Tandem enzymatic resolution yielding L-alpha-aminoalkanedioic acid omega-esters.

abstract：:A series of aminomethylenebisphosphonate derivatives was synthesized and evaluated for their antiresorptive activities using a parathyroid hormone (PTH)-induced hypercalcemia model in rats (PIH model). Among these compounds, (cycloheptylamino)methylenebis(phosphonic acid) (3j) was finally selected for further investig...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi M,Sakamoto S,Yoshida M,Abe T,Isomura Y

更新日期：1993-04-01 00:00:00

abstract：:The purpose of this study was to develop and test a novel and simple method for evaluating the disintegration time of rapidly disintegrating tablets (RDTs) in vitro, since the conventional disintegration test described in the pharmacopoeia produces poor results due to the difference of its environmental conditions fro...

journal_title：Chemical & pharmaceutical bulletin

authors： Hoashi Y,Tozuka Y,Takeuchi H

更新日期：2013-01-01 00:00:00

abstract：:(+)-4(5)-[(2R,5R)-5-aminomethyltetrahydrofuran-2-yl]imidazole [(+)-1, imifuramine] and its 2R,5S-stereoisomer (+)-2 were expected as base compounds to develop selective human histamine H4-receptor ligands. The improved synthesis of (+)-1 was done via cyclization of a diazafulvene intermediate generated by Bu3P/N,N,N',...

journal_title：Chemical & pharmaceutical bulletin

authors： Harusawa S,Araki L,Terashima H,Kawamura M,Takashima S,Sakamoto Y,Hashimoto T,Yamamoto Y,Yamatodani A,Kurihara T

更新日期：2003-07-01 00:00:00

abstract：:The relationship between the product patterns and the configurations of 1,2-cycloheptane- and 1,2-cyclooctanediols 9 in the cyclocondensations with oxalyl chloride in the presence of triethylamine at 0 degrees C has been shown analogous to that obtained for 1,2-disubstituted acyclic ethylene glycols 1: cis-1,2-cyclooc...

journal_title：Chemical & pharmaceutical bulletin

authors： Itaya T,Iida T,Natsutani I,Ohba M

更新日期：2002-01-01 00:00:00

abstract：:The analysis of genotoxic impurities (GTIs) in active pharmaceutical ingredients (APIs) is a challenging task. The target detection limit (DL) in an API is typically around 1 ppm (1 µg/g API). Therefore, a sensitive and selective analytical method is required for their analysis. 4-Chloro-1-butanol, an alkylating agent...

journal_title：Chemical & pharmaceutical bulletin

authors： Harigaya K,Yamada H,Yaku K,Nishi H,Haginaka J

更新日期：2014-01-01 00:00:00

abstract：:Solid dispersions were prepared by the evaporation of ethanol after dissolving into ethanol a water soluble medicine (oxprenolol hydrochloride (OXP)), four grades of water insoluble ethylcellulose (EC) and four grades of water soluble hydroxypropyl cellulose (HPC), both having different molecular weights. The precise ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yuasa H,Ozeki T,Kanaya Y,Oishi K

更新日期：1993-05-01 00:00:00

abstract：:As part of the search for new topical antiinflammatory agents, various 21-substituted corticosteroids having sulfur-containing moieties were prepared and tested for vasoconstrictive activity in humans. A structure-activity relationship study revealed that substitution of the 21-hydroxy group with a lower alkyl-thio gr...

journal_title：Chemical & pharmaceutical bulletin

authors： Mitsukuchi M,Ikemoto T,Taguchi M,Higuchi S,Abe S,Yasui H,Hatayama K,Sota K

更新日期：1989-07-01 00:00:00

abstract：:A series of 43 stilbene derivatives that showed cytotoxicity against human lung carcinoma (A549) was analyzed using comparative molecular field analysis (CoMFA) for defining the hypothetic pharmacophore model. The polyoxylated stilbenes were found to be active inhibitors of tubulin polymerization. Several cis-stilbene...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim S,Min SY,Lee SK,Cho WJ

更新日期：2003-05-01 00:00:00

abstract：:The absorption of insulin (from porcine pancreas) from the rectum of rabbits after the administration of hollow-type suppositories containing insulin and five kinds of cyclodextrins (CyDs) was investigated. Three types of suppositories were employed: suppository I containing insulin (approximately 26 IU/mg) and variou...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe Y,Matsumoto Y,Seki M,Takase M,Matsumoto M

更新日期：1992-11-01 00:00:00

abstract：:The metabolism of 2,4-dinitrotoluene (2,4-DNT), 2,4-dinitrobenzyl alcohol (2,4-DNB), 2,4-dinitrobenzaldehyde (2,4-DNBAl), 2,6-DNT, 2,6-DNB and 2,6-DNBAl in the microsomal and cytosol fractions prepared from unfortified male Wistar and male Sprague-Dawley (S.D.) rat livers was investigated. Data obtained by high-perfor...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori M,Kawajiri T,Sayama M,Miyahara T,Kozuka H

更新日期：1989-07-01 00:00:00

abstract：:From the Fresh leaves of Hovenia dulcis Thunb. var. tomentella Makino, five five new dammarane glycosides named hodulosides VI-X (1-5) were isolated. Their structures were determined on the basis of chemical and spectral evidence. Hodulosides VII-X showed antisweet activities. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa K,Nagai Y,Yoshida M,Arihara S

更新日期：1993-10-01 00:00:00

abstract：:Enantiomerically pure (1S,3S)- and (1S,3R)-1-amino-3-(hydroxymethyl)cyclopentanes have been efficiently synthesized from L-aspartic acid. The title compounds are isosteres of ribose and may be used to construct nucleoside analogs with important antiviral and antineoplastic activities as demonstrated by a concise total...

journal_title：Chemical & pharmaceutical bulletin

authors： Rapoport H,Chen Y,Mohareb RM,Ahn JH,Sim TB,Ho JZ

更新日期：2003-10-01 00:00:00

abstract：:We have developed a catalytic aerobic oxidative dimerization reaction of benzofuranones using a Pd(II)-µ-hydroxo complex. Radical-radical cross-coupling of the resulting dimers with azo compounds enabled the one-pot synthesis of structurally congested benzofuranones having two distinct vicinal all-carbon quaternary ce...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohnishi R,Sugawara M,Ezawa T,Sohtome Y,Sodeoka M

更新日期：2020-01-01 00:00:00

abstract：:The intercalation reaction of diclofenac sodium (DFS) with layered inorganic compounds, gamma-titanium phosphate (gamma-TiP), proton type titanium oxide (H-TiO2) and sodium type synthetic mica (Na-TSM), was examined on. The direct reaction of DFS in ethanol-water mixed solvent resulted in the large amount accommodatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Tajima T,Suzuki N,Watanabe Y,Kanzaki Y

更新日期：2005-11-01 00:00:00

abstract：:A high-performance liquid chromatographic method and a UV derivative spectrophotometric method for the determination of famciclovir, a highly active antiviral agent, in tablets were developed in the present work. The various parameters, such as linearity, precision, accuracy, specificity, robustness, limit of detectio...

journal_title：Chemical & pharmaceutical bulletin

authors： Srinubabu G,Sudharani B,Sridhar L,Rao JS

更新日期：2006-06-01 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：:In line with the recent globalization of the drug supply chain and promotion of the use of generic drugs worldwide, quality assurance is required for drugs globally. In particular, controlling impurities is one of the biggest areas of interest regarding pharmaceutical quality, and it is desirable that the latest scien...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuhama M,Saito R,Miyazaki S

更新日期：2020-01-01 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：:Anhydrous theophylline was prepared by heating theophylline monohydrate at temperatures between 60 degrees C and 140 degrees C. The effects of dehydration temperatures on the moisture absorption and dissolution behavior of anhydrous theophylline were investigated in this study. The hydration rate of anhydrous theophyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2001-12-01 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

abstract：:seco-Macrosphelide E has been isolated from a strain of Periconia byssoides originally separated from the sea hare Aplysia kurodai. Its absolute stereostructure, with the same configuration as that of macrosphelide E, have been elucidated on the basis of spectroscopic analyses and unambiguous synthesis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura H,Ono M,Yamada T,Numata A,Akita H

更新日期：2002-02-01 00:00:00

abstract：:Liposome uptake by HepG2 human hepatoma cells was investigated in comparison with the uptake by J774 murine macrophage-like cells. HepG2 cells accumulated liposomes (egg yolk phosphatidylcholine (EPC)/Chol; 75/25, diameter 0.2 micron) at 37 degrees C comparably to J774 macrophage-like cells. Confocal microscopic obser...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishiwata H,Sato SB,Kobayashi S,Oku M,Vertut-Doï A,Miyajima K

更新日期：1998-12-01 00:00:00

abstract：:A convenient and economical synthesis of 4-hydroxy-2,3-dimethoxybenzaldehyde has been developed. This was used as the starting material for the first total syntheses of (+/-)-isopiline, (+/-)-preocoteine, (+/-)-oureguattidine and (+/-)-3-methoxynordomesticine in which the key step involved formation of ring C of the a...

journal_title：Chemical & pharmaceutical bulletin

authors： Nimgirawath S,Udomputtimekakul P,Taechowisan T,Wanbanjob A,Shen Y

更新日期：2009-04-01 00:00:00

abstract：:The prediction of a protein three-dimensional (3D) structure is one of the most important challenges in computational structural biology. We have developed an automatic protein 3D structure prediction method called FAMSD. FAMSD is based on a comparative modeling method which consists of the following four steps: (1) g...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanou K,Iwadate M,Hirata T,Terashi G,Umeyama H,Takeda-Shitaka M

更新日期：2009-12-01 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：:Three cytotoxic cardenolides, acovenosigenin A 3-O-alpha-L-ramnopyranoside (1), euonymoside A (2) and euonymusoside A (3), were isolated from the woods of Euonymus alata (Celastraceae). The chemical structure of a new cardenolide, euonymusoside A (3) has been elucidated on the basis of extensive spectral analysis and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitanaka S,Takido M,Mizoue K,Nakaike S

更新日期：1996-03-01 00:00:00

abstract：:Three new norlanostane-type triterpene glycosides, scillanostasides A, B, and C, and two new lanostane-type triterpene glycosides, scillanostasides D and E, were isolated from the bulbs of Scilla scilloides Druce (Liliaceae) along with one known norlanostane-type triterpene heptaglycoside, scillascilloside G-1. Their ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Toyohisa D,Morishita T,Horita H,Yasuda S,Nishida Y,Tanaka T,Okawa M,Kinjo J,Yoshimitsu H,Nohara T

更新日期：2011-01-01 00:00:00

abstract：:Oral gel formulations are known as easy to administer drug products for patients who have problems taking drugs including those with conditions such as dysphagia. In addition, there are numerous commercially available oral gel products, most of which are immediate-release formulation that release their pharmaceutical ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hishikawa Y,Kakino Y,Tsukamoto H,Tahara K,Onodera R,Takeuchi H

更新日期：2016-01-01 00:00:00

abstract：:To investigate the possible mechanism of the stimulatory effect of a hot water extract from Artemisia leaf (Artemisia princeps PANPANINI) (AFE) on the proliferation of endothelial cells, cells from bovine aorta were cultured for 72 h in RPMI1640 medium supplemented with 10% fetal calf serum in the presence of 5 microg...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaji T,Kaga K,Miezi N,Hayashi T,Ejiri N,Sakuragawa N

更新日期：1990-09-01 00:00:00

abstract：:The interaction between FSM-16 and flurbiprofen (FBP) in the mesopores of FSM-16 was investigated by using three types of FSM-16 with different pore diameters, i.e., FSM-16(Oc), FSM-16(Do) and FSM-16(Doc) (pore diameters 16.0, 21.6, 45.0 A, respectively). Solid dispersions of 30% FBP-70% FSM-16 were prepared by solven...

journal_title：Chemical & pharmaceutical bulletin

authors： Tozuka Y,Wongmekiat A,Kimura K,Moribe K,Yamamura S,Yamamoto K

更新日期：2005-08-01 00:00:00