New bicyclic taxane diterpenoids from Taxus sumatrana.

abstract：:Total syntheses of structurally and biologically intriguing natural products relying on new synthetic methodologies are described. This article features cinchona alkaloid-catalyzed asymmetric Morita-Baylis-Hillman reactions, heterocycle syntheses based on rhodium-catalyzed C-H amination and indium-catalyzed Conia-ene ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hatakeyama S

更新日期：2014-01-01 00:00:00

abstract：:The metabolic pathway of butylated hydroxytoluene (BHT) to the ring-oxygenated metabolites 2,6-di-tert-butylhydroquinone (BHQ) and 2,6-di-tert-butyl-p-benzoquinone (BBQ) was examined in rats. After intraperitoneal administration of 3,5-di-tert-butyl-4-hydroxybenzoic acid (BHT-acid), which had been regarded as one of t...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto K,Tajima K,Takemura M,Mizutani T

更新日期：1991-02-01 00:00:00

abstract：:The synthesis and structure-activity-relationship (SAR) for a series of N-substituted piperazinyl carbamoyl 7-15 and piperazinyl acetyl 18-26 derivatives of tetrahydropapaverine have been carried out. The general synthetic methods of carbamoyl tetrahydropapaverine analogues involve N-substituted piperazines and carbam...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaur J,Ghosh NN,Talwar A,Chandra R

更新日期：2002-09-01 00:00:00

abstract：:A novel series of 2-acyl-3-carboxyl-tetrahydroisoquinoline derivatives were synthesized and biologically evaluated. Among them, (S)-2-{(E)-3-furan-2-ylacryloyl}-7-[(2E,4E)-5-(2,4,6-trifluorophenyl)penta-2,4-dienyloxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (compound 17u) was identified as a potent protein ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Morishita K,Shoji Y,Fukui M,Ito Y,Kitao T,Ozawa SI,Hirono S,Shirahase H

更新日期：2018-01-01 00:00:00

abstract：:A full account is given of the first chemical synthesis of the antitumor antibiotic guanine 7-oxide (5) and its 9-substituted derivatives (24a--k and 26). Coupling of appropriate primary amines (17a--e, g--k) with phenacyl bromide (16) produced, after treatment with HCl, the corresponding N-substituted phenacylamine h...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawa K,Nishii M,Inagaki J,Nohara F,Saito T,Itaya T,Fujii T

更新日期：1992-02-01 00:00:00

abstract：:Melt pelletization of lactose 450 M was carried out in an 8-l high shear mixer using PEG 3000 as the meltable binder. The pore size and size distribution of the melt pellets were determined using mercury intrusion porosimetry. The pore size distribution of melt pellets was found to be bimodal. With a higher binder con...

journal_title：Chemical & pharmaceutical bulletin

authors： Wong TW,Chan LW,Heng PW

更新日期：2000-11-01 00:00:00

abstract：:Two new pyrrole oligoglycosides, plancipyrrosides A and B (1 and 2), were isolated from methanol extract of the Vietnamese starfish Acanthaster planci using various chromatographic procedures. Their structures were elucidated by spectroscopic methods including one and two dimensional (1D- and 2D)-NMR and Fourier trans...

journal_title：Chemical & pharmaceutical bulletin

authors： Vien LT,Hanh TT,Huong PT,Dang NH,Thanh NV,Lyakhova E,Cuong NX,Nam NH,Kiem PV,Kicha A,Minh CV

更新日期：2016-11-01 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：:Improved synthesis of the trans-3,5-disubstituted pyrrolidin-3-ylthio side-chain of the novel carbapenem 1 was achieved via stereoselective reduction of the 1-aryl-1-butanone derivative 5 and successive intramolecular cyclization of the resulting chiral alcohol 6. The 1-aryl-1-butanone derivative 5 was obtained by a c...

journal_title：Chemical & pharmaceutical bulletin

authors： Hashihayata T,Sakoh H,Goto Y,Hirose M,Sakuraba S,Imamura H,Sugimoto Y,Yamada K,Morishima H

更新日期：2001-11-01 00:00:00

abstract：:One novel sesquiterpene with new skeleton, (6S)-2-methyl-6-(4-hydroxyphenyl-3-methyl)-2-hepten-4-one (1), two new bisabolane sesquiterpenes, (6S)-2-methyl-6-(4-hydroxyphenyl)-2-hepten-4-one (2), (6S)-2-methyl-6-(4-formylphenyl)-2-hepten-4-one (3), and two calebin derivatives, 4''-(4'''-hydroxyphenyl-3'''-methoxy)-2''-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng Y,Qiu F,Takahashi K,Liang J,Qu G,Yao X

更新日期：2007-06-01 00:00:00

abstract：:The analgesic components were isolated from a Bornean medicinal plant, Tabernaemontana pauciflora Blume (syn. Ervatamia blumeana Mark gr.), and the major components were identified as coronaridine and 3-(2-oxopropyl)coronaridine. Four minor components were estimated to be 5R- and 5S-(2-oxopropyl)coronaridine, 3-(2-oxo...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuyama E,Gao LH,Yamazaki M

更新日期：1992-08-01 00:00:00

abstract：:Racemic 1-acetoxy-2-phenylpropane (12) and 1-acetoxy-2-(2-naphthyl)propane (33) were hydrolyzed with lipase at 35-36 degrees C for 2 and 24 h to give predominantly (S)-2-phenyl-1-propanol (11) and (S)-2-(2-naphthyl)-1-propanol (32), respectively. However, racemic 1-acetoxy-2-(1-naphthyl)propane (25) was recovered inta...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto T,Takeda Y,Iwata E,Sakamoto M,Ishida T

更新日期：1994-06-01 00:00:00

abstract：:Mutant activin receptor-like kinase-2 (ALK2) was reported to be closely associated with the pathogenesis of fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG), and therefore presents an attractive target for therapeutic intervention. Through in silico virtual screenings and structu...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekimata K,Sato T,Sakai N,Watanabe H,Mishima-Tsumagari C,Taguri T,Matsumoto T,Fujii Y,Handa N,Honma T,Tanaka A,Shirouzu M,Yokoyama S,Miyazono K,Hashizume Y,Koyama H

更新日期：2019-01-01 00:00:00

abstract：:The abnormal aggregation of amyloid β-peptide (Aβ) is central to the pathogenesis of Alzheimer's disease, the major form of dementia. Aromatic π-π interactions have been suggested to play a crucial role in the aggregation of not only Aβ, but also other amyloidogenic proteins. In this study, each or all phenylalanine (...

journal_title：Chemical & pharmaceutical bulletin

authors： Genji M,Yano Y,Hoshino M,Matsuzaki K

更新日期：2017-01-01 00:00:00

abstract：:Two new stilbene glucosides [(+)-alpha-viniferin 13b-O-beta-glucopyranoside and resveratrol 12-C-beta-glucopyranoside] and two new resveratrol oligomers, hemsleyanols A and B, were isolated from the bark of Shorea hemsleyana along with four known resveratrol oligomers. The structures of the isolates, including the rel...

journal_title：Chemical & pharmaceutical bulletin

authors： Ito T,Tanaka T,Ido Y,Nakaya KI,Iinuma M,Riswan S

更新日期：2000-07-01 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：:Benzoxazinorifamycin reacted with various secondary amines to yield various 5'-substituted aminobenzoxazinorifamycin derivatives. The derivatives exhibited potent activities against gram-positive bacteria and mycobacteria. The antimicrobial activities of these compounds against Mycobacterium tuberculosis and Mycobacte...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamane T,Hashizume T,Yamashita K,Hosoe K,Hidaka T,Watanabe K,Kawaharada H,Kudoh S

更新日期：1992-10-01 00:00:00

abstract：:A mechanism for the relatively high permeability of vitamin C in relation to the change in the protein domain of the stratum corneum has been proposed. Firstly, the skin permeation characteristics of vitamin C (l-[1-14C]-ascorbic acid) using whole skin and stripped skin of the hairless mouse were investigated. By empl...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee AR,Tojo K

更新日期：1998-01-01 00:00:00

abstract：:A novel macrocyclic diterpene, jatrophenone, has been isolated from the whole plant of Jatropha gossypifolia. The structure of the compound was established by detailed studies of its one- and two-dimensional (1D and 2D) NMR spectra. The compound possesses significant antibacterial activity. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ravindranath N,Venkataiah B,Ramesh C,Jayaprakash P,Das B

更新日期：2003-07-01 00:00:00

abstract：:A new resveratrol dimer and a new C-glucosyl resveratrol were isolated from stem wood of Hopea utilis along with nine stilbenoid derivatives comprising bergenin and (+)-lyoniresinol. The structures have been elucidated on the basis of the spectroscopic evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka T,Ito T,Ido Y,Nakaya K,Iinuma M,Chelladurai V

更新日期：2001-06-01 00:00:00

abstract：:In order to synthesize four stereoisomers of cystathionine (CYT), D- and L-homocysteines (D- and L-Hcy) were synthesized from methionine (Met) by a facile procedure. L-Met was reacted with dichloroacetic acid in concentrated hydrochloric acid under reflux to give (4S)-1,3-thiazane-2,4-dicarboxylic acid hydrochloride [...

journal_title：Chemical & pharmaceutical bulletin

authors： Shiraiwa T,Nakagawa K,Kanemoto N,Kinda T,Yamamoto H

更新日期：2002-08-01 00:00:00

abstract：:Three new limonoids, cipadesins D--F (1--3), together with 8,15-dihydroxy-13E-labdane, beta-sitosterol and beta-daucosterol, were isolated from the leaves and bark of Cipadessa cinerascens. Their structures were elucidated by spectral evidence. X-Ray crystallographic analysis confirmed the structure of 1. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yuan XH,Li BG,Xu CX,Zhou M,Qi HY,Zhang GL

更新日期：2007-06-01 00:00:00

abstract：:Three new compounds were isolated from a MeOH extract of the leaves of Syzygium samarangense, one new cyanogenic glucoside, taxiphyllin 6'-O-gallate (1), one new megastigmane glucoside, actinidioionoside 6'-O-gallate (2), and one new sulfated flavonoid rhamnoside, myricetrin 2″-O-sulfate (3), together with 14 known co...

journal_title：Chemical & pharmaceutical bulletin

authors： Samy MN,Sugimoto S,Matsunami K,Otsuka H,Kamel MS

更新日期：2014-01-01 00:00:00

abstract：:The release properties of phenylpropanolamine hydrochloride (PPA) from ethylcellulose (EC) matrix granules prepared by an extrusion granulation method were examined. The release process could be divided into two parts; the first and second stages were analyzed by applying square-root time law and cube-root law equatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukui A,Fujii R,Yonezawa Y,Sunada H

更新日期：2004-03-01 00:00:00

abstract：:New gamma-pyrones, 9'-oxopodopyrone (3) and 8-methyl-9'-oxopodopyrone (4) were isolated from the leaves of Gonystylus keithii, along with known gamma-pyrones, 10'-oxopodopyrone (1) and 8-methyl-10'-oxopodopyrone (2). These gamma-pyrones markedly inhibited the bovine parathyroid hormone (PTH)-induced Ca release from ne...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanazawa T,Ohkawa Y,Kuda T,Minobe Y,Tani T,Nishizawa M

更新日期：1997-06-01 00:00:00

abstract：:The metabolism of 2,4-dinitrotoluene (2,4-DNT), 2,4-dinitrobenzyl alcohol (2,4-DNB), 2,4-dinitrobenzaldehyde (2,4-DNBAl), 2,6-DNT, 2,6-DNB and 2,6-DNBAl in the microsomal and cytosol fractions prepared from unfortified male Wistar and male Sprague-Dawley (S.D.) rat livers was investigated. Data obtained by high-perfor...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori M,Kawajiri T,Sayama M,Miyahara T,Kozuka H

更新日期：1989-07-01 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：:N-Nitrosodialkylamines are alkylating carcinogens which are metabolically activated to alpha-hydroxy nitrosamines through oxidative dealkylation by cytochrome P450. In this study, the dealkylation step in the activation of N-nitrosodibenzylamine (NDBz) was investigated with metalloporphyrin/oxidant model systems under...

journal_title：Chemical & pharmaceutical bulletin

authors： Okochi E,Mochizuki M

更新日期：1995-12-01 00:00:00

abstract：:A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted-1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydr...

journal_title：Chemical & pharmaceutical bulletin

authors： Megally Abdo NY,Kamel MM

更新日期：2015-01-01 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