Rupestines F-M, new guaipyridine sesquiterpene alkaloids from Artemisia rupestris.

abstract：:Stereoselective synthesis of the 16-membered diolide 27, a fully functionalized congener of lepranthin (1), is described. The requisite five asymmetric carbon centers in monomer 23 were constructed in a highly stereoselective manner by using different epoxide-opening reactions of α,β-unsaturated γ,δ-epoxy esters and e...

journal_title：Chemical & pharmaceutical bulletin

authors： Takada H,Nagumo S,Yasui E,Mizukami M,Miyashita M

更新日期：2011-01-01 00:00:00

abstract：:To reverse the adverse reactions of alkylxanthines and to develop novel inhibitors of cyclic AMP phosphodiesterase 4 (PDE4), a series of heterocycle [a]-, [b]-, [c,d]-, and [i]-condensed purines were designed and synthesized. Although all compounds did not display PDE1 and PDE3 inhibitory activities, several heterocyc...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki H,Yamamoto M,Shimura S,Miyamoto K,Yamamoto K,Sawanishi H

更新日期：2002-09-01 00:00:00

abstract：:The CHCl3 extract of the root of Angelica japonica showed high inhibitory activity against human gastric adenocarcinoma (MK-1) cell growth. From this extract, a new furanocoumarin named japoangelone and four furanocoumarin ethers of falcarindiol, named japoangelols A-D, were isolated together with caffeic acid methyl ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujioka T,Furumi K,Fujii H,Okabe H,Mihashi K,Nakano Y,Matsunaga H,Katano M,Mori M

更新日期：1999-01-01 00:00:00

abstract：:Seven halogenated derivatives of delta 9-tetrahydrocannabinol (delta 9-THC, 1) substituted on the aromatic ring at the 2 and/or 4 position, 2 (4)-fluoro- (2), 2,4-difluoro- (3), 2-chloro- (4), 2-bromo- (5), 2,4-dibromo- (6), 2-iodo- (7) and 2,4-diiodo-delta 9-THC (8) were synthesized and pharmacological effects such a...

journal_title：Chemical & pharmaceutical bulletin

authors： Usami N,Kobana K,Yoshida H,Kimura T,Watanabe K,Yoshimura H,Yamamoto I

更新日期：1998-09-01 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：:Biodegradable pasty-type copolyesters with a relatively low molecular weight of 4500 were synthesized by direct copolycondensation of epsilon-caprolactone (CL) and delta-valerolactone (VL) in the absence of catalysts to evaluate in vivo capabilities of the polymer for implantable controlled release devices in drug del...

journal_title：Chemical & pharmaceutical bulletin

authors： Imasaka K,Yoshida M,Fukuzaki H,Asano M,Kumakura M,Mashimo T,Yamanaka H,Nagai T

更新日期：1991-08-01 00:00:00

abstract：:Three new carotenoids with a 3-methoxy-5-keto-5,6-seco-4,6-cyclo-beta end group (1-3) have been isolated from the seeds of Pittosporum tobira. Their structures were elucidated by detailed analyses of nuclear magnetic resonance and UV data. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujiwara Y,Maruwaka H,Toki F,Hashimoto K,Maoka T

更新日期：2001-08-01 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：:The aim of this study was to search for a novel choline acetyltransferase (ChAT) activator from plants traditionally grown in Korea. An ethanol extract from Chaenomeles sinensis Koehne showed the highest ChAT-activating effect in vitro in an assay that used human neuroblastoma cells and [(14)C]acetyl-CoA. The active c...

journal_title：Chemical & pharmaceutical bulletin

authors： Kwon YK,Choi SJ,Kim CR,Kim JK,Kim HK,Choi JH,Song SW,Kim CJ,Park GG,Park CS,Shin DH

更新日期：2015-01-01 00:00:00

abstract：:To understand more fully the effect of polyunsaturated fatty acids (PUFAs) on lipid bilayers, we investigated the effects of treatment with fatty acids on the properties of a model membrane. Three kinds of liposomes comprising dipalmitoylphosphatidylcholine (DPPC), dioleylphosphatidylcholine (DOPC), and cholesterol (C...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Hagiwara C,Sugibayashi K,Takayama K

更新日期：2008-08-01 00:00:00

abstract：:Two new flavonoid glycosides, 5-hydroxy-7,8-dimethoxy (2R)-flavanone-5-O-beta-D-glucopyranoside (1) and 5-hydroxy-7,8,2',5'-tetramethoxy-flavone-5-O-beta-D-glucopyranoside (2), and a new diterpenoid, andrographic acid (3), along with andrographidine A (4) were isolated from Andrographis paniculata, and their structure...

journal_title：Chemical & pharmaceutical bulletin

authors： Li W,Xu X,Zhang H,Ma C,Fong H,van Breemen R,Fitzloff J

更新日期：2007-03-01 00:00:00

abstract：:A series of novel disulfides containing 1,3,4-thiadiazole moiety were designed, synthesized, and the structures of all products were identified by spectral data (IR, NMR, and high resolution (HR)-MS). Their in vitro antiproliferative activities were evaluated using 2-(2-methoxy-4-nitro-phenyl)-3-(4-nitro-phenyl)-5-(2,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang S,Liu XJ,Tang R,Wang HX,Liu HY,Liu YM,Chen BQ

更新日期：2017-01-01 00:00:00

abstract：:Two novel analogs of a biosynthetic precursor of lipid A (2) were synthesized. The one analog (3) has acyl groups identical to those of 2, and the other (4) has tetradecanoyl groups in place of the (R)-3-hydroxytetradecanoyl groups of 2. Both 3 and 4 possess an alpha-glycosidically-bound phosphonooxyethyl group in pla...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusama T,Soga T,Ono Y,Kumazawa E,Shioya E,Osada Y,Kusumoto S,Shiba T

更新日期：1991-08-01 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：: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

abstract：:In order to understand the relation between the electronic structure of neurotransmitters and the brain, a model of the brain based on absolute hardness (eta) and absolute electronegativity (chi) is described. It was found that the coordinate r(chi, eta) of electronic structures of neurotransmitters obtained using the...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi S,Terao Y

更新日期：2004-05-01 00:00:00

abstract：:The developmental change of uridine diphosphate-glucuronyltransferase (UDPGT) was studied using hepatic microsomes of rat fetuses on days 18 and 21 of gestation. Total phospholipid content was higher on day 21 than on day 18, although no significant difference in the composition between the two stages was observed. Li...

journal_title：Chemical & pharmaceutical bulletin

authors： Nanbo T

更新日期：1991-09-01 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：:We studied the possibility of using ursodeoxycholic acid (UDCA) as an excipient to create an amorphous composite that can be administered to animals in preclinical studies of experimental drugs. Three UDCA-based amorphous samples composed of nifedipine (NIF), indomethacin (IND), and naproxen (NAP) were found by screen...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanida S,Yoshimoto A,Yoshida M,Uchiyama H,Kadota K,Tozuka Y

更新日期：2019-01-01 00:00:00

abstract：:In an investigation of a new class of deoxyribonucleic acid (DNA)-intercalating antitumor agents, novel acridinyl-substituted uracils have been synthesized and evaluated for activity against L1210 leukemia in vivo, and against bacteria and fungus. These compounds were prepared by the novel enamine reaction between 9-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Kimura M,Okabayashi I,Kato A

更新日期：1989-03-01 00:00:00

abstract：:Fifteen triterpenoid saponins were isolated from the berries of Hedera colchica and their structures established on the basis of chemical and spectroscopic evidence. Among them, two are new compounds: coichiside A (3) and colchiside B (15) and four are described for the first time in the berries of Hedera colchica (co...

journal_title：Chemical & pharmaceutical bulletin

authors： Mshvildadze V,Elias R,Faure R,Debrauwer L,Dekanosidze G,Kemertelidze E,Balansard G

更新日期：2001-06-01 00:00:00

abstract：:Racemic 1-acetoxy-2-phenylpropane (12) and 1-acetoxy-2-(2-naphthyl)propane (33) were hydrolyzed with lipase at 35-36 degrees C for 2 and 24 h to give predominantly (S)-2-phenyl-1-propanol (11) and (S)-2-(2-naphthyl)-1-propanol (32), respectively. However, racemic 1-acetoxy-2-(1-naphthyl)propane (25) was recovered inta...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto T,Takeda Y,Iwata E,Sakamoto M,Ishida T

更新日期：1994-06-01 00:00:00

abstract：:We have improved sample pre-treatment for the effective removal of polyphenols and simple analysis of caffeine in tea using a cartridge filled with polyvinylpolypyrroridone (PVPP). Nearly 100% of catechins were removed from the green tea sample and caffeine was completely recovered in the range of 98.2-101.3% by sampl...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamauchi Y,Nakamura A,Kitai M,Hatanaka K,Kohno I,Tanimoto T

更新日期：2007-09-01 00:00:00

abstract：:Six new oleanane-type triterpene saponins, called reiniosides A-F, were isolated from the roots of Polygala reinii Fr. et Sav. and their structures were elucidated by spectroscopic and chemical means. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyase T,Saitoh H,Shiokawa K,Ueno A

更新日期：1995-03-01 00:00:00

abstract：:The 1-BuOH-soluble fraction of the methanol (MeOH) extract of Diospyros maritima was separated by chromatographic techniques to give three new oleanane-type and one new ursane-type triterpene glucoside, named ebenamariosides A-D (1-4); two megastigmanes were also isolated. The structures of triterpene glucosides was e...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawakami S,Miura E,Nobe A,Inagaki M,Nishimura M,Matsunami K,Otsuka H,Aramoto M

更新日期：2019-01-01 00:00:00

abstract：:We designed and synthesized a new class of peptidomimetic human immunodeficiency virus protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl isostere as the active moiety. From a structure-activity relatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimoto T,Hattori N,Takaku H,Kisanuki S,Fukazawa T,Terashima K,Kato R,Nojima S,Misawa S,Ueno T,Imai J,Enomoto H,Tanaka S,Sakikawa H,Shintani M,Hayashi H,Kiso Y

更新日期：2000-09-01 00:00:00

abstract：:Chemical investigation of the seeds of Adonis aestivalis has led to the isolation of a new cardenolide (3β,5α,14β,17β-tetrahydroxycard-20,22-enolide) (1), two new glycosides (2, 3) of 1, and a new strophanthidin hexaglycoside (4), together with a known compound, strophanthidin 3-O-β-D-glucopyranoside (5). The structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubo S,Kuroda M,Matsuo Y,Masatani D,Sakagami H,Mimaki Y

更新日期：2012-01-01 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：:In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have...

journal_title：Chemical & pharmaceutical bulletin

authors： Yi W,Cao R,Chen Z,Yu L,Wen H,Yan Q,Ma L,Song H

更新日期：2010-05-01 00:00:00

abstract：:The binding of carprofen (CP) to human serum albumin (HSA) and bovine serum albumin (BSA) was compared using equilibrium dialysis method. The affinity of CP for the primary binding site was BSA > HSA. However, the number of primary binding sites (n1) was 1.94 on HSA, considerably greater than that on BSA (0.79). The d...

journal_title：Chemical & pharmaceutical bulletin

authors： Kohita H,Matsushita Y,Moriguchi I

更新日期：1994-04-01 00:00:00