Amino acid derivatives with anticonvulsant activity.

abstract：:A practical protocol to obtain accurate heat capacity values of pharmaceutical compounds using modulated-temperature differential scanning calorimetry was established. Three pharmaceutical compounds, acetaminophen, indomethacin, and tri-O-methyl-β-cyclodextrin were used as model compounds. Powder samples did not produ...

journal_title：Chemical & pharmaceutical bulletin

authors： Harada T,Kawakami K,Yoshihashi Y,Yonemochi E,Terada K,Moriyama H

更新日期：2013-01-01 00:00:00

abstract：:Benzoxazinorifamycin reacted with various secondary amines to yield various 5'-substituted aminobenzoxazinorifamycin derivatives. The derivatives exhibited potent activities against gram-positive bacteria and mycobacteria. The antimicrobial activities of these compounds against Mycobacterium tuberculosis and Mycobacte...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamane T,Hashizume T,Yamashita K,Hosoe K,Hidaka T,Watanabe K,Kawaharada H,Kudoh S

更新日期：1992-10-01 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

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：: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：:As part of our search for active agents against systemic fungal infections, a new series of triazole compounds with a thiolane ring was synthesized. Their antifungal activities were investigated in vitro and in vivo. Some of these thiolanetriazoles showed promising activity, comparable to that of ketoconazole, against...

journal_title：Chemical & pharmaceutical bulletin

authors： Konosu T,Takeda N,Tajima Y,Yasuda H,Oida S

更新日期：1990-05-01 00:00:00

abstract：:Novel 4,5,6,7-tetrahydrothieno[3,2-c]pyridines, 1-thienyl-1,2,3,4-tetrahydroisoquinolines and related compounds, in which the benzene rings of (+)-1 (FR115427) were replaced with heteroaromatic rings such as thiophene, furan, benzothiophene and indole, were synthesized and evaluated for anticonvulsant activity against...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohkubo M,Kuno A,Katsuta K,Ueda Y,Shirakawa K,Nakanishi H,Kinoshita T,Takasugi H

更新日期：1996-04-01 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：:An antibiotic formycin A inhibited growth of Vibrio parahaemolyticus under certain conditions, which suggested that formycin A was taken up by cells under these conditions. We found that formycin A was transported via the adenosine transport system which we previously reported as a Na(+)-coupled cotransport system. We...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Tomita Y,Mitani Y,Tsuda M,Tsuchiya T

更新日期：1991-05-01 00:00:00

abstract：:A new oleanan-type triterpene and three new cincholic acid glycosides were isolated from Peruvian "Una de Gato" (Cat's claw, plant of origin: Uncaria tomentosa), a traditional herbal medicine in Peru. Their structures were determined by spectroscopic analysis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima M,Hashimoto K,Sandoval M,Aimi N,Takayama H

更新日期：2004-10-01 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：:A new gluco indole alkaloid, 3,4-dehydro-5-carboxystrictosidine, was obtained from Peruvian Uña de Gato (Cat's Claw, original plant: Uncaria tomentosa) together with two known gluco indole alkaloids. This compound was the first example of isolation of a gluco monoterpenoid indole alkaloid having a 3,4-dihydro-beta-car...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima M,Hashimoto K,Yokoya M,Takayama H,Aimi N,Sakai SI

更新日期：2000-10-01 00:00:00

abstract：:Eight new myriocin analogs, 2-epi-myriocin, Z-14-deoxomyriocin, and nor-deoxomyriocins, and a known myriocin derivative, 14-deoxomyriocin, were synthesized from 2-deoxy-D-glucose via common intermediates in previous myriocin and Z-myriocin syntheses. The immunosuppressive activities of new myriocin analogs and Z-myrio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Yokokawa Y,Okuno Y,Yagi N,Murakami N

更新日期：1994-12-01 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：:Two series of new pyridines bearing thiazoline (3a--n) and thiazolidinone (5a--e) moieties were prepared via the cyclization of the corresponding substituted pyridyl thiourea (2a--g) with an appropriately substituted phenacyl bromide or chloroacetic acid, respectively. The antimicrobial activity was determined for rep...

journal_title：Chemical & pharmaceutical bulletin

authors： Hassan HY,el-Koussi NA,Farghaly ZS

更新日期：1998-05-01 00:00:00

abstract：:A highly sensitive high-performance liquid chromatography with fluorescence detection for the determination of arachidonic acid metabolites is described. The metabolites are converted into corresponding fluorescent derivatives by reaction with 3-bromomethyl-6,7-methylenedioxy-1-methyl-2(1H)-quinoxalinone in the presen...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Takehiro O,Ishida J,Nakamura M

更新日期：1989-10-01 00:00:00

abstract：:A series of N-(trifluoromethyl-2-pyridinyl)alkane- and arenesulfonamides 2-5 have been synthesized by the substitution reaction of 2-chloro(trifluoromethyl)pyridines 6 with alkane- and arenesulfonamides 7. Their inhibitory activities against secretory phospholipase A₂ of porcine pancreas were examined and the analog N...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakayama H,Morita Y,Kimura H,Ishihara K,Akiba S,Uenishi J

更新日期：2011-01-01 00:00:00

abstract：:The purpose of this study was to mask the intensely bitter taste of metoclopramide HCl and to formulate a rapid disintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing metoclopramide HCl with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratio by the extrusion-precipi...

journal_title：Chemical & pharmaceutical bulletin

authors： Randale SA,Dabhi CS,Tekade AR,Belgamwar VS,Gattani SG,Surana SJ

更新日期：2010-04-01 00:00:00

abstract：:2,3-Epoxy-4-hydroxy-4-((E,E)-3,6-octadienyl)cyclopentanone (dl-carbacerulenin 5) was synthesized via the epoxyketones 15a and 15b as a mimic of the active form of the antibiotics cerulenin 1, a potent inhibitor of fatty acid synthetase (FAS). The monobenzyl ethers (12 and 13), synthetic intermediates of 15, were prepa...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimazawa R,Ogawa Y,Morisaki N,Funabashi H,Kawaguchi A,Iwasaki S

更新日期：1992-11-01 00:00:00

abstract：:Cigarette smoke, a collection of many toxic chemicals, contributes to the pathogenesis of smoking-related diseases such as chronic obstructive pulmonary disease and cancer. Much work has been done on the chemical analysis of ingredients in cigarette smoke, but there are few reports on the active ingredients that can m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi Y,Horiyama S,Honda C,Suwa K,Nakamura K,Kunitomo M,Shimma S,Toyoda M,Sato H,Shizuma M,Takayama M

更新日期：2013-01-01 00:00:00

abstract：:Debenzylating enzyme from Aspergillus niger enzyme (commercial crude cellulase) catalyzes the hydrolysis of cetraxate benzyl ester hydrochloride (2), a precursor of the antiulcer agent (1). The enzyme was highly purified by three kinds of chromatographies (hydrophobic, ion exchange, gel filtration) with a recovery of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroda H,Miyadera A,Imura A,Suzuki A

更新日期：1989-11-01 00:00:00

abstract：:Fourier transform infrared/attenuated total reflection (FT-IR/ATR) spectroscopy was used to examine the effect of fatty acids, fatty amines and propylene glycol (PG) on the molecular mobility of rat stratum corneum lipids and keratinized proteins, using a hydrophobic solute, indomethacin, and a polar solute, 5- and 6-...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi Y,Yasukawa H,Yamaoka Y,Kato Y,Morimoto Y,Fukumori Y,Fukuda T

更新日期：1992-07-01 00:00:00

abstract：:The pharmacological activity of four new progesterone derivatives: 4-bromo-17alpha-(p-fluorobenzoyloxy)-4-pregnene-3,20-dione (7), 4-bromo-17alpha-(p-bromobenzoyloxy)-4-pregnene-3,20-dione (8), 4-bromo-17alpha-(p-chlorobenzoyloxy)-pregnene-3,20-dione (9) and 4-bromo-17alpha-(p-toluoyloxy)-4-pregnene-3,20-dione (10) wa...

journal_title：Chemical & pharmaceutical bulletin

authors： Cabeza M,Heuze I,Bratoeff E,Murillo E,Ramirez E,Lira A

更新日期：2001-09-01 00:00:00

abstract：:We found that diarylmethanols and diaryl ketones were smoothly reduced to the corresponding diarylalkanes using supercritical 2-propanol in good yields. Furthermore, we determined the specific reaction of fluorene using supercritical methanol at high temperature. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hatano B,Kubo D,Tagaya H

更新日期：2006-09-01 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：:A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PA...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki H,Ogiku T,Sai H,Moritani Y,Ohtani A,Ohmizu H

更新日期：2009-09-01 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：:Starting from benzo- or thienocycloalkaneacetic acids, we have prepared a series of 1-(3-p-fluorobenzoylpropyl)-4-(1-oxo-benzo- or thienocycloalkyl-2-ethyl)piperazines 8a-e containing both semirigid and linear butyrophenones pharmacophores. The affinities of these compounds for dopamine (D2) and 5-hydroxytryptamine (5...

journal_title：Chemical & pharmaceutical bulletin

authors： Raviña E,Fueyo J,Masaguer CF,Negreira J,Cid J,Loza I,Honrubia A,Tristán H,G-Ferreiro T,Fontenla JA,Rosa E,Calleja JM,De Ceballos ML

更新日期：1996-03-01 00:00:00

abstract：:A series of phthalazine and 1,2,3-benzotriazine derivatives which have heterocyclylpiperidino groups was synthesized and tested for cardiotonic activity in anesthetized dogs. Several 6,7-dimethoxyphthalazine derivatives showed relatively potent cardiotonic activity comparable to that of amrinone. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomoto Y,Obase H,Takai H,Teranishi M,Nakamura J,Kubo K

更新日期：1990-08-01 00:00:00

abstract：:A series of joro spider toxins, novel polyamines sharing a common moiety of 2,4-dihydroxyphenylacetyl cadaverine, have been identified using various bioassays, such as inhibition of a glutamatergic transmission and insecticidal activity. In this paper, we tried to chemically find still unknown polyamine toxins in the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiba T,Akizawa T,Matsukawa M,Pan-Hou H,Yoshioka M

更新日期：1994-09-01 00:00:00