Synthesis and HIV-1 integrase inhibition of novel bis- or tetra-coumarin analogues.

abstract：:We describe here a Tf₂NH-catalyzed formal (3+3) cycloaddition of silyl enol ethers with acrylates as a new domino reaction. In the domino sequence, the catalyst activates Michael addition, deprotonation of the resulting silyloxonium cation and intramolecular Claisen condensation. It was found that reaction modes signi...

journal_title：Chemical & pharmaceutical bulletin

authors： Azuma T,Takemoto Y,Takasu K

更新日期：2011-01-01 00:00:00

abstract：:Remote loading of insulin and bovine serum albumin (BSA) into neutral or positively-charged liposomes by incubation under a transmembrane pH gradient or non-pH gradient was investigated. Trapping efficiencies in several incubation conditions were compared with those of the conventional reverse-phase evaporation vesicl...

journal_title：Chemical & pharmaceutical bulletin

authors： Hwang SH,Maitani Y,Takayama K,Nagai T

更新日期：2000-03-01 00:00:00

abstract：:A series of 5-(4-aryl- or 4-arylcarbonylpiperazin-1-yl)-5-deoxy-1,4: 3,6-dianhydro-L-iditol 2-nitrates was prepared in order to obtain orally active, nitrate-type vasodilators with reduced side effects. Our drug design was based on a small reduction in the lipophilicity compared to that of 5-deoxy-5-[4-(3-phenylthiopr...

journal_title：Chemical & pharmaceutical bulletin

authors： Hayashi H,Ikeda J,Kubo K,Moriyama T,Karasawa A,Suzuki F

更新日期：1993-06-01 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：:2,8-Dimethyl-1-oxa-8-azaspiro[4,5]decan-3-one (17), designed by incorporating the tetrahydrofuran ring moiety of muscarone into an 8-azaspiro[4,5]decane skeleton, and related 1-oxa-8-azaspiro[4.5]decanes were synthesized and assessed as M1 muscarinic agonists for the symptomatic treatment of dementia of Alzheimer's ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsukamoto S,Fujii M,Yasunaga T,Matsuda K,Wanibuchi F,Hidaka K,Furuya T,Tamura T

更新日期：1995-05-01 00:00:00

abstract：:This report describes the synthesis and antiviral effects of (6'R)-6'-C-ethynyl, -ethenyl, and -ethyl derivatives of neplanocin A (7a, 8a, and 9a, respectively) and the corresponding 6'S-diastereomers (7b, 8b, and 9b, respectively), as examples of 6'-C-substituted analogues of neplanocin A. Grignard reaction of the 6'...

journal_title：Chemical & pharmaceutical bulletin

authors： Shuto S,Obara T,Saito Y,Yamashita K,Tanaka M,Sasaki T,Andrei G,Snoeck R,Neyts J,Padalko E,Balzarini J,De Clercq E,Matsuda A

更新日期：1997-07-01 00:00:00

abstract：:In this study we report the synthesis and pharmacological evaluation of four new progesterone derivatives; 17alpha-hydroxy-16beta-methylpregna-4,6-diene-3,20-dione 12, 17alpha-cyclopropylcarbonyloxy-16beta-methylpregna-4,6-diene-3,20-dione 13, 17alpha-cyclobutylcarbonyloxy-16beta-methylpregna-4,6-diene-3,20-dione 14, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ramírez E,Cabeza M,Bratoeff E,Heuze I,Pérez V,Valdez D,Ochoa M,Teran N,Jimenez G,Ramírez T

更新日期：2005-12-01 00:00:00

abstract：:Mucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the t...

journal_title：Chemical & pharmaceutical bulletin

authors： Ruiz-Caro R,Gago-Guillan M,Otero-Espinar FJ,Veiga MD

更新日期：2012-01-01 00:00:00

abstract：:In order to gain an understanding of protein binding of sulfadimethoxine (SDM) and its major metabolite, N4-acetylsulfadimethoxine (N4-AcSDM), the binding of SDM and N4-AcSDM to human and rabbit serum albumin (HSA and RSA) was investigated using circular dichroism (CD), fluorescence and dialysis techniques. The CD spe...

journal_title：Chemical & pharmaceutical bulletin

authors： Otagiri M,Nakamura H,Maruyama T,Imamura Y,Takadate A

更新日期：1989-02-01 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

abstract：:A series of about fifty novel 5-arylfuro[2,3-d]pyrimidine derivatives were synthesized as potential inhibitors of dihydrofolate reductase (DHFR) arising from different species. Weak enzyme inhibition was observed for most of the compounds, with only a few reaching IC50 values less than 30 microM. With regards to antib...

journal_title：Chemical & pharmaceutical bulletin

authors： Wahid F,Monneret C,Dauzonne D

更新日期：1999-02-01 00:00:00

abstract：:Acidic segment of an acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor, R-106578 was synthesized by enantioselective hydrogenation of the Z-olefine (9-(Z)) using (R)-2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (BINAP)-Ru(OAc)2 as a catalyst in methanol at 100 degrees C, 5 kgf/cm2 of H2 pressure. The requisite Z-o...

journal_title：Chemical & pharmaceutical bulletin

authors： Murakami M,Kobayashi K,Hirai K

更新日期：2000-10-01 00:00:00

abstract：:The effect of propranolol (PPL), phenoxybenzamine (PBZ) or bicuculline (BCL) on the diazepam (DZP)-induced changes of pineal melatonin synthesis in male rats was examined in vivo and in vitro. Administration of PBZ did not affect the inhibitory action of DZP on pineal melatonin synthesis in vivo. A single injection of...

journal_title：Chemical & pharmaceutical bulletin

authors： Wakabayashi H,Shimada K,Satoh T

更新日期：1991-10-01 00:00:00

abstract：:Conjugates of 2-aminooxyethyliminodiacetic acid with estrone, testosterone, epiandrosterone, 17-alpha-hydroxy-progesterone and progesterone were synthesized and their complexes with Tc-99m were successfully prepared in good yields, which indicated the agent to be promising for metal-labeling of biomolecules and relate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoda R,Karube Y,Takata J,Nagata Y,Matsushima Y

更新日期：1999-03-01 00:00:00

abstract：:The purpose of this study was to determine which foods and/or drinks are capable of reducing the bitterness of topiramate when consumed together with the medicine. The inhibitory effects of foods/drinks (yoghurt and nine other foods/drinks) on the bitterness of topiramate (5 mg/mL) were evaluated with a taste sensor u...

journal_title：Chemical & pharmaceutical bulletin

authors： Haraguchi T,Uchida T,Hazekawa M,Yoshida M,Nakashima M,Sanda H,Hase T,Tomoda Y

更新日期：2016-01-01 00:00:00

abstract：:The bitter and sweet forms of a plant species differing with alkaloid contents may provide a model system for investigation of alkaloid biosynthesis at a molecular level. The pattern and concentration of quinolizidine alkaloids were determined by capillary GC-MS in bitter and sweet plants of Lupinus angustifolius. Bit...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirai MY,Suzuki H,Yamazaki M,Saito K

更新日期：2000-10-01 00:00:00

abstract：:The gamma subunit of enolase (gamma-enolase) was purified from the brain tissues of cow, dog, goat, pig, rabbit, and rat. The purification was achieved in only three steps: ammonium sulfate-precipitation, DE 53 cellulose ion-exchange chromatography, and polyacrylamide gel electrophoresis (PAGE) in a preparative mode. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoki T,Tanaka T,Watabe H

更新日期：1992-05-01 00:00:00

abstract：:Nonenzymatically glycated human serum albumin was incubated with ferric ion at 37 degrees C in 0.2 M phosphate buffer, pH 7.4, up to 30 days. In the incubation mixture, amino acids, tyrosine and phenylalanine, were detected, suggesting site specific cleavage of glycated human serum albumin. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai T,Takanashi M,Tsuchiya S

更新日期：1992-06-01 00:00:00

abstract：:A series of 2-(4-methylphenyl)benzothiazoles was synthesized and evaluated using an adjuvant-induced arthritic rat model. This class of desired compounds affecting the immune response was found using hemagglutination assay. 4-Acetoxy-2-(4-methylphenyl)benzothiazole (7m), KB-2683, was most potent in the adjuvant-induce...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori N,Tsukamoto G,Imamura A,Ohashi M,Saito T,Yoshino K

更新日期：1992-09-01 00:00:00

abstract：:Diabetic embryopathy is a diabetic complication, in which maternal hyperglycemia in early pregnancy causes birth defects in newborn infants. Under maternal diabetic conditions, hyperglycemia disturbs intracellular molecular activities and organelles functions. These include protein misfolding in the endoplasmic reticu...

journal_title：Chemical & pharmaceutical bulletin

authors： Han L,Jiang Z,Zheng X,Qiu J,Hu Y,Li X

更新日期：2019-01-01 00:00:00

abstract：:Thioglycosides are available donors in glycosylation due to the stability of the anomeric C-S bond under general reaction conditions of protection and deprotection, and offer orthogonality in their activation. We report now that the hypervalent iodine effectively induced glycosylation reaction of thioglycosides with v...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajimoto T,Morimoto K,Ogawa R,Dohi T,Kita Y

更新日期：2016-01-01 00:00:00

abstract：:A prevention method of the sorption of bromhexine HCl to plastic materials used in packaging was investigated. Four kinds of plastic packaging materials were used: Polyethylene (PE), polyethylene terephthalate (PET), polypropylene (PP) and polyacrylonitrile (PAN). Three polyethylenes having different densities were us...

journal_title：Chemical & pharmaceutical bulletin

authors： Kukita T,Furuuchi S,Nemoto M,Yoshida T

更新日期：1992-11-01 00:00:00

abstract：:A series of benzylamides of N-alkylated, N-acylated or free nine cyclic and one linear amino acids as potential anticonvulsants have been synthesized. The structures of the obtained compounds were designed on the basis of the previously determined structure and physicochemical properties/anticvonvulsant activity relat...

journal_title：Chemical & pharmaceutical bulletin

authors： Paruszewski R,Strupińska M,Stables JP,Swiader M,Czuczwar S,Kleinrok Z,Turski W

更新日期：2001-05-01 00:00:00

abstract：:Fourteen new bisnor- and norditerpene dilactones, makilactones E-R, having a 7alpha : 8alpha-epoxy-9,11-enolide substructure, were isolated from a methanolic extract of the root and the bark of Podocarpus macrophyllus D. DON (Podocarpaceae) with thirteen known bisnor- and norditerpenoids, and the structures of those n...

journal_title：Chemical & pharmaceutical bulletin

authors： Sato K,Inaba Y,Park HS,Akiyama T,Koyama T,Fukaya H,Aoyagi Y,Takeya K

更新日期：2009-07-01 00:00:00

abstract：:The tumor microenvironment is considered as one of the important targets for anticancer drug discovery. In particular, nutrient deficiency may be observed in tumor microenvironment; biakamides A-D (1-4) isolated from marine sponge Petrosaspongia sp. as growth inhibitors against cancer cells adapted to glucose-deprived...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida R,Matsumoto H,Ichii S,Kobayashi M,Arai M,Kotoku N

更新日期：2019-03-01 00:00:00

abstract：:We investigated the kinetics of in vitro transformation of a dichlorinated propyl paraben (2-propyl 3,5-dichloro-4-hydroxybenzoate; Cl2PP) by the rat liver S9 fraction and assessed the aryl hydrocarbon receptor (AhR) agonist activity of the metabolite products identified in HPLC and GC/MS analysis and by metabolite sy...

journal_title：Chemical & pharmaceutical bulletin

authors： Terasaki M,Wada T,Nagashima S,Makino M,Yasukawa H

更新日期：2016-01-01 00:00:00

abstract：:We investigated the distribution and stability of pirarubicin in human blood obtained from 12 healthy volunteers. The distribution of pirarubicin into blood cells showed marked temperature- and concentration-dependencies and the Arrhenius plot for pirarubicin uptake in blood was biphasic. Therefore, pirarubicin appear...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagasawa K,Kitada N,Tsuji C,Ogawa M,Yokoyama T,Ohnishi N,Iwakawa S,Okumura K

更新日期：1992-10-01 00:00:00

abstract：:A new monomethylated ganglioside, DSG-A (3), was obtained, together with four known gangliosides, compounds (1, 2, 4, 5), from the lipid fraction of the chloroform/methanol extract of the ovary of the sea urchin Diadema setosum. The structures of the new ganglioside was determined on the basis of chemical and spectros...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada K,Tanabe K,Miyamoto T,Kusumoto T,Inagaki M,Higuchi R

更新日期：2008-05-01 00:00:00

abstract：:Four new diterpenes, 3-oxosaprorthoquinone (1), 3-oxomicrostegiol (2), 3-oxoisotaxodione (3), and taiwaninal (4), together with two known compounds, 3-oxosapriparaquinone (5) and 6-dehydrohinokiol (6), were isolated from the roots of Taiwania cryptomerioides. The structures of 1-4 were principle elucidated based on sp...

journal_title：Chemical & pharmaceutical bulletin

authors： Chyu CF,Lin HC,Kuo YH

更新日期：2005-01-01 00:00:00

abstract：:From the leaves of Cananga odorata var. odorata, three relatively large molecules, namely two aryl naphthalene lignan diesters of canangafruticoside A and one cyclobutane lignan diester of canangafruticoside A, were isolated along with four known compounds. The structures of the new compounds were elucidated based on ...

journal_title：Chemical & pharmaceutical bulletin

authors： Katsui H,Sugimoto S,Matsunami K,Otsuka H,Lhieochaiphant S

更新日期：2017-01-01 00:00:00