Discovery of Novel 7-[(1R,5S)-1-Amino-5-fluoro-3-azabicyclo[3.3.0]octan-3-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropane]-8-(methoxy or methyl)quinolones.

abstract：:Isoprenylated flavonoids 5,7-dihydroxy-3'-(2-hydroxy-3-methyl-3-butenyl)-3,6,4'-trimethoxyflavone (1), 3,7-dihydroxy-3'-(2-hydroxy-3-methyl-3-butenyl)-5,6,4'-trimethoxyflavone (2) and an isoprenylated acetophenone derivative (3) have been isolated from Duranta repens along with known compounds, 5-hydroxy-3,6,7,4'-tetr...

journal_title：Chemical & pharmaceutical bulletin

authors： Anis I,Ahmed S,Malik A,Yasin A,Choudary MI

更新日期：2002-04-01 00:00:00

abstract：:Tumor necrosis factor (TNF), a cytokine produced in macrophages, also acts as an endogenous pyrogen (EP). To investigate whether TNF has a role in the fever induced by Nocardia rubra cell wall skeleton (N-CWS), the relationship between fever and TNF production was studied in guinea pigs. N-CWS injected i.v. to guinea ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohara K,Hirano Y,Ishida H,Mori J,Tensho A

更新日期：1989-10-01 00:00:00

abstract：:From Jatropha cilliata M. Arg., a Peruvian medicinal plant, isoorientin and orientin were isolated as anxiolytic components by using the isolation guide of anti-conflict effect in mice. Several related flavonoids were also tested for this effect. Another bioassay-guided isolation using the acetic acid-induced writhing...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuyama E,Okamoto Y,Yamazaki M,Satake M

更新日期：1996-02-01 00:00:00

abstract：:From the water-soluble portion of the methanolic extract of the fruit of anise (Pimpinella anisum L.), which has been used as a spice and medicine since antiquity, twelve new and five known glucosides of phenylpropanoids, including four stereoisomers of anethole glycol 2'-O-beta-D-glucopyranoside and four stereoisomer...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishikawa T,Fujimatu E,Kitajima J

更新日期：2002-11-01 00:00:00

abstract：:Several E-ring-modified analogues of (RS)-camptothecin were synthesized by total synthesis via Friedländer condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camp...

journal_title：Chemical & pharmaceutical bulletin

authors： Ejima A,Terasawa H,Sugimori M,Ohsuki S,Matsumoto K,Kawato Y,Yasuoka M,Tagawa H

更新日期：1992-03-01 00:00:00

abstract：:A new series of highly potent angiotensin-converting enzyme (ACE) inhibitors, 1-(N2-substituted L-lysyl-gamma-D-glutamyl)octahydro-1H-indole-2-carboxylic acids, was synthesized; various acyl groups were introduced at the alpha-amino group of the N-terminal P1 Lys. The effect of the N2-acyl groups on in vitro inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Sawayama T,Tsukamoto M,Sasagawa T,Nishimura K,Deguchi T,Takeyama K,Hosoki K

更新日期：1990-01-01 00:00:00

abstract：:A series of novel 1,5-diphenylpyrazole derivatives bearing hydrophilic substituents was prepared. The anti-inflammatory and analgesic activities of these compounds were evaluated by using the adjuvant arthritis and Randall-Selitto assays in rats, and the structure-activity relationships were studied. The optimal compo...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsuji K,Konishi N,Spears GW,Ogino T,Nakamura K,Tojo T,Ochi T,Shimojo F,Senoh H,Matsuo M

更新日期：1997-09-01 00:00:00

abstract：:2,8-Dimethyl-1-oxa-8-azaspiro[4,5]decan-3-one (17), designed by incorporating the tetrahydrofuran ring moiety of muscarone into an 8-azaspiro[4,5]decane skeleton, and related 1-oxa-8-azaspiro[4.5]decanes were synthesized and assessed as M1 muscarinic agonists for the symptomatic treatment of dementia of Alzheimer's ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Tsukamoto S,Fujii M,Yasunaga T,Matsuda K,Wanibuchi F,Hidaka K,Furuya T,Tamura T

更新日期：1995-05-01 00:00:00

abstract：:Asymmetric total synthesis of benzene analogues of galbonolide, a 14-membered antifungal macrolide, possessing a benzene ring instead of a conjugated diene structure, was achieved starting from chiral 1-aryl-1-propanol obtained by enzyme-catalyzed kinetic resolution with high enantioselectivity. Representatively, a me...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakoh H,Sakuraba S,Sugimoto Y,Imamura H,Jona H,Yamada K,Bamba-Nagano R,Hashizume T,Morishima H

更新日期：2004-01-01 00:00:00

abstract：:The discovery of a novel class of state-dependent voltage-gated sodium channel (NaV)1.7 inhibitors is described. By the modification of amide or urethane bond in NaV1.7 blocker III, structure-activity relationship studies that led to the identification of novel NaV1.7 inhibitor 2i (DS01171986) were performed. Compound...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Kobayashi H,Suzuki S,Shibuya S,Kimoto H,Domon Y,Kubota K,Kitano Y,Yokoyama T,Shimizugawa A,Koishi R,Fujiwara C,Asano D,Shinozuka T

更新日期：2020-01-01 00:00:00

abstract：:Effect of the basic property of reactants (tertiary amine catalysts, a substrate amine, and acid neutralizers) on catalytic dehydrocondensation between a carboxylic acid and an amine by using 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) was studied. The reaction yield was affected by the acid-base equilibrium among re...

journal_title：Chemical & pharmaceutical bulletin

authors： Kunishima M,Kitamura M,Tanaka H,Nakakura I,Moriya T,Hioki K

更新日期：2013-01-01 00:00:00

abstract：:Two sensitive and selective spectrofluorimetric and spectrophotometric stability-indicating methods have been developed for the determination of some non-steroidal anti-inflammatory oxicam derivatives namely lornoxicam (Lx), tenoxicam (Tx) and meloxicam (Mx) after their complete alkaline hydrolysis. The methods are ba...

journal_title：Chemical & pharmaceutical bulletin

authors： Taha EA,Salama NN,Fattah Lel-S

更新日期：2006-05-01 00:00:00

abstract：:An examination was made on the effect of fumaric acid on an experimental systemic candidiasis. Male ICR mice were innoculated into the tail veins with 10(6) yeast cells of Candida albicans and treated with daily intraperitoneal injections of fumaric acid at the dose of 40 mg/kg/d. The results indicated that the admini...

journal_title：Chemical & pharmaceutical bulletin

authors： Akao M,Kuroda K

更新日期：1991-11-01 00:00:00

abstract：:The syntheses and anti-inflammatory activities of novel thieno[2,3-b]pyridine and thieno[2,3-b:5,4-c']-dipyridine derivatives are described. These compounds were designed by modification of the quinoline template of a new type of disease-modifying antirheumatic drug (DMARD), TAK-603, and prepared by the Friedländer re...

journal_title：Chemical & pharmaceutical bulletin

authors： Baba A,Mori A,Yasuma T,Unno S,Makino H,Sohda T

更新日期：1999-07-01 00:00:00

abstract：:It is well-known that baicalin-berberine complex (1) precipitates in the water decoction of numerous Chinese Medicinal formulae containing Radix Scutellariae and Rhizoma Coptidis or Cortex Phellodendri. In the current study, ionic interaction between the carboxylate ion of baicalin and the quaternary ammonium ion of b...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang JR,Tanaka T,Zhang H,Kouno I,Jiang ZH

更新日期：2012-01-01 00:00:00

abstract：:New triazine-type dehydrocondensing reagents, such as ROMP-Trz-Cl and ROMP(OH)-Trz-Cl, were synthesized by a ring opening metathesis polymerization (ROMP) method, and these showed higher loading than conventional polymer-supported condensing reagents. These polymers effect the formation of amides in good yields by add...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Kameyama S,Tani S,Kunishima M

更新日期：2007-05-01 00:00:00

abstract：:A simple one-step synthesis was accomplished for the preparation of N-phosphoramidophosphonates by a direct reaction of phosphoramidate (1) with heterocyclic aldehydes (2a-j) and dialkyl phosphites at 60-70 degrees C in the presence of tetramethylguanidine. The tetramethylguanidine not only catalyses this reaction but...

journal_title：Chemical & pharmaceutical bulletin

authors： Veera Narayana Reddy M,Balakrishna A,Kumar MA,Reddy GC,Sankar AU,Reddy CS,Krishna TM

更新日期：2009-12-01 00:00:00

abstract：:Arginine-vasopressin (AVP) was acylated with various acyl azides (2a-j) in pH 9.1 buffer to give AVP derivatives (11a-j) modified at the tyrosine side chain with a carbohydrate via a spacer arm. Glycoconjugates of AVP modified at the N-terminal amide (12a-e) were also synthesized from AVP and carboxylic acids (3a-e) u...

journal_title：Chemical & pharmaceutical bulletin

authors： Susaki H,Suzuki K,Ikeda M,Yamada H,Watanabe HK

更新日期：1998-10-01 00:00:00

abstract：:A series of 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives was synthesized and evaluated for its ability to reverse a scopolamine-induced learned impairment in a one-trial passive avoidance task (antiamnestic activity). 2-(4-Allyl-1-piperazinyl)-4-pentyloxyquinazoline (4) showed more potent antiamnestic activity th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori M,Iemura R,Hara H,Sukamoto T,Ito K,Ohtaka H

更新日期：1991-02-01 00:00:00

abstract：:This paper describes syntheses and doxorubicin-inclusion abilities of beta-cyclodextrin (CyD) derivatives with a hydroquinone alpha-glycoside residue attached at the primary side. The hydroquinone glycoside having an alpha-D-glucosidic or 2-acetamido-2-deoxy-alpha-D-glucosidic linkage became a useful component for pro...

journal_title：Chemical & pharmaceutical bulletin

authors： Oda Y,Miura M,Hattori K,Yamanoi T

更新日期：2009-01-01 00:00:00

abstract：:Fe2+-dependent lipid peroxidation in phosphatidylcholine (PC) liposomes, assessed by thiobarbituric acid-reactive substances (TBARS) production, was stimulated in the presence of Fe3+ in a concentration-dependent manner. The rates of nitroblue tetrazolium (NBT) reduction and Fe2+ oxidation (Fe2+ disappearance and Fe3+...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohyashiki T,Kadoya A,Kushida K

更新日期：2002-02-01 00:00:00

abstract：:Four new cembrane diterpenes (1-4) and fifteen known cembranoids (5-19) were isolated from an Okinawan soft coral Lobophytum crassum. The structures of these four new cembranoids were determined on the basis of spectroscopic evidence. In particular, the absolute stereochemistry of 1, 2, 5 and 6 were elucidated by the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wanzola M,Furuta T,Kohno Y,Fukumitsu S,Yasukochi S,Watari K,Tanaka C,Higuchi R,Miyamoto T

更新日期：2010-09-01 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：: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：:The mechanism of the electrochemical oxidation of 2,5-dihydroxybenzoic acid and 3,4-dihydroxybenzaldehyde in the presence of 3-hydroxy-1H-phenalene-1-one as a nucleophile has been studied in water/acetonitrile (80/20 v/v) solution using cyclic voltammetry and controlled-potential coulometry methods. The results indica...

journal_title：Chemical & pharmaceutical bulletin

authors： Nematollahi D,Amani A

更新日期：2008-04-01 00:00:00

abstract：:The manufacture of highly drug-loaded fine globular granules eventually applied for orally disintegrating tablets has been investigated using a unique multi-functional rotor processor with acetaminophen, which was used as a model drug substance. Experimental design and statistical analysis were used to evaluate potent...

journal_title：Chemical & pharmaceutical bulletin

authors： Iwao Y,Kimura S,Ishida M,Mise R,Yamada M,Namiki N,Noguchi S,Itai S

更新日期：2015-01-01 00:00:00

abstract：:We describe here (2+2) cycloaddition reaction of alkyl enol ethers with acrylates catalyzed by triethylsilyl triflic imide (Et3SiNTf2), which was in situ generated from triethylsilane and triflic imide. The reaction efficiently provides substituted cyclobutanes bearing alkoxy function in a stereoselective manner. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takasu K,Miyakawa Y,Ihara M,Tokuyama H

更新日期：2008-08-01 00:00:00

abstract：:Two new cangorosin A type triterpene dimers, which composed of two triterpene units jointed by two ether linkages between the A and B rings, were isolated from the Brazilian medicinal plant "xuxuá" (Maytenus chuchuhuasca). Structures of new isolates, xuxuasins A (1) and B (2), were established based on several spectro...

journal_title：Chemical & pharmaceutical bulletin

authors： Shirota O,Sekita S,Satake M,Morita H,Takeya K,Itokawa H

更新日期：2004-09-01 00:00:00

abstract：:The differences in biological activities among polychlorinated dibenzo-p-dioxins (dioxins) are strongly dependent on the substitution pattern of chlorine at various positions on the parent dibenzo-p-dioxin molecule. The absolute hardness, eta, of dioxins shows a good correlation with the potency of biological activity...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi S,Sameshima K,Ishii Y,Tanaka A

更新日期：1995-10-01 00:00:00

abstract：:From the seeds of Pharbitis nil (Convolvulaceae), two new oleanene-type triterpene glycosides, pharbitosides A (1) and B (2), together with beta-sitosterol, beta-sitosterol glucoside (daucosterol), caffeic acid, and methyl caffeate were isolated. The structure of pharbitoside A (1) was elucidated to be queretaroic aci...

journal_title：Chemical & pharmaceutical bulletin

authors： Jung DY,Ha H,Lee HY,Kim C,Lee JH,Bae K,Kim JS,Kang SS

更新日期：2008-02-01 00:00:00