Further metabolism of 3,5-di-tert-butyl-4-hydroxybenzoic acid, a major metabolite of butylated hydroxytoluene, in rats.

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：:A quantitative structure property relationship (QSPR) study was performed to develop a model that relates the structures of 150 drug organic compounds to their aqueous solubility (log S(w)). Molecular descriptors derived solely from 3D structure were used to represent molecular structures. A subset of the calculated d...

journal_title：Chemical & pharmaceutical bulletin

authors： Ghasemi J,Saaidpour S

更新日期：2007-04-01 00:00:00

abstract：:A novel crystalline Zn(II) complex of L-carnosine was prepared and evaluated for inhibitory activity against gastric ulceration in rats. The complex was found to be much more active than various other Zn(II) compounds. It was characterized by means of infrared (IR) spectroscopy, solid-state carbon-13 (13C) and nitroge...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsukura T,Takahashi T,Nishimura Y,Ohtani T,Sawada M,Shibata K

更新日期：1990-11-01 00:00:00

abstract：:We synthesized the racemates of the five presumed metabolites (1b-f) of (S)-(--)-N-tert-butyl-4,4-diphenyl-2-cyclopentenylamine hydrochloride (FK584, S(--)-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate their inhibitory a...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi K,Miyao Y,Yamano K,Yamamoto T,Terai T,Kusunoki T,Tsubaki K,Shiokawa Y

更新日期：1996-06-01 00:00:00

abstract：:An efficient one-pot step by step t-BuOK-mediated procedure for the synthesis of N-arylindoles has been developed in moderate to good yields. The protocol involves the consecutive deprotection of N-arylsulfonylindoles as latent indoles and subsequent S(N)Ar reactions with activated aryl halides. This tandem reaction a...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu H,Fan LL

更新日期：2009-03-01 00:00:00

abstract：:Synthesis and pharmacological evaluation of novel thienopyridazinones and related compounds are described. A thiophene ring was found to be able to replace the benzene ring of a phthalazinone without loss of biological activities. This observation supports our hypothesis that the benzene ring plays an important role i...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Maruyama N,Koga T,Kamei K,Akima M,Kuroki T,Hamana M,Ohi N

更新日期：1995-02-01 00:00:00

abstract：:Glycyrrhetinic acid (Ia) and eighteen related derivatives were examined for antiulcer activity using stress-induced gastric lesions (restraint plus water immersion at 25 degrees C) in mice and rats as screening tests. Among the compounds tested, dihemiphthalate derivatives of 18 alpha- or 18 beta-olean-12-ene-3 beta,3...

journal_title：Chemical & pharmaceutical bulletin

authors： Yano S,Harada M,Watanabe K,Nakamaru K,Hatakeyama Y,Shibata S,Takahashi K,Mori T,Hirabayashi K,Takeda M

更新日期：1989-09-01 00:00:00

abstract：:A series of 7-substituted-6-fluoro-1-fluoromethyl-4-oxo-4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives (2a-1) was prepared and evaluated for antibacterial activity. These compounds were obtained by deacylation of 4-benzoyloxy-2-(1-chloro-2-fluoroethyl)thio-6,7- difluoroquinoline-3-carboxylate (10) and...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuoka M,Segawa J,Amimoto I,Masui Y,Tomii Y,Kitano M,Kise M

更新日期：1999-12-01 00:00:00

abstract：:One new guaiane-type sesquiterpene glycoside, 2'-O-E-caffeoyl-8alpha-hydroxy-11alpha,13-dihydro-3beta-O-beta-D-glucozaluzanin C (1), was isolated from the whole herb of Ainsliaea fragrans (Compositae), together with five known sesquiterpene lactones: 8alpha-hydroxy-11alpha,13-dihydro-3beta-O-beta-D-glucozaluzanin C (2...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang H,Wu T,Yan M,Liu G,Li P,Zhang XQ,Ye WC,Zhang LY

更新日期：2009-06-01 00:00:00

abstract：:The reaction of the N-furfuryloxamic acid sodium salt (12) with 1,1'-oxalyldiimidazole (ODI) yielded the imidazolide (13) as an intermediate, and this directly reacted with 2-aminothiazole derivatives (14) or 2-aminobenzothiazole derivatives (15) under essentially neutral conditions to afford the N'-12-(substituted th...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa T,Tsutsui C

更新日期：2000-09-01 00:00:00

abstract：:Two new lignans, pseuderesinol (1), pseuderanoside (2) and a new triterpene, pseuderanic acid (3) were isolated from the dried root of Pseuderanthemum carruthersii (SEEM.) GUILL. var. atropurpureum (BULL.) FOSB. (Acanthaceae), together with ten known compounds, including five lignans, (+)-eudesmin (4), (+)-magnolin (5...

journal_title：Chemical & pharmaceutical bulletin

authors： Vo TN,Nguyen PL,Tuong LT,Pratt LM,Vo PN,Nguyen KP,Nguyen NS

更新日期：2012-01-01 00:00:00

abstract：:Polypropyleneglycol (PPG) was used as a dispersion medium for the preparation of microspheres (MS) consisting of starch, gelatin, whey protein or dextran. Aqueous solutions of the polymers were dispersed in PPG at various initial temperatures and then the systems were cooled to 0.5 degrees C to allow water in the disp...

journal_title：Chemical & pharmaceutical bulletin

authors： Seki T,Shinohara K,Kato N,Uchida M,Natsume H,Morimoto K,Juni K

更新日期：2007-03-01 00:00:00

abstract：:During the search for new antitrypanosomal drug leads, four antitrypanosomal compounds, of three depsipeptides and one nortriterpenoid, were isolated from cultures of the mutant strain IU-3 of the insect pathogenic fungus Ophiocordyceps coccidiicola NBRC 100683. Their structures were identified by the analysis of high...

journal_title：Chemical & pharmaceutical bulletin

authors： Ganaha M,Yoshii K,Ōtsuki Y,Iguchi M,Okamoto Y,Iseki K,Ban S,Ishiyama A,Hokari R,Iwatsuki M,Otoguro K,Ōmura S,Hashimoto T,Noji M,Umeyama A

更新日期：2016-01-01 00:00:00

abstract：:The analysis of genotoxic impurities (GTIs) in active pharmaceutical ingredients (APIs) is a challenging task. The target detection limit (DL) in an API is typically around 1 ppm (1 µg/g API). Therefore, a sensitive and selective analytical method is required for their analysis. 4-Chloro-1-butanol, an alkylating agent...

journal_title：Chemical & pharmaceutical bulletin

authors： Harigaya K,Yamada H,Yaku K,Nishi H,Haginaka J

更新日期：2014-01-01 00:00:00

abstract：:Arginine vasopressin (AVP) has a dual action mainly in the periphery, i.e., vasoconstriction and water reabsorption via V1A and V2 receptors; it may play a role in a number of diseases, including congestive heart failure (CHF), hypertension, renal disease, edema, and hyponatremia. We have attempted to develop a new se...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuhisa A,Taniguchi N,Koshio H,Yatsu T,Tanaka A

更新日期：2000-01-01 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：: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：:Our aim is to test the characteristics and expression activity in brain capillary endothelial cells (BCECs) of DNA-loaded nanoparticles before and after the modification with Antennapedia peptide (Antp). Chitosan (CH), polyethylenimine (PEI) and polyamidoamine (PAMAM) were chosen to prepare the nanoparticles; Lipofect...

journal_title：Chemical & pharmaceutical bulletin

authors： Huang R,Yang W,Jiang C,Pei Y

更新日期：2006-09-01 00:00:00

abstract：:An efficient synthesis of the antiviral and antioxidative chromene (1) was achieved. A small amount of chromene 1 could be derived from plastoquinones 2 and 3, the major constituents of the brown alga, Sargassum micracanthum. By the following synthetic scheme involving its application, many kinds of analogs can be syn...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori J,Iwashima M,Takeuchi M,Saito H

更新日期：2006-03-01 00:00:00

abstract：:Novel 9alpha and 9beta-hydroxy grayanotoxin II derivatives were prepared by photo-sensitized oxygenation of iso-grayanotoxin II and oxidation of grayanotoxin II tetraacetate with selenium dioxide respectively. The lethal dosage of 9alpha and 9beta-hydroxy grayanotoxin II were lower than that of grayanotoxin II. In add...

journal_title：Chemical & pharmaceutical bulletin

authors： Terai T,Osakabe K,Katai M,Sakaguchi K,Narama I,Matsuura T,Katakawa J,Tetsumi T

更新日期：2003-03-01 00:00:00

abstract：:Telmisartan (anti-hypertensive) is insoluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less (bioavailability 42%). In the present study an attempt has been made to prepare immediate release tablets of...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekar V,Chellan VR

更新日期：2008-04-01 00:00:00

abstract：:A nondestructive, efficient, and rapid method for quantitative analysis of two bioactive components (salidroside and p-tyrosol) in Rhodiola crenulata, a traditional Tibetan medicine, by Fourier transform near-infrared (FT-NIR) spectroscopy was developed. Near-infrared diffuse reflectance spectra in the range of 4000 t...

journal_title：Chemical & pharmaceutical bulletin

authors： Li T,He X

更新日期：2016-01-01 00:00:00

abstract：:Targeted protein degradation by small molecules is an emerging modality with significant potential for drug discovery. We previously developed chimeric molecules, termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which induce the ubiquitylation and proteasomal de...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohoka N,Ujikawa O,Shimokawa K,Sameshima T,Shibata N,Hattori T,Nara H,Cho N,Naito M

更新日期：2019-03-01 00:00:00

abstract：:A convenient and economical synthesis of 4-hydroxy-2,3-dimethoxybenzaldehyde has been developed. This was used as the starting material for the first total syntheses of (+/-)-isopiline, (+/-)-preocoteine, (+/-)-oureguattidine and (+/-)-3-methoxynordomesticine in which the key step involved formation of ring C of the a...

journal_title：Chemical & pharmaceutical bulletin

authors： Nimgirawath S,Udomputtimekakul P,Taechowisan T,Wanbanjob A,Shen Y

更新日期：2009-04-01 00:00:00

abstract：:The aim of this study was to fabricate deformable chitosan (CS) microspheres for arterial embolization. CS microspheres containing poly(ethylene glycol) (PEG) were prepared by ionotropic gelation; PEG was then removed from the CS microspheres to produce the highly porous structure to allow deformability. The porosity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kang MJ,Park JM,Choi WS,Lee J,Kwak BK,Lee J

更新日期：2010-03-01 00:00:00

abstract：:The structures of the ternary palladium(II) complexes of the formulations [Pd(Gly)(bpy)](+)Cl(-).4H(2)O (Gly=glycine; bpy=2,2'-bipyridine) (1), [Pd(Gly)(phen)](+)Cl(-).4H(2)O (2) (phen=1,10-phenanthroline) and {[Pd(Gly)(bpa)](+)Cl(-)}(2).6H(2)O (3) (bpa=2,2'-bipyridylamine) were determined. All complexes are positivel...

journal_title：Chemical & pharmaceutical bulletin

authors： Yodoshi M,Okabe N

更新日期：2008-07-01 00:00:00

abstract：:A reaction of methyl (4R,5R)-4,5-epoxy-2(E)-hexenoate 1 with N-benzylmethylamine gave a diastereomerically pure methyl (4R,5R)-4,5-epoxy-(3S)-N-benzylmethylamino hexanoate 6 and methyl (4S,5R)-4-N-benzyl-methylamino-5-hydroxy-2(E)-hexenoate 7. The former was chemoenzymatically converted to (-)-osmundalactone 11, which...

journal_title：Chemical & pharmaceutical bulletin

authors： Saotome C,Ono M,Akita H

更新日期：2001-07-01 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：:3Beta,4beta:15,16-diepoxy-13(16),14-clerodadiene (1) and a new clerodane diterpenoid designated thysaspathone (2) were isolated from the liverwort Thysananthus spathulistipus, while Radula appressa produced radulannin A (3), radulannin L (4), 2-geranyl-3,5-dihydroxybibenzyl (5), 2(S)-2-methyl-2-(4-methyl-3-pentenyl)-7...

journal_title：Chemical & pharmaceutical bulletin

authors： Harinantenaina L,Takahara Y,Nishizawa T,Kohchi C,Soma G,Asakawa Y

更新日期：2006-07-01 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