Syntheses of cerulenin and its analogs. II. Synthesis and biological activity of dl-carbacerulenin, a carbocyclic analog of cerulenin.

abstract：:The mechanism of the deprotonation of 2-butanone (1) with methoxide anion (2) was studied by ab initio molecular orbital (MO) methods. Calculations of the thermodynamic stabilities of each complex and the regioselectivity of the reaction were performed using a static isodensity surface polarized continuum model (IPCM)...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda H,Yukawa M,Niiya T

更新日期：2006-05-01 00:00:00

abstract：:We synthesize optically active (R)-terbutaline 2, which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of...

journal_title：Chemical & pharmaceutical bulletin

authors： Uchimoto H,Ikeda M,Tanida S,Ohhashi K,Chihara Y,Shigeta T,Arimitsu K,Yamashita M,Nishide K,Kawasaki I

更新日期：2017-01-01 00:00:00

abstract：:Detailed chemical studies on the cytotoxic fraction from the leaves of Dysoxylum cumingianum have resulted in the isolation of two new triterpene glucosides, cumingianosides P (18) and Q (19), with an apotirucallane-type skeleton. The structures of 18 and 19 were determined by spectral examinations, and by conversion ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujioka T,Sakurai A,Mihashi K,Kashiwada Y,Chen IS,Lee KH

更新日期：1997-01-01 00:00:00

abstract：:Three new limonoids, cipadesins D--F (1--3), together with 8,15-dihydroxy-13E-labdane, beta-sitosterol and beta-daucosterol, were isolated from the leaves and bark of Cipadessa cinerascens. Their structures were elucidated by spectral evidence. X-Ray crystallographic analysis confirmed the structure of 1. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yuan XH,Li BG,Xu CX,Zhou M,Qi HY,Zhang GL

更新日期：2007-06-01 00:00:00

abstract：:The purpose of this study was to elucidate the effect of high-temperature storage on the stability of ranitidine, specifically with respect to the potential formation of N-nitrosodimethylamine (NDMA), which is classified as a probable human carcinogen. Commercially available ranitidine reagent powders and formulations...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe Y,Yamamoto E,Yoshida H,Usui A,Tomita N,Kanno H,Masada S,Yokoo H,Tsuji G,Uchiyama N,Hakamatsuka T,Demizu Y,Izutsu KI,Goda Y,Okuda H

更新日期：2020-10-01 00:00:00

abstract：:A method was developed for semi-preparative scale enantioseparation of racemic homochlorcyclizine (HCZ) by high performance liquid chromatography (HPLC) on Chiralcel OD column. The best resolution was achieved using an eluent composed of n-hexane plus 0.2 M isopropylamine. By this method, about 5.0 mg of racemic HCZ c...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishikata M,Nakai A,Fushida H,Miyake K,Arita T,Kitagawa S,Kunitomo M,Iseki K,Miyazaki K

更新日期：1992-05-01 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 competitive inclusion complexations in the ternary phenacetin/competitors/beta-cyclodextrin (beta-CyD) systems were investigated by the solubility method, where m-bromobenzoic acid (m-BBA) and o-toluic acid (o-TA) were used as competitors. The solubility changes of the drug and competitors as a function of beta-Cy...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono N,Hirayama F,Arima H,Uekama K

更新日期：2001-01-01 00:00:00

abstract：:Novel nucleoside analogues of structure 3-5 were synthesized starting from (+/-)-cis-2-amino-3-cyclopentenylmethanol (1). The chlorine derivative 3 inhibited both HIV-1 and HIV-2 replication in MT-4 cells with IC(50) values of 10.67 microM and of 13.79 microM, respectively. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Canoa P,González-Moa MJ,Teijeira M,Terán C,Uriarte E,Pannecouque C,De Clercq E

更新日期：2006-10-01 00:00:00

abstract：:A new antibiotic indole trimer named trisindoline (1) was isolated, together with a known dioxopiperazine brevianamide F (2), from the culture of a bacterium of Vibrio sp., which was separated from the Okinawan marine sponge Hyrtios altum. The structure of trisindoline (1) has been determined on the bases of physicoch...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi M,Aoki S,Gato K,Matsunami K,Kurosu M,Kitagawa I

更新日期：1994-12-01 00:00:00

abstract：:Two new clerodane-type diterpenoids trivially named as ballotenic acid (1) and ballodiolic acid (2) have been isolated from Ballota limbata along with three the known compounds; beta-amyrin, oleanolic acid, and beta-sitosterol. The structure elucidation of the new compounds was based primarily on two-dimensional (2D)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Ahmad VU,Farooq U,Hussain J,Ullah F,Nawaz SA,Choudhary MI

更新日期：2004-04-01 00:00:00

abstract：:Tryptanthrin is an ancient medicine which recently was also found to have a function of downregulating multidrug resistance (MDR). However, tryptanthrin is insoluble in water, which limits its availability for delivery into cancer cells. There is a need to improve delivery systems to increase the inhibition of MDR. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Fang YP,Lin YK,Su YH,Fang JY

更新日期：2011-01-01 00:00:00

abstract：:The crystal of bovine trypsin complexed with a potent inhibitor, 4-[4-(N,N- dimethylcarbamoylmethoxycarbonylmethyl)phenoxycarbonylphenyl ]guanidinium (FOY-305) in the novel orthorhombic from with a low molecular packing density was studied by the X-ray diffraction method. Using synchrotron radiation, the intensity dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto O,Taga T,Matsushima M,Higashi T,Machida K

更新日期：1990-08-01 00:00:00

abstract：:Two new lignans, pseuderesinol (1), pseuderanoside (2) and a new triterpene, pseuderanic acid (3) were isolated from the dried root of Pseuderanthemum carruthersii (SEEM.) GUILL. var. atropurpureum (BULL.) FOSB. (Acanthaceae), together with ten known compounds, including five lignans, (+)-eudesmin (4), (+)-magnolin (5...

journal_title：Chemical & pharmaceutical bulletin

authors： Vo TN,Nguyen PL,Tuong LT,Pratt LM,Vo PN,Nguyen KP,Nguyen NS

更新日期：2012-01-01 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：:Adipocyte fatty acid binding protein (A-FABP; FABP4), which is predominantly expressed in macrophages and adipose tissue, regulates fatty acid storage and lipolysis, and is also an important mediator of inflammation. Here, we report a synthesis of (14)C-labeled 2-[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yl...

journal_title：Chemical & pharmaceutical bulletin

authors： Okada T,Hiromura M,Otsuka M,Enomoto S,Miyachi H

更新日期：2012-01-01 00:00:00

abstract：:A moisturizing cream mixed with a steroid ointment is frequently prescribed to patients suffering from atopic dermatitis. However, there is a concern that the mixing operation causes destabilization. The present study was performed to investigate the stability of such preparations closely using magnetic resonance imag...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Funatani C,Yamamoto Y,Fukami T,Koide T,Hayashi Y,Takayama K

更新日期：2017-01-01 00:00:00

abstract：:The fluorometric thiobarbituric acid (TBA) assay of blood plasma was performed under various conditions in order to assess whether the assay reflects lipid peroxidation. The TBA-reactivity of malonaldehyde was not dependent on the pH values of the reaction and was little affected by tert-butyl hydroperoxide (tert-BuOO...

journal_title：Chemical & pharmaceutical bulletin

authors： Kojima T,Kikugawa K,Kosugi H

更新日期：1990-12-01 00:00:00

abstract：:The combination of electrolysis and the Fe(III)(PA)3/O2/CH3CN system was investigated for allylic hydroxylation of octahydronaphthalene derivatives. Substrates with a bridgehead double bond gave the allylic alcohol with alpha-preference, while non-bridgehead olefin did not react smoothly. This system is a useful tool ...

journal_title：Chemical & pharmaceutical bulletin

authors： Okamoto I,Funaki W,Nobuchika S,Sawamura M,Kotani E,Takeya T

更新日期：2005-02-01 00:00:00

abstract：:Atranorin, lichexanthone, and the (+)-usnic, diffractaic, divaricatic, perlatolic, psoromic, protocetraric, and norstictic acids isolated from the lichens Parmotrema dilatatum (VAIN.) HALE, Usnea subcavata MOTYKA, Usnea sp., Ramalina sp., Cladina confusa (SANT.) FOLMM. & AHTI, Dirinaria aspera HÄSÄNEN, and Parmotrema ...

journal_title：Chemical & pharmaceutical bulletin

authors： Brandão LF,Alcantara GB,Matos Mde F,Bogo D,Freitas Ddos S,Oyama NM,Honda NK

更新日期：2013-01-01 00:00:00

abstract：:The purpose of this study was to determine which foods and/or drinks are capable of reducing the bitterness of topiramate when consumed together with the medicine. The inhibitory effects of foods/drinks (yoghurt and nine other foods/drinks) on the bitterness of topiramate (5 mg/mL) were evaluated with a taste sensor u...

journal_title：Chemical & pharmaceutical bulletin

authors： Haraguchi T,Uchida T,Hazekawa M,Yoshida M,Nakashima M,Sanda H,Hase T,Tomoda Y

更新日期：2016-01-01 00:00:00

abstract：:N-(2-Dimethylaminoethyl)carboxamide (1a-d), 2-dimethylaminoethyl alkyl ether (2a, b), and 2-dimethylaminoethyl 2-hydroxy-2-phenethyl ether (3a-c) and its amino and methylene analogues (3d, 4) have been screened for antiamnestic and antihypoxic activities in mice. A clear reversing effect on electroconvulsive shock-ind...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono S,Yamafuji T,Chaki H,Todo Y,Maekawa M,Kitamura K,Tai M,Narita H

更新日期：1995-09-01 00:00:00

abstract：:Hot aqueous extracts of 134 Chinese crude drugs were subjected to screening for inhibitory activity on K+ contracture of guinea pig taenia coli, and significant activity was observed in 17 crude drugs. Chemical investigations of two crude drugs, Kakko and Ubai, which originate from Pogostemon cablin and Prunus mume, r...

journal_title：Chemical & pharmaceutical bulletin

authors： Ichikawa K,Kinoshita T,Sankawa U

更新日期：1989-02-01 00:00:00

abstract：:Three new spirostanol glycosides (1-3) and a new furostanol glycoside (4), together with two known spirostanol glycosides (5 and 6) were isolated from the whole plants of Agave utahensis (Agavaceae). The structures of the new compounds were determined by spectroscopic analysis and the results of hydrolytic cleavage. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokosuka A,Mimaki Y

更新日期：2007-01-01 00:00:00

abstract：:Several microorganisms showed the ability to transform the harman alkaloids, harmaline (1), harmalol (2) and harman (5). Harmaline (1) and harmalol (2) were converted by Rhodotorula rubra ATCC 20129 into the tryptamines, 2-acetyl-3-(2-acetamidoethyl)-7-methoxyindole (3) and 2-acetyl-3-(2-acetamidoethyl)-7-hydroxyindol...

journal_title：Chemical & pharmaceutical bulletin

authors： Herath W,Mikell JR,Ferreira D,Khan IA

更新日期：2003-06-01 00:00:00

abstract：:In order to synthesize four stereoisomers of cystathionine (CYT), D- and L-homocysteines (D- and L-Hcy) were synthesized from methionine (Met) by a facile procedure. L-Met was reacted with dichloroacetic acid in concentrated hydrochloric acid under reflux to give (4S)-1,3-thiazane-2,4-dicarboxylic acid hydrochloride [...

journal_title：Chemical & pharmaceutical bulletin

authors： Shiraiwa T,Nakagawa K,Kanemoto N,Kinda T,Yamamoto H

更新日期：2002-08-01 00:00:00

abstract：:We have engineered a novel, non-viral, multifunctional gene vector (STR-CH(2)R(4)H(2)C) that contained stearoyl (STR) and a block peptide consisting of Cys (C), His (H), and Arg (R). STR-CH(2)R(4)H(2)C can form a stable nano-complex with plasmid DNA (pDNA) based on electronic interactions and disulfide cross linkages....

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Kanazawa T,Ogawa T,Suda Y,Takashima Y,Fukuda T,Okada H

更新日期：2011-01-01 00:00:00

abstract：:A new flavonol triglycoside, isorhamnetin 3-O-beta-D-xylopyranosyl-(1"-->3)-alpha-L-rhamnopyranosyl-(1'''-->6")-beta-D-galactopyranoside, has been isolated from the leaves of Hammada scoparia together with two known compounds, isorhamnetin 3-O-beta-D-apiofuranosyl-(1'''-->2")[alpha-L-rhamnopyranosyl-(1"-->6")]-beta-D-...

journal_title：Chemical & pharmaceutical bulletin

authors： Ben Salah H,Jarraya R,Martin MT,Veitch NC,Grayer RJ,Simmonds MS,Damak M

更新日期：2002-09-01 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：:Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether. (3). The hypotensive and beta-blocking activities of 1 and its optical isomers were examined when given intravenou...

journal_title：Chemical & pharmaceutical bulletin

authors： Seki T,Kanada A,Nakao T,Shiraiwa M,Asano H,Miyazawa K,Ishimori T,Minami N,Shibata K,Yasuda K

更新日期：1998-01-01 00:00:00