A novel method for estimation of transition temperature for polymorphic pairs in pharmaceuticals using heat of solution and solubility data.

abstract：:A simple method to synthesize (+/-)-2-O-(4-coumaroyl)-3-(4-hydroxyphenyl)lactic acid (1), a key intermediate in rosmarinic acid biosynthesis in higher plant cells, was established by condensation of protected 4-coumaric acid and (+/-)-3-(4-hydroxyphenyl)lactic acid followed by deprotection. A stable supply of 1 thus a...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuno M,Nagatsu A,Ogihara Y,Mizukami H

更新日期：2001-12-01 00:00:00

abstract：:To develop non-prodrugs of taxoids with satisfactory stability in vivo, high water-solubility, and potent antitumor activity, we prepared several 10-O-sec-aminoethyl docetaxel analogs (3) and evaluated their cytotoxicity against mouse leukemia and human tumor cell lines, microtubule disassembly-inhibitory activity, an...

journal_title：Chemical & pharmaceutical bulletin

authors： Uoto K,Takenoshita H,Yoshino T,Hirota Y,Ando S,Mitsui I,Terasawa H,Soga T

更新日期：1998-05-01 00:00:00

abstract：:Stereoisomers of thiol proteinase inhibitor (TPI) were synthesized by a conventional solution method. Among them, iNoc-D-Gln-Val-Val-Ala-Ala-pNA weakly inhibited the amidolytic activity of papain, although iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited papain activity fairly potently. However, the other five D-amino acid-cont...

journal_title：Chemical & pharmaceutical bulletin

authors： Iguchi S,Hirano K,Okamoto H,Okamoto Y,Okada Y

更新日期：1996-08-01 00:00:00

abstract：:The tandem action of serine protease (alpha-chymotrypsin or subtilisin BPN') and Aspergillus genus aminoacylase on racemic N-acetyl-alpha-aminoalkanedioic acid alpha,omega-diester produced L-alpha-aminoalkanedioic acid omega-ester in good yield and high optical purity. L-alpha-Aminosuberic acid omega-ester thus obtain...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishino N,Arai T,Ueno Y,Ohba M

更新日期：1996-01-01 00:00:00

abstract：:Self Microemulsifying Drug Delivery Systems (SMEDDS) are a novel alternative to the conventional transdermal delivery systems. SMEDDS are water-free systems, made up of oils and surfactants that can readily form a microemulsion upon dilution within an aqueous medium. Before SMEDDS can be used as a drug delivery system...

journal_title：Chemical & pharmaceutical bulletin

authors： Zargar-Shoshtari S,Wen J,Alany RG

更新日期：2010-10-01 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：:The structures of new neo-lignans, isoamericanol A (1) and americanol A (2) isolated from the seeds of Phytolacca americana have been elucidated on the basis of spectroscopic data and then confirmed by chemical correlation with the previously known isoamericanin A (3) and americanin A (4). Isoamericanol A, americanol ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Hasegawa T,Toda M,Kodama M,Okazaki H

更新日期：1992-01-01 00:00:00

abstract：:The effect of chromomycin A3 binding on the geometry of DNA duplex (plasmid pBR322) has been examined using topoisomerase I relaxation followed by gel electrophoresis. To determine the equilibrium constant of this drug-DNA binding-dissociation reaction in the same concentration range (ca. 10(-5) M) in the same buffer ...

journal_title：Chemical & pharmaceutical bulletin

authors： Utsuno K,Kojima K,Maeda Y,Tsuboi M

更新日期：1998-11-01 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：:A novel series of N-arylpiperazine-1-carboxamide derivatives was synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Reporter assays indicated that trans-2,5-dimethylpiperazine derivatives are potent AR antagonists, and in this series trans-N-4-[4-cy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kinoyama I,Taniguchi N,Kawaminami E,Nozawa E,Koutoku H,Furutani T,Kudoh M,Okada M

更新日期：2005-04-01 00:00:00

abstract：:Analogues with the scaffolds of 3-cyano-4-alkoxyphenyl-6-bromoaryl-2-pyridone and 2-amino-3-cyano-4-alkoxyphenyl-6-bromoarylpyridine were synthesized. Cyclization of the 2-amino derivatives with formic acid and formamide gave the corresponding pyrido[2,3-d]pyrimidin-4(3H)-one and the pyrido[2,3-d]-pyrimidin-4-amine de...

journal_title：Chemical & pharmaceutical bulletin

authors： Abadi AH,Hany MS,Elsharif SA,Eissa AA,Gary BD,Tinsley HN,Piazza GA

更新日期：2013-01-01 00:00:00

abstract：:The purpose of this study was to predict the stability of imipenem in a mixed infusion. The hydrolysis of imipenem in aqueous solution was found to be accelerated by pH, and by increasing concentrations of sodium bisulfite (SBS) and L-cysteine. Equations were derived for the degradation rate constants (k(obs)) of pH, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Takasu Y,Shimizu K,Asahara K,Uchida T

更新日期：2013-01-01 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：:To understand more fully the effect of polyunsaturated fatty acids (PUFAs) on lipid bilayers, we investigated the effects of treatment with fatty acids on the properties of a model membrane. Three kinds of liposomes comprising dipalmitoylphosphatidylcholine (DPPC), dioleylphosphatidylcholine (DOPC), and cholesterol (C...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Hagiwara C,Sugibayashi K,Takayama K

更新日期：2008-08-01 00:00:00

abstract：:Licorice is one of the ancient and most frequently applied herbs for its diverse phytochemicals. At present, wild resources of licorice have rapidly declined with increasing demand and the proportion of cultivated products in the market is quickly growing. However, the different level in chemical composition between t...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang C,Cai Z,Shi J,Chen S,Tan M,Chen J,Chen L,Zou L,Chen C,Liu Z,Liu X

更新日期：2019-01-01 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：:A new dihydrobenzofuran neolignan, herpepropenal, was isolated from the seeds of Herpetospermum caudigerum. Its chemical structure was established based on spectroscopic analysis. In this work, the inhibitory effects of herpepropenal on hepatitis B virus DNA and on the replication and expression of hepatitis B surface...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang F,Zhang HJ,Zhang YY,Chen WS,Yuan HL,Lin HW

更新日期：2010-03-01 00:00:00

abstract：:Novel saponins that retain a free carboxyl group at the C-17 position and various sugars linked at the C-3 position of hederagenin aglycone were synthesized via stereospecific glycosylation. Since these natural products represented by Pulsatilla saponin D (PSD) were obtained in very small amounts, the total synthesis ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim M,Park Y,Chung WY,Park KK,Jung M

更新日期：2015-01-01 00:00:00

abstract：:The effects of various chelating agents, sodium N-benzyl-D-glucamine dithiocarbamate (BGD), sodium N-p-methylbenzyl-D-glucamine dithiocarbamate (MBGD), sodium N-p-hydroxymethylbenzyl-D-glucamine dithiocarbamate (HBGD), and N-p-carboxybenzyl-D-glucamine dithiocarbamate (CBGD), which were newly synthesized, and sodium N...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimada H,Kiyozumi M,Kawagoe M,Fukudome S,Kojima S

更新日期：1990-03-01 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：:Values of inhibition constants, Ki, and concentrations required for 50% inhibition, IC50, for a collection of structurally diverse competitive inhibitors of calf spleen purine nucleoside phosphorylase have been determined employing inosine as substrate. These values have been employed to create predictive quantitative...

journal_title：Chemical & pharmaceutical bulletin

authors： Andricopulo AD,Yunes RA

更新日期：2001-01-01 00:00:00

abstract：:Stomatitis induced by radiation therapy or cancer chemotherapy is a factor in sleep disorders and/or eating disorders, markedly decreasing patient quality of life. In recent years, disintegrating oral films that are easy to handle have been developed; therefore, we focused on the formulation of these films. We prepare...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawano Y,Sasatsu M,Mizutani A,Hirose K,Hanawa T,Onishi H

更新日期：2016-06-01 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：:A new gluco indole alkaloid, 3,4-dehydro-5-carboxystrictosidine, was obtained from Peruvian Uña de Gato (Cat's Claw, original plant: Uncaria tomentosa) together with two known gluco indole alkaloids. This compound was the first example of isolation of a gluco monoterpenoid indole alkaloid having a 3,4-dihydro-beta-car...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima M,Hashimoto K,Yokoya M,Takayama H,Aimi N,Sakai SI

更新日期：2000-10-01 00:00:00

abstract：:Three new cardiac glycosides named cheiranthoside VIII (1), cheiranthoside IX (2) and cheiranthoside X (3) were isolated from the seeds of Erysimum cheiranthoides. Based on spectroscopic data, the structures of 1-3 were characterized as strophanthidin 3-O-beta-D-glucopyranosyl-(1-->4)-beta-D-antiaropyranoside, cheiran...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei ZH,Nakayama H,Kuniyasu A,Tai BS,Nohara T

更新日期：2002-06-01 00:00:00

abstract：:The compound tentatively named TL-1 was isolated from Talaromyces luteus as a metabolite having monoamine oxidase (MAO) inhibitory potency. TL-1 showed mixed-type inhibition of MAO in mouse liver when kynuramine was used as a substrate, and the IC50 was 6.6 microM. The inhibition constants (Ki) for MAO-A and -B in mou...

journal_title：Chemical & pharmaceutical bulletin

authors： Satoh Y,Yamazaki M

更新日期：1989-01-01 00:00:00

abstract：:A new spiroketallactone, epi-danshenspiroketallactone A (1) and a new C18-norditerpenoid, normiltioane (2) along with 21 known compounds, were isolated from cell cultures of Salvia miltiorrhiza. Their structures were elucidated on the basis of extensive spectroscopic analyses. In the in vitro assays, the compounds 9-1...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang DW,Liu X,Xie D,Chen R,Tao XY,Zou JH,Dai J

更新日期：2013-01-01 00:00:00

abstract：:We synthesize optically active (R)-terbutaline 2, which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of...

journal_title：Chemical & pharmaceutical bulletin

authors： Uchimoto H,Ikeda M,Tanida S,Ohhashi K,Chihara Y,Shigeta T,Arimitsu K,Yamashita M,Nishide K,Kawasaki I

更新日期：2017-01-01 00:00:00

abstract：:The MeOH extract of the stem barks of Drypetes tessmanniana (Euphorbiaceae) afforded two new triterpene derivatives characterized as 3beta-O-(E)-3,5-dihydroxycinnamoyl-11-oxo-olean-12-ene and 3beta,6alpha-dihydroxylup-20(29)-ene together with seven known compounds. Their structures were established on the basis of spe...

journal_title：Chemical & pharmaceutical bulletin

authors： Dongfack MD,Van-Dufat HT,Lallemand MC,Wansi JD,Seguin E,Tillequin F,Wandji J

更新日期：2008-09-01 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