Studies on cerebral protective agents. X. Synthesis and evaluation of anticonvulsant activities for novel 4,5,6,7-tetrahydrothieno[3,3-c]pyridines and related compounds.

abstract：:Fourteen flavonol glycosides including two new compounds were isolated from the leaves of two Diospyros plants (D. cathayensis and D. rhombifolia). The structures of isolated compounds were determined by spectroscopic analysis. The scavenging activity of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical of the isolated com...

journal_title：Chemical & pharmaceutical bulletin

authors： Furusawa M,Tanaka T,Ito T,Nakaya K,Iliya I,Ohyama M,Iinuma M,Murata H,Inatomi Y,Inada A,Nakanishi T,Matsushita S,Kubota Y,Sawa R,Takahashi Y

更新日期：2005-05-01 00:00:00

abstract：:Amodiaquine (AQ) is an antimalarial which is effective against chloroquino-resistant strains of Plasmodium falciparum but whose clinical use is severely restricted because of associated hepatotoxicity and agranulocytosis. "One-pot" synthesis of formamidines likely to be transformed into AQ derivatives is reported. Com...

journal_title：Chemical & pharmaceutical bulletin

authors： Delarue S,Girault S,Dali Ali F,Maes L,Grellier P,Sergheraert C

更新日期：2001-08-01 00:00:00

abstract：:Two monomethylated GM(3)-Type ganglioside molecular species, 1 and 2, have been obtained from the polar lipid fraction of the chloroform/methanol extract of the starfish Luidia maculata. The structures of these gangliosides have been determined on the basis of chemical and spectroscopic evidence as 1-O-[8-O-methyl-(N-...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawatake S,Inagaki M,Isobe R,Miyamoto T,Higuchi R

更新日期：2002-10-01 00:00:00

abstract：:A series of 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives was synthesized and evaluated for its ability to reverse a scopolamine-induced learned impairment in a one-trial passive avoidance task (antiamnestic activity). 2-(4-Allyl-1-piperazinyl)-4-pentyloxyquinazoline (4) showed more potent antiamnestic activity th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori M,Iemura R,Hara H,Sukamoto T,Ito K,Ohtaka H

更新日期：1991-02-01 00:00:00

abstract：:Bis[2-[(E)-2-octenoylamino]ethyl] disulfide (compd. I-3) inhibited collagen- and arachidonic acid-induced rat platelet aggregation, although not adenosine 5'-diphosphate (ADP)-induced rat platelet aggregation. Based on these results, we then investigated the inhibitory effect of compd. I-3 on thromboxane B2 formation ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimura T,Nakajima H,Tsujikawa K,Yasuda N,Haruyama M,Okabe M,Iwai M,Yokoyama K

更新日期：1989-03-01 00:00:00

abstract：:We developed a rapid and efficient analytical technique for cyclosporine A using HPLC on a column packed with 2-µm nonporous octadecylsilyl silica particles. Under optimized conditions, cyclosporine A was separated with high resolution from other cyclic peptides within 3 min, because the mass transfer resistance in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Kato K,Nanjo K,Goda Y

更新日期：2018-01-01 00:00:00

abstract：:A new cycloartane bisdesmoside and two new trinorcycloartane glycosides, along with four known cycloartane compounds, were isolated from the rhizomes of Cimicifuga dahurica (Ranunculaceae). The structures of the new compounds were elucidated as 3-O-alpha-L-arabinopyranosyl cimigenol 15-O-beta-D-glucopyranoside, 24-hyd...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang QW,Ye WC,Hsiao WW,Zhao SX,Che CT

更新日期：2001-11-01 00:00:00

abstract：:A new glucocerebroside, linckiacerebroside A (1) and a known glucocerebroside S-2a-3 (2), have been isolated from the cerebroside molecular species obtained from the less polar fraction of the CHCl3/MeOH extract of the starfish Linckia laevigata, together with three pseudo homogeneous glucocerebroside, 3, 4, and 5. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Maruta T,Saito T,Inagaki M,Shibata O,Higuchi R

更新日期：2005-10-01 00:00:00

abstract：:A new cytotoxic substance, designated russuphelin A (1), has been isolated from the mushroom Russula subnigricans Hongo (Basidiomycetes). The structure was elucidated as 2,6-bis(2,6-dichloro-4-hydroxyphenyloxy)-1,4-dimethoxy-benzene on the basis of spectroscopic data and confirmed by total synthesis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi A,Agatsuma T,Matsuda M,Ohta T,Nunozawa T,Endo T,Nozoe S

更新日期：1992-12-01 00:00:00

abstract：:A new flavonol, morin-3-O-alpha-rhamnopyranoside (1), along with four known flavonols, kaempferol 3-O-alpha-rhamnopyranoside (2), kaempferol 3-O-beta-glucopyranoside (3), quercetin 3-O-alpha-rhamnopyranoside (4) and (+)-catechin (5), were isolated from the methanolic extract of Muehlenbeckia platyclada. The structures...

journal_title：Chemical & pharmaceutical bulletin

authors： Yen CT,Hsieh PW,Hwang TL,Lan YH,Chang FR,Wu YC

更新日期：2009-03-01 00:00:00

abstract：:To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng XW,Huang N,Xu H,Yang WB,Yang LM,Qu H,Zheng YT

更新日期：2010-07-01 00:00:00

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：:We previously reported an increase in aminobutyrate aminotransferase (GABA-T) activity in the cerebrum of Alzheimer patients. In the present study, we investigated whether such findings are common in the usual aging process as well. We examined the activity of various enzymes, which were examined in the previous study...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoyagi T,Wada T,Kojima F,Nagai M,Harada S,Takeuchi T,Hirokawa K

更新日期：1990-06-01 00:00:00

abstract：:A simple one-step synthesis was accomplished for the preparation of N-phosphoramidophosphonates by a direct reaction of phosphoramidate (1) with heterocyclic aldehydes (2a-j) and dialkyl phosphites at 60-70 degrees C in the presence of tetramethylguanidine. The tetramethylguanidine not only catalyses this reaction but...

journal_title：Chemical & pharmaceutical bulletin

authors： Veera Narayana Reddy M,Balakrishna A,Kumar MA,Reddy GC,Sankar AU,Reddy CS,Krishna TM

更新日期：2009-12-01 00:00:00

abstract：:Analysis of the structural requirements of compound 1 (SR48968), a potent NK2 receptor antagonist, revealed that the 4-phenyl group of the piperidine is essential for binding with the NK2 receptor and occupies an equatorial position. Energy calculation of a variety of substituted 4-phenyl piperidines revealed that spi...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Fujii M,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:Microdialysis sampling method coupled to high-performance liquid chromatography with UV detection was applied to continuous monitoring of in vivo unbound flomoxef concentration in rat blood. By comparison with ultrafiltration method, it was demonstrated that it gave reliable results for the unbound drug monitoring in ...

journal_title：Chemical & pharmaceutical bulletin

authors： Saisho Y,Umeda T

更新日期：1991-03-01 00:00:00

abstract：:Seven antioxidative serotonin derivatives were isolated from safflower (Carthamus tinctorius L.) oil cake. Their structures were established as N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]ferulamide (1), N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-p-coumaramide (2), N,N'-[2,2'-(5,5'-dihydroxy-4,4'-bi-1H-indol-3,3'-yl)diethyl]- di-p-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang HL,Nagatsu A,Watanabe T,Sakakibara J,Okuyama H

更新日期：1997-12-01 00:00:00

abstract：:A series of 4-phenoxy-2-(1-piperazinyl)quinazolines was synthesized and examined for anticonvulsive and antihypoxic activities. Many of the compounds exhibited potent anticonvulsive activity comparable to that of carbamazepine or phenytoin. Among them, 4-phenoxy-2-(4-propyl-1-piperazinyl)quinazoline (5w) was selected ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori M,Iemura R,Hara H,Ozaki A,Sukamoto T,Ohtaka H

更新日期：1990-03-01 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：:2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor γ (PPARγ) and PPARα agonist activities and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otake K,Azukizawa S,Takahashi K,Fukui M,Shibabayashi M,Kamemoto H,Kasai M,Shirahase H

更新日期：2011-01-01 00:00:00

abstract：:The bulbs of Habranthus brachyandrus (Amaryllidaceae) have been extensively analyzed for their chemical constituents, resulting in the isolation of eight flavan derivatives (1-8), four of which are new naturally occurring compounds; a new hydroxybutyric acid glucoside (9); three known phenolic compounds (10-12); and s...

journal_title：Chemical & pharmaceutical bulletin

authors： Jitsuno M,Yokosuka A,Sakagami H,Mimaki Y

更新日期：2009-10-01 00:00:00

abstract：:The resistance to crushing after a self-setting bioactive calcium phosphate cement, consisting of various particle sizes of tetracalcium phosphate (TECP), dicalcium phosphate dihydrate (DCPD) and hydroxyapatite (HAP), had hardened was tested after setting at 37 degrees C, 100% RH. X-ray diffraction suggested that the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otsuka M,Matsuda Y,Suwa Y,Fox JL,Higuchi WI

更新日期：1993-11-01 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：:An uncommon, previously unreported p-quinone-lignan compound called justicidone (4-(1,3-benzodioxol-5-yl)-6-methoxynaphtho[2,3-c]furan-1,5,8(3H)-trione) (2), along with the known savinin (1) were isolated from Justicia hyssopifolia (Acanthaceae). Their structures were determined by spectroscopic methods. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Andrés Pérez J,Boluda C,López H,Manuel Trujillo J

更新日期：2004-01-01 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：:A new route to (+)-estrone has been developed starting from the chiral building block having a bicyclo[3.2.1]octane framework based on the inherent stereochemical chemical nature of the chiral building block. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hanada K,Miyazawa N,Ogasawara K

更新日期：2003-01-01 00:00:00

abstract：:Two new lignans, 4-methoxymagnaldehyde B (1) and coumanolignan (2), were isolated from the stem bark of Magnolia obovata, together with 11 known compounds (3-13). The structures of compounds 1 and 2 were determined to be 5'-allyl-2'-hydroxyphenyl-4-methoxy-3-cinnamic aldehyde (1) and 6-allyl-8-(5'-allyl-2'-hydroxyphen...

journal_title：Chemical & pharmaceutical bulletin

authors： Youn U,Chen QC,Lee IS,Kim H,Yoo JK,Lee J,Na M,Min BS,Bae K

更新日期：2008-01-01 00:00:00

abstract：:The effect of substituents at the C-3 position on the degradation kinetics of the pivaloyloxymethyl (POM) ester of delta 3 cephalosporin in phosphate buffer solution (pH 6-8) was investigated. In the degradation, the isomerization process to the delta 2 ester was the rate-determining step. In this study, the logarithm...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyauchi M,Kurihara H,Fujimoto K,Kawamoto I,Ide J,Nakao H

更新日期：1989-09-01 00:00:00

abstract：:N-9-Fluorenylmethoxycarbonyl-Se-4-methoxybenzylselenocysteine++ + [Fmoc-Sec(MBzl)-OH] was synthesized from selenocystine and successfully applied to Fmoc-based solid-phase peptide synthesis. The stability and the deprotection conditions of the Se-MBzl group were examined. The diselenide bond of a peptide was directly ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koide T,Itoh H,Otaka A,Yasui H,Kuroda M,Esaki N,Soda K,Fujii N

更新日期：1993-03-01 00:00:00

abstract：:Four new prenylated bibenzyls, named aglaiabbrevins A-D (2, 4-6), were isolated from the leaves of Aglaia abbreviata, along with two known related analogues, 3,5-dihydroxy-2-[3,7-dimethyl-2(E),6-octadienyl]bibenzyl (7) and 3,5-dihydroxy-2-(3-methyl-2-butenyl)bibenzyl (8). The structures of the new compounds were eluci...

journal_title：Chemical & pharmaceutical bulletin

authors： Sun P,Jiang CS,Zhang Y,Liu AH,Liang TJ,Li J,Guo YW,Jiang JM,Mao SC,Wang B

更新日期：2017-01-01 00:00:00