A new route to (+)-estrone using a bicyclo[3.2.1]octane chiral building block.

abstract：:From the herb of Luffa acutangula ROXB. (Cucurbitaceae), seven oleanane-type triterpene saponins, acutosides A--G, were isolated and their structures were determined. Acutoside A is oleanolic acid 3-O-beta-D-glucopyranosyl-(1----2)-beta-D-glucopyranoside. Acutosides B, D, E, F and G have a common prosapogenin structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagao T,Tanaka R,Iwase Y,Hanazono H,Okabe H

更新日期：1991-03-01 00:00:00

abstract：:A series of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5HT3) receptor antagonistic activities by means of assays of 5-HT3 receptor binding and the ability to antagonize the von Bezold-Jarisch reflex in rats. Replacement of the 1,4-benzoxazine ring with a 1,4...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroita T,Marubayashi N,Sano M,Kanzaki K,Inaba K,Kawakita T

更新日期：1996-11-01 00:00:00

abstract：:We designed a single unit type tablet formulation containing nateglinide to decrease both postprandial blood glucose level (PBG) and fasting blood glucose level (FBG) in normal beagle dogs. The tablet was a dry coated tablet comprising both a core tablet (an erosion matrix tablet: a controlled release portion(nateglin...

journal_title：Chemical & pharmaceutical bulletin

authors： Makino C,Sakai H,Okano A,Yabuki A

更新日期：2009-09-01 00:00:00

abstract：:The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydr...

journal_title：Chemical & pharmaceutical bulletin

authors： Giammona G,Giannola LI,Carlisi B,Bajardi ML

更新日期：1989-08-01 00:00:00

abstract：:Two novel pentanorcucurbitane triterpenes, 22-hydroxy-23,24,25,26,27-pentanorcucurbit-5-en-3-one (1) and 3,7-dioxo-23,24,25,26,27-pentanorcucurbit-5-en-22-oic acid (2) together with a new trinorcucurbitane triterpene, 25,26,27-trinorcucurbit-5-ene-3,7,23-trione (3) were isolated from the methyl alcohol extract of the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen CR,Liao YW,Wang L,Kuo YH,Liu HJ,Shih WL,Cheng HL,Chang CI

更新日期：2010-12-01 00:00:00

abstract：:A calcium-binding protein, regucalcin, was isolated from rat liver cytosol. Rabbit-anti-regucalcin antiserum, which was raised against regucalcin conjugated by glutaraldehyde to bovine serum albumin, was applied to glutaraldehyde-fixed whole mounts and subsequently visualized using the peroxidase-antiperoxidase method...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamaguchi M,Isogai M,Kato S,Mori S

更新日期：1991-06-01 00:00:00

abstract：:Two novel tropoloisoquinoline alkaloids, Pareirubrines A and B, have been isolated as antileukemic substances from Cissampelos pareira (Menispermaceae), together with the same skeleton alkaloids, grandirubrine and isoimerubrine. Their structures were elucidated by nuclear magnetic resonance (NMR) studies, and their so...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Matsumoto K,Takeya K,Itokawa H,Iitaka Y

更新日期：1993-08-01 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：:Anti-tauro 1 beta-hydroxycholic acid antisera were prepared by immunizing rabbits with N-(1 beta,3 alpha, 7 alpha, 12 alpha-tetrahydroxy-5 beta-cholan-24-oyl)-2- aminopropionic acid-bovine serum albumin (BSA) conjugate. The antisera raised had high affinity (1.25-1.46 x 10(9) M-1) and specificity for conjugated 1 beta...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikegawa S,Murai T,Yoshimura T,Tohma M

更新日期：1992-07-01 00:00:00

abstract：:Chemical and pharmacological studies of Panax vietnamensis (Vietnamese ginseng; VG) have been reported since its discovery in 1973. However, the content of each saponin in different parts of VG has not been reported. In this study, 17 ginsenosides in the different underground parts of P. vietnamensis were analyzed by ...

journal_title：Chemical & pharmaceutical bulletin

authors： Le TH,Lee GJ,Vu HK,Kwon SW,Nguyen NK,Park JH,Nguyen MD

更新日期：2015-01-01 00:00:00

abstract：:The latex of Euphorbia nivulia afforded three new ingol diterpenes, 3-acetyl-8-methoxyl-7-angolyl-12-hydroxylingol (7), 3,12-diacetyl-7-hydroxy-8-methoxylingol (8), and 3,12-diacetyl-7-angolyl-8-hydroxylingol (9) along with five known ingol diterpenes 2-6 and a known triterpene cyclonivulinol (1). Their structures wer...

journal_title：Chemical & pharmaceutical bulletin

authors： Ravikanth V,Lakshmi Niranjan Reddy V,Vijender Reddy A,Ravinder K,Prabhakar Rao T,Siva Ram T,Anand Kumar K,Prakesh Vamanarao D,Venkateswarlu Y

更新日期：2003-04-01 00:00:00

abstract：:Sodium nitroprusside (SNP) releases nitric oxide (NO), a powerful vasodilator, and thus widely used in intensive care unit for treating hypertension emergency. However, cardiac toxicity after SNP administration is a clinical problem. For finding a natural compound that suppressing SNP-induced cardiac toxicity, we test...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee SR,Kwak JH,Noh SJ,Pronto JR,Ko KS,Rhee BD,Xu Z,Kim N,Han J

更新日期：2014-01-01 00:00:00

abstract：:Two new bile acids, tauroselocholic acid (1) and tauroansocholic acid (2), a new natural bile acid, cygnocholic acid (3) were respectively isolated from bear bile powder Selenaretos thibetanus CUVIER and bile of geese Anser anser domesticus, together with seven known compounds. By spectrum analysis of MS, 1D and 2D NM...

journal_title：Chemical & pharmaceutical bulletin

authors： Bi D,Chai XY,Song YL,Lei Y,Tu PF

更新日期：2009-05-01 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：: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：:Certain amide-containing anthraquinone, xanthone, and carbazole derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal carcinoma (NPC-TW01), lung carcinoma (NCI-H661), and leukemia (Jurkat). Among them, 2-(9,10...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen LC,Juang SH,Chang KM,Tzeng CC,Chen JJ,Chen IL,Wang TC

更新日期：2014-01-01 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：:Using a microcalorimetric method, we have measured the heat production in states 3 and 4 respiration of a mitochondrial preparation from rat heart ventricle. Adenosine triphosphate production in state 3 respiration was also determined for the same preparation after heat production was measured. In Tris-buffered soluti...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamura K,Hayatsu H,Watanabe I,Nakano T,Sugawara Y,Nishii Y

更新日期：1989-11-01 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：: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：:Self-organizing map (SOM) of Kohonen seems to be a promising approach beyond the standard one to regression for some classification problems encountered in the field of pharmacy. We apply them, therefore, to the quantitative structure-activity relationship (QSAR) in carboquinones and benzodiazepines, and show their us...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawakami J,Hoshi K,Ishiyama A,Miyagishima S,Sato K

更新日期：2004-06-01 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：:Simple one-pot methods for preparation of 2-oxazolines have been developed using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM). Treatment of a mixture of carboxylic acids and 2-haloethylammonium salts with DMT-MM in methanol followed by refluxing in the presence of KOH gives oxazolines. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Takechi Y,Kimura N,Tanaka H,Kunishima M

更新日期：2008-12-01 00:00:00

abstract：:Mycalamide A and mycalamide B, isolated as antiviral and antitumor agents from a New Zealand sponge of the genus Mycale, converted the morphology of ras-transformed NRK-cells to normal morphology at 10 and 1 ng/ml, respectively. The effect on protein synthesis suggests that these agents converted the morphology by pre...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawara H,Higashi K,Uchino K,Perry NB

更新日期：1991-08-01 00:00:00

abstract：:A practical protocol to obtain accurate heat capacity values of pharmaceutical compounds using modulated-temperature differential scanning calorimetry was established. Three pharmaceutical compounds, acetaminophen, indomethacin, and tri-O-methyl-β-cyclodextrin were used as model compounds. Powder samples did not produ...

journal_title：Chemical & pharmaceutical bulletin

authors： Harada T,Kawakami K,Yoshihashi Y,Yonemochi E,Terada K,Moriyama H

更新日期：2013-01-01 00:00:00

abstract：:beta-Cyclododecyl aspartate was prepared and its application to peptide synthesis was examined. Derivatives of beta-cyclododecyl aspartate are more likely to crystallize and should be useful for peptide synthesis. The cyclododecyl ester was much stable to bases than the benzyl ester and rather more stable than the cyc...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawasaki K,Murakami T,Koshino K,Namikawa M,Maeda M,Hama T,Mayumi T

更新日期：1994-04-01 00:00:00

abstract：:The synthesis and biological evaluation of [2-Valine-A] insulin ([Val2-A]insulin) is reported. In this insulin, the isoleucine residue in position A2, invariant in the majority of mammalian insulins, is substituted by valine. The same substitution, along with four others, occurs naturally in the insulin produced by th...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohta N,Burke GT,Katsoyannis PG

更新日期：1989-03-01 00:00:00

abstract：:Dryocrassyl formate, sitostanyl formate, and 12alpha-hydroxyfern-9(11)-ene were isolated from the fresh fronds of Cyathea podophylla. Their structures were elucidated by spectroscopic techniques and synthesis. Ten known triterpenoids, three derivatives of phytol, a stanol, and beta-tocopherol were also identified from...

journal_title：Chemical & pharmaceutical bulletin

authors： Arai Y,Hattori T,Hamaguchi N,Masuda K,Takano A,Shiojima K

更新日期：2003-11-01 00:00:00

abstract：:Total synthetic studies on natural products with promising biological profiles, coupled with their intriguing structural features, are described. The target molecules dealt with in this article are five helianane-type sesquiterpenes (heliannuols A, D and K and heliespirones A and C) and three meroterpenes (breviones A...

journal_title：Chemical & pharmaceutical bulletin

authors： Shishido K

更新日期：2013-01-01 00:00:00

abstract：:Alkaline sucrose density gradient and agarose gel electrophoresis methods were used to observe lambda deoxyribonucleic acid (DNA) strand breaks by the reaction system of reduced glutathione (GSH) with alloxan in the presence of Fe(3+)-ethylenediaminetetraacetic acid (EDTA). When DNA was incubated in the reaction syste...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai K,Haga K,Ogiso T

更新日期：1992-08-01 00:00:00