Synthesis and biological evaluation of indoloquinolines and pyridocarbazoles: a new example of unexpected photoreduction accompanying photocyclization.

abstract：:Synthesis of (1R,2S,5S,6R,8S)-3-azabicyclo[3.3.0]octane-2,6,8-tricarboxylic acid (2) from trans-4-hydroxy-L-proline (5) was attempted. A Diels-Alder reaction of 3,4-dehydroproline derivative 9 and cyclopentadiene afforded a single stereoisomer 11. The Diels-Alder adduct was smoothly converted to the hydrochloride of 2...

journal_title：Chemical & pharmaceutical bulletin

authors： Arakawa Y,Ohnishi M,Yoshimura N,Yoshifuji S

更新日期：2003-08-01 00:00:00

abstract：:Hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC), a polymer in which a small amount of HPMC is stearoxyl substituted, was used as an emulsifier of emulsion-type lotion. A high-pressure homogenizer (microfluidizer) was used. The viscosity of the 1% HM-HPMC aqueous gel decreased after passing through the...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujii M,Wada F,Honda N,Miura K,Hashizaki K,Taguchi H,Koizumi N,Watanabe Y

更新日期：2020-01-01 00:00:00

abstract：:C1q/tumor necrosis factor (TNF)-related protein 12 (CTRP12) is a secretory protein that participates in the regulation of glucose and lipid metabolism in obesity and diabetes. Its role in cardiovascular disease, particularly sepsis-induced cardiac injury, is unclear. Here, we stimulated cardiomyocytes with lipopolysac...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou MQ,Jin E,Wu J,Ren F,Yang YZ,Duan DD

更新日期：2020-01-01 00:00:00

abstract：:A method for the preparation of insulin derivatives having protected sulfhydryl group(s) on definite site(s) on the molecule which uses anion-exchange high performance liquid chromatography on a TSKgel DEAE-2SW column for separation is described. Porcine insulin reacts with N-succinimidyl S-acetylthioacetate to afford...

journal_title：Chemical & pharmaceutical bulletin

authors： Nanami M,Zaitsu K,Ohkura Y

更新日期：1992-04-01 00:00:00

abstract：:In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-(spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Kakefuda A,Nagaoka H,Yamamoto O,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:Stereocontrolled syntheses of model compounds related to a major antigenic epitope against antibupleurum 2IIc/PG-1-IgG from antiulcer pectic polysaccharide are described. A trisaccharide derivative (13) was prepared as a precursor and a novel and simple approach for the rational design of a glycocluster and glycodendr...

journal_title：Chemical & pharmaceutical bulletin

authors： Jin Y,Hada N,Oka J,Kanie O,Daikoku S,Kanie Y,Yamada H,Takeda T

更新日期：2006-04-01 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：:Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4...

journal_title：Chemical & pharmaceutical bulletin

authors： Takai K,Enomoto T

更新日期：2018-01-01 00:00:00

abstract：:Silicone has been utilized as a carrier material for sustained release system of lipophilic drugs. Extensive studies revealed that drug release rate is influenced by factors such as physicochemical properties of the drug and additives.(1-5)) When a lipophilic drug is highly potent at low concentrations, the drug relea...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajihara M,Sugie T,Sano A,Fujioka K,Urabe Y,Tanihara M,Imanishi Y

更新日期：2003-01-01 00:00:00

abstract：:20(S)-Camptothecin derivatives having nitro, amino, chloro, bromo, hydroxyl and methoxyl groups in the A-ring were synthesized. B-Ring hydrogenated camptothecin (2a) was converted into 10-hydroxycamptothecin (6e) by treatment with lead tetraacetate in trifluoroacetic acid. 10-Substituted derivatives (6) were obtained ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sawada S,Matsuoka S,Nokata K,Nagata H,Furuta T,Yokokura T,Miyasaka T

更新日期：1991-12-01 00:00:00

abstract：:Melt pelletization of lactose 450 M was carried out in an 8-l high shear mixer using PEG 3000 as the meltable binder. The pore size and size distribution of the melt pellets were determined using mercury intrusion porosimetry. The pore size distribution of melt pellets was found to be bimodal. With a higher binder con...

journal_title：Chemical & pharmaceutical bulletin

authors： Wong TW,Chan LW,Heng PW

更新日期：2000-11-01 00:00:00

abstract：:[D-Leu8]Dynorphin(1--8)-NH2 analogs, in which each peptide bond was systematically replaced with a psi(CH2NH) peptide bond, were synthesized by the solid-phase method. The psi(CH2NH) bond was introduced by the Boc-amino acid aldehyde/NaCNBH3 method on a solid support. In the syntheses of the analogs, undesirable doubl...

journal_title：Chemical & pharmaceutical bulletin

authors： Ambo A,Adachi T,Sasaki Y

更新日期：1995-09-01 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：:Five glycyrrhetinic acid (Ib) derivatives have been synthesized to try to improve the antioxidant activity. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA pr...

journal_title：Chemical & pharmaceutical bulletin

authors： Ablise M,Leininger-Muller B,Wong CD,Siest G,Loppinet V,Visvikis S

更新日期：2004-12-01 00:00:00

abstract：:A novel γ-cyclodextrin (γ-CD) based carrier for molecular encapsulation of cancer chemotherapeutic agent doxorubicin (DOX) was synthesized and fully characterized by various analytical approaches. The γ-CD derivative, with a β-naphthyl alanine residue attached in its primary face, exhibits potent binding capacity with...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu D,Wang L,Gourevich D,Kabha E,Arditti F,Athamna M,Cochran S,Melzer A,Gnaim JM

更新日期：2014-01-01 00:00:00

abstract：:The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydr...

journal_title：Chemical & pharmaceutical bulletin

authors： Giammona G,Giannola LI,Carlisi B,Bajardi ML

更新日期：1989-08-01 00:00:00

abstract：:Two new iridoids, named patridoid I (1) and patridoid II (2), were isolated from the whole plant of Patrinia saniculaefolia (Valerianaceae), together with the known one, nardostachin (3). The structures of compounds 1 and 2 were established on the basis of spectroscopic methods, including two dimensional (2D NMR) and ...

journal_title：Chemical & pharmaceutical bulletin

authors： An RB,Min BS,Na MK,Chang HW,Son KH,Kim HP,Lee HK,Bae K,Kang SS

更新日期：2003-05-01 00:00:00

abstract：:The synthesis of optically active acyclic analogues of 3'-azido-3'-deoxythymidine, which lack only the 2'-CH2 of the sugar, is described. The synthesis of some nucleoside analogues that contain the N-acetyl-D-neuraminic acid moiety is also described. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Murata M,Achiwa K

更新日期：1990-03-01 00:00:00

abstract：:The differences in biological activities among polychlorinated dibenzo-p-dioxins (dioxins) are strongly dependent on the substitution pattern of chlorine at various positions on the parent dibenzo-p-dioxin molecule. The absolute hardness, eta, of dioxins shows a good correlation with the potency of biological activity...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi S,Sameshima K,Ishii Y,Tanaka A

更新日期：1995-10-01 00:00:00

abstract：:A series of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5HT3) receptor antagonistic activities by means of assays of 5-HT3 receptor binding and the ability to antagonize the von Bezold-Jarisch reflex in rats. Replacement of the 1,4-benzoxazine ring with a 1,4...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroita T,Marubayashi N,Sano M,Kanzaki K,Inaba K,Kawakita T

更新日期：1996-11-01 00:00:00

abstract：:Antimutagenic activity-guided fractionation of an extract prepared from the thorns of Gleditsia sinensis LAM. led to the isolation of one triterpenoid and four steroids, which were identified as D:C-friedours-7-en-3-one (1), stigmast-4-ene-3,6-dione (2), stigmastane-3,6-dione (3), stigmasterol (4), and beta-sitosterol...

journal_title：Chemical & pharmaceutical bulletin

authors： Lim JC,Park JH,Budesinsky M,Kasal A,Han YH,Koo BS,Lee SI,Lee DU

更新日期：2005-05-01 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：:We have attempted to prepare micronized drug particles and to maintain the micronized state long-term in order to improve the solubility of a practically insoluble drug, griseofulvin (GF). GF nanoparticles (GFNPs) prepared by high-pressure homogenization were micronized to about 45 nm (mean particle size). GFNPs were ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kamiya S,Nozawa Y,Miyagishima A,Kurita T,Sadzuka Y,Sonobe T

更新日期：2006-02-01 00:00:00

abstract：:Anion-exchange resins modified with metal-porphine (M-Pr) have been investigated to develop a solid catalyst in the oxidative reaction of phenols by O2 in air. Co-Pr, which is easily prepared and separable from the reaction mixture, has been proved to accelerate the oxidative reaction of phenols such as 3,5-di-tertbut...

journal_title：Chemical & pharmaceutical bulletin

authors： Iwado A,Mifune M,Kato J,Oda J,Chikuma M,Motohashi N,Saito Y

更新日期：2000-11-01 00:00:00

abstract：:A new cyclic tetrapeptide (1), along with known congeners (2, 3), was isolated from the fungus Phoma sp. derived from the giant jellyfish Nemopilema nomurai. The absolute configuration of 1 was determined using the modified Mosher's method and Marfey's method. Compound 1 displayed a weak suppressive effect on the prod...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim EL,Li JL,Xiao B,Hong J,Yoo ES,Yoon WD,Jung JH

更新日期：2012-01-01 00:00:00

abstract：:Aspartame (L-alpha-aspartyl-L-phenylalanine methyl ester) is a dipeptide sweetener about 200 times as sweet as sugar. It exists in crystal forms such as IA, IB, IIA, and IIB, which differ in crystal structure and in the degree of hydration. Among these, IIA is the most stable crystal form, and its crystal structure ha...

journal_title：Chemical & pharmaceutical bulletin

authors： Ebisawa K,Nagashima N,Fukuhara K,Kumon S,Kishimoto S,Suzuki E,Yoneda S,Umeyama H

更新日期：2000-05-01 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：:Sulfonic acid functionalized silica catalyzed the three-component reaction of aromatic amines, alpha,beta-unsaturated aldehydes and beta-keto esters forming the corresponding 1,4-dihydropyridines in short reaction times and in high yields. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Das B,Suneel K,Venkateswarlu K,Ravikanth B

更新日期：2008-03-01 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：:The regioselective intramolecular 1,3-dipolar cycloaddition of the phenylsulfonylallene-nitrone derivatives has been developed. This reaction showed that the distal double bond of the allene exclusively reacted with the nitrone group to produce the bicyclic isoxazolidine derivatives regardless of the substitution patt...

journal_title：Chemical & pharmaceutical bulletin

authors： Inagaki F,Kobayashi H,Mukai C

更新日期：2012-01-01 00:00:00