosides named cheiranthoside VIII (1), cheiranthoside IX (2) and cheiranthoside X (3) were isolated from the seeds of Erysimum cheiranthoides. Based on spectroscopic data, the structures of 1-3 were characterized as strophanthidin 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-antiaropyranoside, cheiran...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei ZH,Nakayama H,Kuniyasu A,Tai BS,Nohara T

更新日期：2002-06-01 00:00:00

abstract：:Nuclear factor-κB (NF-κB) is an inducible transcription factor activated by a variety of cytokines, and promotes the transcription of genes involved in cancer, inflammation, autoimmune disease, and viral infection, among others. Because of its involvement in numerous disease processes, considerable research has focuse...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanemaru Y,Momiki Y,Matsuura S,Horikawa T,Gohda J,Inoue J,Okamoto Y,Fujita M,Otsuka M

更新日期：2011-01-01 00:00:00

abstract：:To find a novel acyl-CoA: cholesterol acyltransferase inhibitor, a series of sulfamide derivatives were synthesized and evaluated. Compound 1d, in which carboxymethyl moiety at the 5-position of Pactimibe was replaced by a sulfamoylamino group, showed 150-fold more potent anti-foam cell formation activity (IC(50): 0.0...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi K,Ohta M,Shoji Y,Kasai M,Kunishiro K,Miike T,Kanda M,Shirahase H

更新日期：2010-08-01 00:00:00

abstract：:The microbial transformation of five flavans (1-5) by endophytic fungi isolated from the tea plant Camellia sinensis was investigated. It was found that the endophytic filamentous fungus Diaporthe sp. oxidized stereoselectively at C-4 position of (+)-catechin (1) and (-)-epicatechin (2) to give the correspondent 3,4-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Agusta A,Maehara S,Ohashi K,Simanjuntak P,Shibuya H

更新日期：2005-12-01 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