Prolyl endopeptidase inhibitory activity of fourteen Kampo formulas and inhibitory constituents of Tokaku-joki-to.

abstract：:Novel C(7)-derivatives of 1-cyclopropyl-6-fluoro-4-quinolone carboxylic acid (3a-o) have been synthesized and evaluated for in vitro antibacterial activity. Compounds 3e (3-aminocyclobutyl), 3g (1-aminocyclopropyl), 3m ((2-aminomethyl)vinyl), and 3o ((1-aminomethyl)vinyl) showed significant inhibitory activity, compar...

journal_title：Chemical & pharmaceutical bulletin

authors： Todo Y,Nitta J,Miyajima M,Fukuoka Y,Ikeda Y,Yamashiro Y,Saikawa I,Narita H

更新日期：1994-10-01 00:00:00

abstract：:When 8-bromoadenosine was incubated with cysteine at pH 7.2 and 37°C, an exclusive product was generated. This product was identified as a cysteine substitution derivative of adenosine at the 8 position, 8-S-L-cysteinyladenosine. The reaction accelerated as pH increased from mildly acidic to basic conditions. The isol...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Ogishi A,Shinohara T,Suito S

更新日期：2018-01-01 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：:Phytochemical investigation of the leaves of Umbilicus pendulinus afforded in addition to 2-O-caffeoyl malate, isoquercitrin and Z-venusol, the new isomer E-venusol. Special NMR experiments were carried out to elucidate the configuration of the two latter compounds. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Viornery L,Saliba C,Daskiewicz JB,Bayet C,Comte G,Fenet B,Gutierrez G,Barron D

更新日期：2000-11-01 00:00:00

abstract：:Two novel pentanorcucurbitane triterpenes, 22-hydroxy-23,24,25,26,27-pentanorcucurbit-5-en-3-one (1) and 3,7-dioxo-23,24,25,26,27-pentanorcucurbit-5-en-22-oic acid (2) together with a new trinorcucurbitane triterpene, 25,26,27-trinorcucurbit-5-ene-3,7,23-trione (3) were isolated from the methyl alcohol extract of the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen CR,Liao YW,Wang L,Kuo YH,Liu HJ,Shih WL,Cheng HL,Chang CI

更新日期：2010-12-01 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：: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：:Three new quinovic acid glycosides, named gongganosides A (1), B (2), and C (3), were isolated from the bark of Bhesa paniculata (Celastraceae), an Indonesian medicinal plant collected in Sumatra Island. The chemical structures have been elucidated on the basis of chemical and physicochemical evidence as quinovic acid...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohashi K,Kojima H,Tanikawa T,Okumura Y,Kawazoe K,Tatara N,Shibuya H,Kitagawa I

更新日期：1994-08-01 00:00:00

abstract：:Two efficient and practical methods of synthesis of the C-10 substituent of DV-7751 (1), a novel quinolone carboxylic acid, were established. The first method utilizes an optical resolution of racemic 8-amino-6-benzyl-6-azaspiro[3.4]octane (13), while the second employs an enantioselective microbial reduction of 6-ben...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyadera A,Satoh K,Imura A

更新日期：2000-04-01 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：:Chemical investigation on the constituents of the cones of Cycas beddomei has resulted in the isolation of a new biflavonoid, 2,3-dihydro-4'''-O-methyl amentoflavone, along with 2,3,2'',3''-tetrahydro hinokiflavone, 2,3,2'',3''-tetrahydro amentoflavone, 2,3-dihydro amentoflavone. The last two compounds were not report...

journal_title：Chemical & pharmaceutical bulletin

authors： Das B,Mahender G,Koteswara Rao Y,Prabhakar A,Jagadeesh B

更新日期：2005-01-01 00:00:00

abstract：:Several kinds of loline-type alkaloids, norloline, loline, N-acetylnorloline, N-acetylloline, N-formylnorloline, N-formylloline and N-methylloline were detected in the urine of race-horses. Furthermore, a new compound of the alkaloids, N-senecioylnorloline, was also found and identified. These compounds were mainly id...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeda A,Suzuki E,Kamei K,Nakata H

更新日期：1991-04-01 00:00:00

abstract：:The characteristic diagram for refolding of denatured reduced lysozyme was prepared in terms of recovered activity by employing urea and LiCl concentrations as two axes of rectangular coordinates. The diagram obtained will serve as a new tool not only for the optimum design of refolding media but also for the study of...

journal_title：Chemical & pharmaceutical bulletin

authors： Tano K,Nohara D,Matsubara M,Sakai T

更新日期：1995-11-01 00:00:00

abstract：:The iron(III) complex of 2,7,12,17-tetraethyl-3,6,11,18-tetra-methylcorrphycene, an isomeric heme, was complexed with apomyoglobin to examine the ligand binding ability of the novel macrocycle under physiological conditions. The reconstituted holoprotein was found to be functionally active at pH 7.4 and 20 degrees C a...

journal_title：Chemical & pharmaceutical bulletin

authors： Neya S,Nakamura M,Imai K,Funasaki N

更新日期：2001-03-01 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：:In the previous paper, we reported the differentiation inducing activities of lignoids from Arctium Fructus (the fruits of Arctium lappa L., Compositae) against mouse myeloid leukemia cells (M1). We reinvestigated the active components of this extract and isolated three new dilignans. Furthermore, structure modificati...

journal_title：Chemical & pharmaceutical bulletin

authors： Umehara K,Nakamura M,Miyase T,Kuroyanagi M,Ueno A

更新日期：1996-12-01 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：:An aniline derivative which corresponds to UV-5 in the preceding paper was isolated from the case L-tryptophan sample associated with eosinophilia-myalgia syndrome (EMS). By spectroscopic analyses, the structure was identified as 3-anilinoalanine. The compound was optically active, and the stereochemistry of alanine m...

journal_title：Chemical & pharmaceutical bulletin

authors： Goda Y,Suzuki J,Maitani T,Yoshihira K,Takeda M,Uchiyama M

更新日期：1992-08-01 00:00:00

abstract：:The pharmacokinetics of [6]-gingerol were investigated in rats with acute renal failure induced by bilateral nephrectomy, or those with acute hepatic failure induced by a single oral administration of carbon tetrachloride (CCl4), to clarify the contribution of the kidney and liver to the elimination process of [6]-gin...

journal_title：Chemical & pharmaceutical bulletin

authors： Naora K,Ding G,Hayashibara M,Katagiri Y,Kano Y,Iwamoto K

更新日期：1992-05-01 00:00:00

abstract：:Bromination of 17-O-acetyltestosterone (17beta-acetoxyandrost-4-en-3-one) (1) was performed with 1, 5, and 10 eq of Br2 in AcOH-Et2O at room temperature. In all cases 2alpha,6beta- (2) and 2alpha,6beta-dibromo-17beta-acetoxyandrost-4-en-3-one (3) were obtained, although the yields were dependent upon the conditions us...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimizu T,Tobari A,Koyanagi J,Kawase M,Saito S

更新日期：2001-01-01 00:00:00

abstract：:A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The "in vitro" antibacterial activity of these compounds and their corresponding alpha-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobi...

journal_title：Chemical & pharmaceutical bulletin

authors： Rival Y,Grassy G,Michel G

更新日期：1992-05-01 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：:Four new triterpene glycosides, named nigellosides A, B, C, and D, were from the air-dried aerial parts of Nigella damascena L. (Ranunculaceae), and the structures were elucidated on the basis of spectroscopic data including 2D NMR spectra and chemical evidence. Their chemical structures have been characterized as 3-O...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshimitsu H,Nishida M,Okawa M,Nohara T

更新日期：2007-03-01 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：:The decomposition products and mutagenic activity in Salmonella typhimurium strains TA98, TA100 and TA104 in the presence and absence of S9 mix of linear dodecylbenzenesulfonate (DBS) in aqueous solution after ozone treatment alone or simultaneous treatment with ozone and ultraviolet (UV) irradiation (ozone/UV treatme...

journal_title：Chemical & pharmaceutical bulletin

authors： Murakami K,Matsumoto H,Kinouchi T,Ohnishi Y

更新日期：1992-06-01 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：:(+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4, 5-tetrahydro-8H-pyrido[4',3':4,5]thieno[3,2-f]triazolo[4,3-a] [1,4]diazepine (E6123) is a very potent platelet-activating factor (PAF) receptor antagonist and shows potent anti-PAF activities at the microgram level in a variety of animal models. In ord...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazawa S,Okano K,Kawahara T,Machida Y,Yamatsu I

更新日期：1992-03-01 00:00:00

abstract：:Four new lanostane triterpene lactones (colossolactone I, colossolactone II, colossolactone III and colossolactone IV) were isolated from the Vietnamese mushroom Ganoderma colossum (FR.) C. F. BAKER along with five known compounds. The structures of the new compounds were determined on the basis of MS, NMR and circula...

journal_title：Chemical & pharmaceutical bulletin

authors： El Dine RS,El Halawany AM,Nakamura N,Ma CM,Hattori M

更新日期：2008-05-01 00:00:00

abstract：:Biotransformation of chrysin by Cunninghamella elegans NRRL 1392 produced apigenin, apigenin 7-sulfate, apigenin 7,4'-disulfate, and a new metabolite identified as chrysin 7-sulfate. On the other hand, fermentation of apigenin, using the same microorganism, yielded apigenin 7-sulfate and apigenin 7,4'-disulfate. The s...

journal_title：Chemical & pharmaceutical bulletin

authors： Ibrahim AR

更新日期：2005-06-01 00:00:00

abstract：:A rapid tandem mass spectrometric (MS-MS) method for the quantification of Oxcarbazepine (OXB) in human plasma using imipramine as an internal standard (IS) has been developed and validated. Chromatographic separation was achieved isocratically on a C18 reversed-phase column within 3.0 min, using a mobile phase of ace...

journal_title：Chemical & pharmaceutical bulletin

authors： Srinubabu G,Ratnam BV,Rao AA,Rao MN

更新日期：2008-01-01 00:00:00