Synthesis of N-(trifluoromethyl-2-pyridinyl)arenesulfonamides as an inhibitor of secretory phospholipase A₂.

abstract：:A series of 2-acyl-6-methoxy-3,3,14-trimethyl-3,14-dihydro-7H-benzo[b]pyrano[3,2-h]acridin-7-ones (4-6) was prepared by treatment of 6-methoxy-3,3,14-trimethyl-3,14-dihydro-7H-benzo[b]pyrano[3,2-h]acridin-7-one (3) with an excess of an appropriate acyl chloride in the presence of aluminum chloride. Treatment of (+/-)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Doan Thi Mai H,Gaslonde T,Michel S,Koch M,Tillequin F,Bailly C,David-Cordonnier MH,Pfeiffer B,Léonce S,Pierré A

更新日期：2005-08-01 00:00:00

abstract：:Gambir, the aqueous extract from Uncaria gambir (Rubiaceae), has been used as an astringent medicine in Asian countries. Investigation of the constituents in the extract led to the isolation of four chalcane-flavan dimers, gambiriin A1 (6), A2 (7), B1 (8), and B2 (9), in addition to (+)-catechin (1), (+)-epicatechin (...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi S,Kuroda K,Doi K,Tanabe M,Shibata T,Yoshida T,Hatano T

更新日期：2007-02-01 00:00:00

abstract：:The resistance to crushing after a self-setting bioactive calcium phosphate cement, consisting of various particle sizes of tetracalcium phosphate (TECP), dicalcium phosphate dihydrate (DCPD) and hydroxyapatite (HAP), had hardened was tested after setting at 37 degrees C, 100% RH. X-ray diffraction suggested that the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otsuka M,Matsuda Y,Suwa Y,Fox JL,Higuchi WI

更新日期：1993-11-01 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：: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：:Three new acylated flavonol glycosides, cypellogins A (1), B (2) and C (3), along with eight known phenolic compounds, were isolated from the dried leaves of Eucalyptus cypellocarpa, and their structures were elucidated using spectroscopic methods, including 2D NMR experiments and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kasajima N,Ito H,Hatano T,Yoshida T,Kaneda M

更新日期：2005-10-01 00:00:00

abstract：:We synthesized some 4,4'- and 2,2'-dihydroxytriphenylmethane derivatives 3a--e and 4a--c by condensation of phenol 1 and aromatic aldehyde 2 in moderate to good yields (30--83%). Most of them showed significant antiviral activity against herpes simplex virus type 1 (anti-HSV-1 activity) in a plaque reduction assay. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Mibu N,Yokomizo K,Uyeda M,Sumoto K

更新日期：2005-09-01 00:00:00

abstract：:Fatty acid synthesis (FAS) is an essential metabolism during the whole growth and development process of the bacterial. Several key enzymes which involved in this biosynthetic pathway have been considered as useful targets for the development of new antibacterial agents. Among them, β-ketoacyl-acyl carrier protein syn...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou Y,Yang YS,Song XD,Lu L,Zhu HL

更新日期：2017-01-01 00:00:00

abstract：:N-(2-Dimethylaminoethyl)carboxamide (1a-d), 2-dimethylaminoethyl alkyl ether (2a, b), and 2-dimethylaminoethyl 2-hydroxy-2-phenethyl ether (3a-c) and its amino and methylene analogues (3d, 4) have been screened for antiamnestic and antihypoxic activities in mice. A clear reversing effect on electroconvulsive shock-ind...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono S,Yamafuji T,Chaki H,Todo Y,Maekawa M,Kitamura K,Tai M,Narita H

更新日期：1995-09-01 00:00:00

abstract：:Phytochemical investigation of the leaves of Umbilicus pendulinus afforded in addition to 2-O-caffeoyl malate, isoquercitrin and Z-venusol, the new isomer E-venusol. Special NMR experiments were carried out to elucidate the configuration of the two latter compounds. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Viornery L,Saliba C,Daskiewicz JB,Bayet C,Comte G,Fenet B,Gutierrez G,Barron D

更新日期：2000-11-01 00:00:00

abstract：:Invasive fungal disease constitutes a growing health problem and development of novel antifungal drugs with high potency and selectivity against new fungal molecular targets are urgently needed. In order to develop potent antifungal agents, a novel series of 6-alkyl-indolo[3,2-c]-2H-thiochroman derivatives were synthe...

journal_title：Chemical & pharmaceutical bulletin

authors： Han XY,Zhong YF,Li SB,Liang GC,Zhou G,Wang XK,Chen BH,Song YL

更新日期：2016-09-01 00:00:00

abstract：:A new oleanan-type triterpene and three new cincholic acid glycosides were isolated from Peruvian "Una de Gato" (Cat's claw, plant of origin: Uncaria tomentosa), a traditional herbal medicine in Peru. Their structures were determined by spectroscopic analysis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima M,Hashimoto K,Sandoval M,Aimi N,Takayama H

更新日期：2004-10-01 00:00:00

abstract：:The CHCl3 extract of the root of Angelica japonica showed high inhibitory activity against human gastric adenocarcinoma (MK-1) cell growth. From this extract, a new furanocoumarin named japoangelone and four furanocoumarin ethers of falcarindiol, named japoangelols A-D, were isolated together with caffeic acid methyl ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujioka T,Furumi K,Fujii H,Okabe H,Mihashi K,Nakano Y,Matsunaga H,Katano M,Mori M

更新日期：1999-01-01 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：:A catalytic amount of tin(IV) chloride catalyzed formal [4+2] cycloaddition reaction of di-tert-butyl 2-ethoxycyclobutane-1,1-carboxylate with ketones or aldehydes to give diethyl 6-ethoxydihydro-2H-pyran-3,3(4H)-dicarboxylates, whereas two equivalents of trimethylsilyl triflate promoted tandem [4+2] cycloaddition and...

journal_title：Chemical & pharmaceutical bulletin

authors： Okado R,Nowaki A,Matsuo J,Ishibashi H

更新日期：2012-01-01 00:00:00

abstract：:Five new components, named multiforisins A, B, C, D, and E, with immunosuppressive activity were isolated from an Ascomycete, Gelasinospora multiforis. Multiforisin A, the main immunosuppressive principle of this fungus, was deduced to be 5-formyl-3-(hydroxymethyl)-4-methoxy-6-(1E-propenyl)-alpha-pyrone. Multiforisins...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujimoto H,Satoh Y,Nakayama M,Takayama T,Yamazaki M

更新日期：1995-04-01 00:00:00

abstract：:We describe here a Tf₂NH-catalyzed formal (3+3) cycloaddition of silyl enol ethers with acrylates as a new domino reaction. In the domino sequence, the catalyst activates Michael addition, deprotonation of the resulting silyloxonium cation and intramolecular Claisen condensation. It was found that reaction modes signi...

journal_title：Chemical & pharmaceutical bulletin

authors： Azuma T,Takemoto Y,Takasu K

更新日期：2011-01-01 00:00:00

abstract：:A series of diarylureas and diarylamides possessing pyrrolo[2,3-d]pyrimidine scaffold was designed and synthesized. The in vitro antiproliferative activities of a selected group of the target compounds against NCI-60 cell line panel were tested and compared with Sorafenib and Imatinib as reference compounds. Most of t...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Gamal MI,Oh CH

更新日期：2014-01-01 00:00:00

abstract：:A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PA...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki H,Ogiku T,Sai H,Moritani Y,Ohtani A,Ohmizu H

更新日期：2009-09-01 00:00:00

abstract：:The purpose of this study was to predict the stability of meropenem in a mixed infusion. The hydrolysis of meropenem 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 (kobs) of pH, ...

journal_title：Chemical & pharmaceutical bulletin

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

更新日期：2015-01-01 00:00:00

abstract：:The percutaneous (p.c.) absorption of clonazepam (CZP), an antiepileptic drug, was investigated in rabbits. CZP was efficiently absorbed from a gel ointment (0.5% CZP, 1g, 9 cm2) with Azone and therapeutic plasma concentrations were maintained for 27 h. The bioavailability of CZP from the gel ointment was 47.2 +/- 3.1...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogiso T,Ito Y,Iwaki M,Yamamoto Y

更新日期：1989-02-01 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：: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：: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：:Nonenzymatically glycated human serum albumin was incubated with ferric ion at 37 degrees C in 0.2 M phosphate buffer, pH 7.4, up to 30 days. In the incubation mixture, amino acids, tyrosine and phenylalanine, were detected, suggesting site specific cleavage of glycated human serum albumin. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakurai T,Takanashi M,Tsuchiya S

更新日期：1992-06-01 00:00:00

abstract：:The pharmacokinetics of [6]-gingerol were investigated in rats with acute renal failure induced by bilateral nephrectomy, or those with acute hepatic failure induced by a single oral administration of carbon tetrachloride (CCl4), to clarify the contribution of the kidney and liver to the elimination process of [6]-gin...

journal_title：Chemical & pharmaceutical bulletin

authors： Naora K,Ding G,Hayashibara M,Katagiri Y,Kano Y,Iwamoto K

更新日期：1992-05-01 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：:Three new hydrolyzable tannins, euphormisins M1, M2, and M3, were isolated from Euphorbia humifusa WILLD., and respectively characterized as 1,3,6-tri-O-galloyl-4-O- brevifolincarboxyl-beta-D-glucose (19), an oxidative metabolite (23) of geraniin, and 1,3,6-tri-O-galloyl-alpha-D-glucose (18), by spectroscopic and chem...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Amakura Y,Liu YZ,Okuda T

更新日期：1994-09-01 00:00:00

abstract：:Chemical investigation of the soft coral Sinularia leptoclados has afforded three new sesquiterpenoids, leptocladols A (1), B (2), and 1-epi-chabrolidione A (3). The relative structures of 1-3 were determined on the basis of extensive spectroscopic analysis. The relative configuration of 1 was further confirmed by a s...

journal_title：Chemical & pharmaceutical bulletin

authors： Su JH,Chiang MY,Wen ZH,Dai CF,Hsu CH,Sheu JH

更新日期：2010-02-01 00:00:00

abstract：:Rapid and precise compositional analysis of copoly (DL-lactic/glycolic acid) (PLGA) was performed by pyrolysis-gas chromatography/mass spectrometry (Py-GC/MS) combined with one-step hydrolysis and methylation in the presence of tetramethylammonium hydroxide (TMAH). Pyrolysis of PLGA with TMAH gave two characteristic p...

journal_title：Chemical & pharmaceutical bulletin

authors： Urakami K,Higashi A,Umemoto K,Godo M,Watanabe C,Hashimoto K

更新日期：2001-02-01 00:00:00