New 5-HT3 (serotonin-3) receptor antagonists. IV. Synthesis and structure-activity relationships of azabicycloalkaneacetamide derivatives.

abstract：:H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OMe, corresponding to the sequence 41-49 of eglin c, inhibited human leukocyte cathepsin G and alpha-chymotrypsin. In order to gain further insight into the relationship between the structure and the inhibitory activity against cathepsin G and alpha-chymotrypsin, peptide fragments...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakabayashi K,Tsuboi S,Fujimoto T,Okada Y,Nagamatsu Y,Yamamoto J

更新日期：1990-12-01 00:00:00

abstract：:The complexations of sulfasalazine (H3Suz) with some of transition metals have been investigated. Three types of complexes, [Mn(HSuz)-2(H2O)4] x 2H2O, [M(HSuz)-2(H2O)2] x xH2O (M=Hg(II), ZrO(II) and VO(II), x=4, 8 and 6, respectively) and [M(HSuz)-2(Cl)(H2O)3] x xH2O (M=Cr(III) and Y(III), x=5 and 6, respectively) wer...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Wahed MG,Refat MS,El-Megharbel SM

更新日期：2008-11-01 00:00:00

abstract：:Polymorphic behaviours of paracetamol and propyphenazone and interaction between these two compounds were investigated using differential scanning calorimetry (DSC), X-ray powder diffraction and Fourier transform-infrared (FT-IR)-spectroscopy. Binary mixtures containing various ratios of the compounds were prepared as...

journal_title：Chemical & pharmaceutical bulletin

authors： Zalac S,Khan MZ,Gabelica V,Tudja M,Mestrović E,Romih M

更新日期：1999-03-01 00:00:00

abstract：:Dryocrassyl formate, sitostanyl formate, and 12alpha-hydroxyfern-9(11)-ene were isolated from the fresh fronds of Cyathea podophylla. Their structures were elucidated by spectroscopic techniques and synthesis. Ten known triterpenoids, three derivatives of phytol, a stanol, and beta-tocopherol were also identified from...

journal_title：Chemical & pharmaceutical bulletin

authors： Arai Y,Hattori T,Hamaguchi N,Masuda K,Takano A,Shiojima K

更新日期：2003-11-01 00:00:00

abstract：:A new synthetic method for chiral oxazolidinone derivatives, therapeutic agents for treating urinary disturbance, is described. The condensed compound obtained from chiral 1-amino-3-phenyl-2-propanol and 1-phenyl-3-morpholino-1-propanone was reduced with Me4NBH(OAc)3 to give the intermediate, 1-(3-morpholino-1-phenylp...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida S,Yamamoto M,Mochizuki N,Nohira H

更新日期：1999-08-01 00:00:00

abstract：:Five new compounds, hibicuslide A (1), hibicuslide B (2), hibicuslide C (3), hibicutaiwanin (4), hibicusin (5), and fifty-one known compounds have been isolated from the stems of Hibiscus taiwanensis. The structures of these compounds were determined by spectroscopic and chemical transformation methods. Among them, ma...

journal_title：Chemical & pharmaceutical bulletin

authors： Wu PL,Wu TS,He CX,Su CH,Lee KH

更新日期：2005-01-01 00:00:00

abstract：:Water-soluble porphyrins containing four platinum(II) complexes per molecule, [5alpha,10beta,15alpha,20beta-tetrakis(2-trans-(alpha,beta,alpha,beta-trans-Pt) and cis-(alpha,beta,alpha,beta-cis-Pt) [PtCl(NH(3))(2)]N-2-aminophenylporphyrin)], were synthesized and characterized. The binding of synthetic nucleotide polyme...

journal_title：Chemical & pharmaceutical bulletin

authors： Munakata H,Imai H,Nakagawa S,Osada A,Uemori Y

更新日期：2003-05-01 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：:(±)-8-Deisopropyladunctin B, the deisopropyl form of adunctin B, which was isolated from the leaves of Piper aduncum (Piperaceae) collected in Papua New Guinea, was synthesized in 0.77% overall yield in 17 steps from 5,7-dimethoxycoumarin-3-carboxylate. The key step was our original stereoconvergent skeleton transform...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomura S,Arimitsu K,Yamaguchi S,Kosuga Y,Kakimoto Y,Komai T,Hasegawa K,Nakanishi A,Miyoshi T,Iwasaki H,Ozeki M,Kawasaki I,Kurume A,Ohta S,Yamashita M

更新日期：2012-01-01 00:00:00

abstract：:The purpose of the present study was the quantitative prediction of the bitterness-suppressing effect of sweeteners (sucrose or sugar alcohols) on the bitterness of famotidine (or quinine sulfate as control) solutions using an artificial taste sensor. Firstly, we examined the response characteristics of the sensor res...

journal_title：Chemical & pharmaceutical bulletin

authors： Hashimoto Y,Matsunaga C,Tokuyama E,Tsuji E,Uchida T,Okada H

更新日期：2007-05-01 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：:The phosphorylation of several D-glucose derivatives has been achieved using inorganic sodium cyclo-triphosphate hexahydrate (P3m), Na3P3O9 x 6H2O, in aqueous solution. In the phosphorylation of D-glucuronic acid, 6-phosphoryl-D-glucose and D-xylose, beta-D-glucuronic acid 1-triphosphate, 6-phosphoryl-beta-D-glucose 1...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue H,Watanabe M,Nakayama H,Tsuhako M

更新日期：2000-06-01 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：:Soluble (SSG, beta-1,3-D-glucan obtained from the culture filtrates of a fungus, Sclerotinia sclerotiorum IFO 9395) and particulate (zymosan) beta-glucans were oxidized by sodium hypochlorite (NaClO), and the oxidized products were analyzed by gel filtration and ion-exchange chromatographies and by limulus G-test to s...

journal_title：Chemical & pharmaceutical bulletin

authors： Miura NN,Ohno N,Adachi Y,Yadomae T

更新日期：1996-11-01 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：:Present studies were undertaken on the preparation of synthetic analogues of bis- or tetra-coumarins and their activity against HIV-1 integrase (HIV-1 IN). Among these coumarin analogues, compounds 14, 16 and 18 were found to be potent molecules against HIV-1 IN at IC50 values of 0.96, 0.58, and 0.49 microM, respectiv...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiang CC,Mouscadet JF,Tsai HJ,Liu CT,Hsu LY

更新日期：2007-12-01 00:00:00

abstract：:The production of sesquiterpene-type phytoalexins with a vetispyradiene skeleton by Hyoscyamus albus hairy roots induced by methyl jasmonate (MeJA) was reported in a previous paper. The production pattern on co-treatment with cupper sulfate and MeJA (CuSO(4)-MeJA) showed a TLC profile differing from that on treatment ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawauchi M,Arima T,Shirota O,Sekita S,Nakane T,Takase Y,Kuroyanagi M

更新日期：2010-07-01 00:00:00

abstract：:A new series of 3-(5-3-methyl-5-[(3-methyl-7-5-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-1,3,4-thiadiazol-2-ylbenzo[b]furan-5-yl)methyl]benzo[b]furan-7-yl-1,3,4-thiadiazol-2-yl)-2-(aryl)-1,3-thiazolan-4-one 5a-j has been synthesized by the reaction of N2-[(E)-1-(4-methylphenyl)methylidene]-5-(3-methyl-5-[3-methyl-7-(5-[(E)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Reddy CS,Rao DC,Yakub V,Nagaraj A

更新日期：2010-06-01 00:00:00

abstract：:The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Sev...

journal_title：Chemical & pharmaceutical bulletin

authors： Ha ES,Baek IH,Cho W,Hwang SJ,Kim MS

更新日期：2014-01-01 00:00:00

abstract：:Jellies for oral administration are dosage forms that contain water, as stipulated in the Japanese Pharmacopeia, and heat is generally applied to the jellies during the manufacturing process. Therefore, it is difficult to formulate drugs that may be affected adversely by water and/or heat. To solve this problem, we tr...

journal_title：Chemical & pharmaceutical bulletin

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

更新日期：2017-01-01 00:00:00

abstract：:In continuation of our efforts to discover novel nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) as potentially "Safe NSAIDs," we report herein the design, synthesis and evaluation of 21 new NO-NSAIDs of commonly used NSAIDs such as aspirin, diclofenac, naproxen, flurbiprofen, ketoprofen, suli...

journal_title：Chemical & pharmaceutical bulletin

authors： Borhade N,Pathan AR,Halder S,Karwa M,Dhiman M,Pamidiboina V,Gund M,Deshattiwar JJ,Mali SV,Deshmukh NJ,Senthilkumar SP,Gaikwad P,Tipparam SG,Mudgal J,Dutta MC,Burhan AU,Thakre G,Sharma A,Deshpande S,Desai DC,Dubash

更新日期：2012-01-01 00:00:00

abstract：:Five new components, named multiforisins A, B, C, D, and E, with immunosuppressive activity were isolated from an Ascomycete, Gelasinospora multiforis. Multiforisin A, the main immunosuppressive principle of this fungus, was deduced to be 5-formyl-3-(hydroxymethyl)-4-methoxy-6-(1E-propenyl)-alpha-pyrone. Multiforisins...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujimoto H,Satoh Y,Nakayama M,Takayama T,Yamazaki M

更新日期：1995-04-01 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 hypoglycemic component, elatoside E, was isolated from the root cortex of Aralia elata SEEM. (Araliaceae) together with elatoside F and eight known oleanolic acid glycosides, elatosides A and C, oleanolic acid 3-O-[alpha-L-arabinofuranosyl (1-->4)]-beta-D-glucopyranosiduronic acid, oleanolic acid 3-O-beta-D-glucop...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Murakami T,Harada E,Murakami N,Yamahara J,Matsuda H

更新日期：1996-10-01 00:00:00

abstract：:The binding of carprofen (CP) to human serum albumin (HSA) and bovine serum albumin (BSA) was compared using equilibrium dialysis method. The affinity of CP for the primary binding site was BSA > HSA. However, the number of primary binding sites (n1) was 1.94 on HSA, considerably greater than that on BSA (0.79). The d...

journal_title：Chemical & pharmaceutical bulletin

authors： Kohita H,Matsushita Y,Moriguchi I

更新日期：1994-04-01 00:00:00

abstract：:Recently, active pharmaceutical ingredients (APIs) have been dramatically expanding from low-molecular weight drugs to peptides, proteins, antibodies, genes, oligonucleotides, cells, and machines. Therefore to develop pharmaceutical technologies and drug delivery systems (DDS) for these APIs, advanced molecules and no...

journal_title：Chemical & pharmaceutical bulletin

authors： Higashi T

更新日期：2019-01-01 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：:A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PA...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki H,Ogiku T,Sai H,Moritani Y,Ohtani A,Ohmizu H

更新日期：2009-09-01 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：:A new sesquiterpene 2,9-humuladien-6-ol-8-one (1) was isolated from methanol extract of Zingiber aromaticum, along with 15 known compounds. The structures of the isolated compounds were elucidated on the basis of spectroscopic analyses. The isolated compounds were tested for their inhibitory activity on the metabolism...

journal_title：Chemical & pharmaceutical bulletin

authors： Subehan,Usia T,Kadota S,Tezuka Y

更新日期：2005-03-01 00:00:00