New iridoids from Gelsemium species.

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：:Anhydrous theophylline was prepared by heating theophylline monohydrate at temperatures between 60 degrees C and 140 degrees C. The effects of dehydration temperatures on the moisture absorption and dissolution behavior of anhydrous theophylline were investigated in this study. The hydration rate of anhydrous theophyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2001-12-01 00:00:00

abstract：:Peptides mimicking chemokine receptor CCR5 were synthesized and their anti-HIV-1 activities evaluated. Prepared compounds, especially a sulfated derivatives, showed significant anti-HIV-1 activities. Furthermore, a hybrid molecule linked to an N-carbomethoxycarbonyl-prolyl-phenylalanine (CPF) moiety had a greater effe...

journal_title：Chemical & pharmaceutical bulletin

authors： Konishi K,Ikeda K,Achiwa K,Hoshino H,Tanaka K

更新日期：2000-02-01 00:00:00

abstract：:The object of this study was to develop hydroxypropyl methylcellulose (HPMC) based cephalexin extended release tablet, which can release the drug for six hours in predetermined rate. Twenty-one batches of cephalexin tablets were prepared by changing various physical and chemical parameters, in order to get required th...

journal_title：Chemical & pharmaceutical bulletin

authors： Saravanan M,Sri Nataraj K,Ganesh KS

更新日期：2003-08-01 00:00:00

abstract：:A series of 1,2,3,4-tetrahydroisoquinoline derivatives containing the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton were prepared and evaluated for their in vitro binding affinities to muscarinic receptors and for antagonism of bradycardia in vivo. Among them, compound 3f had the highest affinity for ...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe T,Kinoyama I,Takizawa K,Hirano S,Shibanuma T

更新日期：1999-05-01 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：: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：:Three new anthraquinone glycosides, lasianthuoside A (1), B (2), and C (3), were isolated from the root of Lasianthus acuminatissimus MERR., The structural elucidation of these anthraquinones was mainly established on the basis of 1D and 2D NMR and HR-MS spectroscopic analysis. Ten known compounds, damnacanthol (4), d...

journal_title：Chemical & pharmaceutical bulletin

authors： Li B,Zhang DM,Luo YM,Chen XG

更新日期：2006-03-01 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：:The inhibitory effects of pure galloylglucose (1,2,3,4,6-penta-O-galloyl-beta-D-glucose) on the respiratory chain of rat liver mitochondria were investigated. The respiratory control ratio (RCR) decreased by 50% on addition of 20 microM pentagalloylglucose to highly coupled mitochondria, but the adenosine-5'-diphospha...

journal_title：Chemical & pharmaceutical bulletin

authors： Adachi H,Konishi K,Horikoshi I

更新日期：1989-05-01 00:00:00

abstract：:A high-performance liquid chromatographic method involving postcolumn fluorescence derivatization is described for the quantification of five fragment peptides (methionine-enkephalin-Thr-Ser-Glu-Lys, methionine-enkephalin-Lys, methionine-enkephalin-Arg, leucine-enkephalin-Lys and leucine-enkephalin-Arg) released by tr...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang GQ,Kai M,Ohkura Y

更新日期：1991-09-01 00:00:00

abstract：:The effect of the modification of insulin (INS) with p-succinylamidophenyl (SA)-alpha-D-glucopyranoside (SAPG), SA-alpha-D-mannopyranoside and SA-alpha-L-arabinopyranoside on the enzymatic degradation and the hypoglycemic effect in rats was studied. When SAPG-INS was administered intraintestinally in the absence of bi...

journal_title：Chemical & pharmaceutical bulletin

authors： Haga M,Saito K,Shimaya T,Maezawa Y,Kato Y,Kim SW

更新日期：1990-07-01 00:00:00

abstract：:Enantiomerically pure (1S,3S)- and (1S,3R)-1-amino-3-(hydroxymethyl)cyclopentanes have been efficiently synthesized from L-aspartic acid. The title compounds are isosteres of ribose and may be used to construct nucleoside analogs with important antiviral and antineoplastic activities as demonstrated by a concise total...

journal_title：Chemical & pharmaceutical bulletin

authors： Rapoport H,Chen Y,Mohareb RM,Ahn JH,Sim TB,Ho JZ

更新日期：2003-10-01 00:00:00

abstract：:In the course of our search for bioactive metabolites from marine organisms, new hexylitaconic acid derivatives (1-4), along with (3S)-hexylitaconic acid (5), were isolated from a sponge-derived fungus Penicillium sp. Based on the NMR and MS data, the structures of compounds 1-4 were defined as α,β-dicarboxylic acid d...

journal_title：Chemical & pharmaceutical bulletin

authors： Li JL,Zhang P,Lee YM,Hong J,Yoo ES,Bae KS,Jung JH

更新日期：2011-01-01 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：:A major lysosomal membrane glycoprotein (LGP107) which has an apparent molecular weight (Mr) of 107 kilodaltons (kDa) was purified from rat liver by a simple method with a yield of 1 mg/87 g wet weight of liver. The purification procedures include; preparation of tritosomal membranes of triton-filled lysosomes (tritos...

journal_title：Chemical & pharmaceutical bulletin

authors： Akasaki K,Yamaguchi Y,Ohta M,Matsuura F,Furuno K,Tsuji H

更新日期：1990-10-01 00:00:00

abstract：:Nitroxyl (HNO), a one-electron-reduced form of nitric oxide, has various biological activities, including a cardioprotective effect. Here, we first synthesized another, more hydrophilic photocontrollable HNO donor (3), which can release HNO in a spatially and temporally controlled manner, and then examined the propert...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuo K,Nakagawa H,Adachi Y,Kameda E,Aizawa K,Tsumoto H,Suzuki T,Miyata N

更新日期：2012-01-01 00:00:00

abstract：:In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) value...

journal_title：Chemical & pharmaceutical bulletin

authors： Pinna GA,Loriga G,Murineddu G,Grella G,Mura M,Vargiu L,Murgioni C,La Colla P

更新日期：2001-11-01 00:00:00

abstract：:Applicability of a previously published equation for calculating the solubility of solutes in supercritical carbon dioxide was extended to calculate the solubility in entrained supercritical carbon dioxide employing 42 experimental data sets collected from the literature. The accuracy of the proposed model was evaluat...

journal_title：Chemical & pharmaceutical bulletin

authors： Jouyban A,Khoubnasabjafari M,Chan HK

更新日期：2005-03-01 00:00:00

abstract：:We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Hirono S

更新日期：2019-01-01 00:00:00

abstract：:The stereoselective introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one was accomplished using Birch reduction and an enolate trapping reaction. It was determined that the allyl group was introduced via an unexpected conformation-flipped from the initi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hiroya K,Takahashi T,Shimomae K,Sakamoto T

更新日期：2005-02-01 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：:A highly sensitive spectrophotometric determination of human serum albumin (HSA) with 3',4',5',6'-tetrachlorogallein (T.Cl.Gall)-Mo(VI) complex in a Triton X-100 + polyvinyl alcohol micellar medium is proposed. This method can be used to determine up to ca. 150 micrograms/10 ml of HSA from the optical absorbance at 64...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujita Y,Mori I,Ikuta K,Nakahashi Y,Kato K,Nakanishi T

更新日期：1989-09-01 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：:The n-BuOH extract of Swertia japonica showed a significant hepatoprotective effect on D-galactosamine (D-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice. The activity-guided fractionation led to the isolation of a new tetrahydroxanthone derivative, tetrahydroswertianolin (1), as well as two known iridoids...

journal_title：Chemical & pharmaceutical bulletin

authors： Hase K,Li J,Basnet P,Xiong Q,Takamura S,Namba T,Kadota S

更新日期：1997-11-01 00:00:00

abstract：:Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developed a synthesis based on the photocyclization of tertiary ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aragon PJ,Yapi AD,Pinguet F,Chezal JM,Teulade JC,Blache Y

更新日期：2007-09-01 00:00:00

abstract：:A novel in-die evaluation method of tablet capping tendency was proposed based on a force-displacement curve and stress relaxation parameter in a tableting process. In our previous study (Chem. Pharm. Bull., 59, 2011, Nakamura et al.), the phase diagram consisting of elastic recovery energy (E(e)) and plastic deformat...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura H,Sugino Y,Watano S

更新日期：2012-01-01 00:00:00

abstract：:We have developed a novel organometallic catalysis and applied it to drug discovery. Two new catalysts were found, ruthenium hydride with a nitrogen-containing heterocyclic carbene (A) and an organopalladium catalyst supported on a sulfur-terminated semiconductor, gallium arsenide (001) (B). Both catalysts are environ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arisawa M

更新日期：2007-08-01 00:00:00

abstract：:Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as ...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee Y,Thapa P,Jeong SH,Woo MH,Choi DH

更新日期：2017-02-01 00:00:00

abstract：:Several benzimidazole derivatives having electron-withdrawing or -donating substituent(s) at the benzene moiety were used as models of the imidazole moiety of purine bases and their nitration with nitrogen dioxide and ozone (so-called Kyodai nitration) were examined. Products were extracted from the reaction mixture w...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaiya T,Nakamura K,Tanaka M,Miyata N,Kohda K

更新日期：2004-05-01 00:00:00