Immobilized triazine-type dehydrocondensing reagents for carboxamide formation: ROMP-Trz-Cl and ROMP(OH)-Trz-Cl.

abstract：:Four new cyclopropyl-triterpenes, 27-nor-3beta-hydroxy-25-oxocycloartane (1), (22E)-25,26,27-trinor-3beta-hydroxycycloart-22-en-24-al (2), 3beta-acetoxy-15alpha-hydroxy-13,27-cyclours-11-ene (3), 3beta-acetoxy-12alpha-formyloxy-13,27-cycloursan-11alpha-ol (4), together with (23E)-27-nor-3beta-hydroxycycloart-23-en-25-...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiang YM,Su JK,Liu YH,Kuo YH

更新日期：2001-05-01 00:00:00

abstract：:N-1 and N-2 substituted pyrazolo[4,5-g]pyrido[1,2-a]benzimidazoles were prepared regioselectively, and cytotoxicities evaluated in vitro against K562 and HL60 cells. All compounds displayed weaker activity than doxorubicin against sensitive lines, but showed the same activity against resistant cell lines (multidrug re...

journal_title：Chemical & pharmaceutical bulletin

authors： Dupuy M,Pinguet F,Blache Y,Chavignon O,Teulade JC,Chapat JP

更新日期：1998-11-01 00:00:00

abstract：:Two different test methods were studied for the evaluation of release profiles of carbon dioxide, CO2, from effervescent suppositories. Three lots of commercial suppositories containing sodium bicarbonate and anhydrous sodium dihydrogen phosphate were used. The volume of CO2 released from these suppositories in normal...

journal_title：Chemical & pharmaceutical bulletin

authors： Hakata T,Iijima M,Okabe T,Kimura S,Sato H,Watanabe Y,Matsumoto M

更新日期：1993-02-01 00:00:00

abstract：:We previously reported 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide 2 as on orally available monoacylglycerol acyltransferase 2 (MGAT2) inhibitor which exhibited an in vivo efficacy at an oral dose of 100 mg/kg in a mouse oral lipid tolerance test. Further optimizatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Busujima T,Tanaka H,Iwakiri K,Shirasaki Y,Munetomo E,Saito M,Masuko A,Kitano K,Io F,Kato K,Kamigaso S,Nozoe A,Sato N

更新日期：2016-01-01 00:00:00

abstract：:H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OMe, corresponding to the sequence 41-49 of eglin c, inhibited human leukocyte cathepsin G and alpha-chymotrypsin. In order to gain further insight into the relationship between the structure and the inhibitory activity against cathepsin G and alpha-chymotrypsin, peptide fragments...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakabayashi K,Tsuboi S,Fujimoto T,Okada Y,Nagamatsu Y,Yamamoto J

更新日期：1990-12-01 00:00:00

abstract：:The microbial transformation of five flavans (1-5) by endophytic fungi isolated from the tea plant Camellia sinensis was investigated. It was found that the endophytic filamentous fungus Diaporthe sp. oxidized stereoselectively at C-4 position of (+)-catechin (1) and (-)-epicatechin (2) to give the correspondent 3,4-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Agusta A,Maehara S,Ohashi K,Simanjuntak P,Shibuya H

更新日期：2005-12-01 00:00:00

abstract：:Three new natural sesquiterpene coumarins, isofeterin (1), lehmannolol (3), sinkianone (4), and one known compound, lehmannolone (2), were isolated from the roots of Ferula teterrima and Ferula sinkiangensis. Their chemical structures were established on the basis of spectroscopic analysis, including X-ray crystallogr...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang JR,An Z,Li ZH,Jing S,Qina HL

更新日期：2006-11-01 00:00:00

abstract：:Direct beta-glucosidation between benzyl alcohol and D-glucose (5) using the immobilized beta-glucosidase from almonds with the synthetic prepolymer ENTP-4000 gave a benzyl beta-D-glucoside (1) in 53% yield. The coupling of the benzyl beta-D-glucopyranoside congener (8) derived from 1 with phenyl 2,3,4-tri-O-acetyl-1-...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawahara E,Fujii M,Kato K,Ida Y,Akita H

更新日期：2005-08-01 00:00:00

abstract：:The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Sev...

journal_title：Chemical & pharmaceutical bulletin

authors： Ha ES,Baek IH,Cho W,Hwang SJ,Kim MS

更新日期：2014-01-01 00:00:00

abstract：:Two alkaloids, megistoquinone I (1) and megistoquinone II (2), were isolated from the bark of Sarcomelicope megistophylla. Their structures have been elucidated on the basis of MS and NMR data. Both belong to quinoline alkaloid series and should be considered as oxidation products of a furo[2,3-b]quinoline precursor. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fokialakis N,Magiatis P,Chinou I,Mitaku S,Tillequin F

更新日期：2002-03-01 00:00:00

abstract：:(±)-8-Deisopropyladunctin B, the deisopropyl form of adunctin B, which was isolated from the leaves of Piper aduncum (Piperaceae) collected in Papua New Guinea, was synthesized in 0.77% overall yield in 17 steps from 5,7-dimethoxycoumarin-3-carboxylate. The key step was our original stereoconvergent skeleton transform...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomura S,Arimitsu K,Yamaguchi S,Kosuga Y,Kakimoto Y,Komai T,Hasegawa K,Nakanishi A,Miyoshi T,Iwasaki H,Ozeki M,Kawasaki I,Kurume A,Ohta S,Yamashita M

更新日期：2012-01-01 00:00:00

abstract：:High-performance liquid chromatography coupled with solid phase extraction method was developed for determination of isofraxidin in rat plasma after oral administration of Acanthopanax senticosus extract (ASE), and pharmacokinetic parameters of isofraxidin either in ASE or pure compound were measured. The HPLC analysi...

journal_title：Chemical & pharmaceutical bulletin

authors： Sun H,Lv H,Zhang Y,Wang X,Bi K,Cao H

更新日期：2007-09-01 00:00:00

abstract：:Optically active structural isomers (1b-f and dst-1b-f) of 3',4'-di-(O)-(-)-camphanoyl-(+)-khellactone (DCK) were synthesized and their anti-human immunodeficiency virus (HIV) activity was investigated. The value of the sensitivity index (SI) of 1b was greater than that of DCK. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishioka H,Uesugi K,Ueda N,Kondo Y,Tsuji M,Abe H,Harayama T,Hamasaki T,Baba M,Takeuchi Y

更新日期：2011-01-01 00:00:00

abstract：:Tranilast, a lipophilic drug with various ophthalmic applications, was used as a model drug to establish the possibility of delivering lipophilic drugs through the eyelid skin. Pharmacokinetics and tissue distribution studies were conducted employing three application methods (topical application onto eyelid skin, eye...

journal_title：Chemical & pharmaceutical bulletin

authors： See GL,Arce F Jr,Itakura S,Todo H,Sugibayashi K

更新日期：2020-01-01 00:00:00

abstract：:Mucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the t...

journal_title：Chemical & pharmaceutical bulletin

authors： Ruiz-Caro R,Gago-Guillan M,Otero-Espinar FJ,Veiga MD

更新日期：2012-01-01 00:00:00

abstract：:The anti-anginal drug Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, is thought to modulate the metabolism during myocardial ischemia by activating pyruvate dehydrogenase activity to promote glucose oxidation. Ranolazine and its five principal metabolites: CVT-2512, CVT-2513, CVT-2514, CVT-2738 and CVT-4...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao Z,Gong S,Guan T,Li Y,Wu X,Sun H

更新日期：2009-11-01 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：:The adsorptive behavior of the anti-inflammatory drug meloxicam was studied by cyclic, differentia-pulse and square-wave voltammetry on a hanging mercury drop electrode (HMDE). The drug was accumulated at HMDE and a well-defined stripping peak current was obtained at -1.42 V vs. Ag/AgCl (saturated KCl) electrode in ac...

journal_title：Chemical & pharmaceutical bulletin

authors： Radi AE,Ghoneim M,Beltagi A

更新日期：2001-10-01 00:00:00

abstract：:Tryptanthrin is an ancient medicine which recently was also found to have a function of downregulating multidrug resistance (MDR). However, tryptanthrin is insoluble in water, which limits its availability for delivery into cancer cells. There is a need to improve delivery systems to increase the inhibition of MDR. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Fang YP,Lin YK,Su YH,Fang JY

更新日期：2011-01-01 00:00:00

abstract：:The iron(III) complex of 2,7,12,17-tetraethyl-3,6,11,18-tetra-methylcorrphycene, an isomeric heme, was complexed with apomyoglobin to examine the ligand binding ability of the novel macrocycle under physiological conditions. The reconstituted holoprotein was found to be functionally active at pH 7.4 and 20 degrees C a...

journal_title：Chemical & pharmaceutical bulletin

authors： Neya S,Nakamura M,Imai K,Funasaki N

更新日期：2001-03-01 00:00:00

abstract：:The miscibility of a drug with excipients in solid dispersions is considered to be one of the most important factors for preparation of stable amorphous solid dispersions. The purpose of the present study was to elucidate the feasibility of (1)H-NMR spin-lattice relaxation measurements to assess the miscibility of a d...

journal_title：Chemical & pharmaceutical bulletin

authors： Aso Y,Yoshioka S,Miyazaki T,Kawanishi T,Tanaka K,Kitamura S,Takakura A,Hayashi T,Muranushi N

更新日期：2007-08-01 00:00:00

abstract：:In the conventional method of mixer blending extraction, the yields of the tomato-saponin, esculeoside A, in the mini and middy tomatoes were found to be 0.043% and 0.046%, respectively. In order to improve the yields, we attempted a more efficient extraction using shock waves. The yields of esculeoside A were 0.0987%...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Takemoto A,Maehara H,Ohno M,Murakami Y,Itoh S,Nohara T

更新日期：2011-01-01 00:00:00

abstract：:In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) value...

journal_title：Chemical & pharmaceutical bulletin

authors： Pinna GA,Loriga G,Murineddu G,Grella G,Mura M,Vargiu L,Murgioni C,La Colla P

更新日期：2001-11-01 00:00:00

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 new monomethylated ganglioside, DSG-A (3), was obtained, together with four known gangliosides, compounds (1, 2, 4, 5), from the lipid fraction of the chloroform/methanol extract of the ovary of the sea urchin Diadema setosum. The structures of the new ganglioside was determined on the basis of chemical and spectros...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada K,Tanabe K,Miyamoto T,Kusumoto T,Inagaki M,Higuchi R

更新日期：2008-05-01 00:00:00

abstract：:A series of novel N6,N6-dialkyl adenosine 3',5'-cyclic phosphates N6,N6-dialkyl cAMPs) was synthesized from 2'-O-p-toluenesulfonyl cAMP (2'-O-tosyl cAMP, 2) and tested for inotropic and chronotropic activities in vitro. Treatment of 2 with excess alkyl halides and sodium hydride followed by detosylation with aqueous N...

journal_title：Chemical & pharmaceutical bulletin

authors： Kataoka S,Yamaji N,Kato M,Kawada T,Imai S

更新日期：1990-11-01 00:00:00

abstract：:A series of benzo[b]furan derivatives having a five-membered heterocyclic substituent at the 2-position were prepared from 2-(1-chloro-2-formylvinyl)benzo[b]furans (2) and 2-(4-alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans. These 2-heterocyclic benzo[b]furans were evaluated for their cysteinyl leukotriene receptor (cys...

journal_title：Chemical & pharmaceutical bulletin

authors： Akai Y,Tabuchi Y,Ando K,Ito A,Sakata Y,Kawasaki I,Ohishi T,Yamashita M,Ohta S,Nishide K,Ohishi Y

更新日期：2012-01-01 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：:In the previous paper, we reported the differentiation inducing activities of lignoids from Arctium Fructus (the fruits of Arctium lappa L., Compositae) against mouse myeloid leukemia cells (M1). We reinvestigated the active components of this extract and isolated three new dilignans. Furthermore, structure modificati...

journal_title：Chemical & pharmaceutical bulletin

authors： Umehara K,Nakamura M,Miyase T,Kuroyanagi M,Ueno A

更新日期：1996-12-01 00:00:00

abstract：:A series of 8-methoxy or 8-methylquinolones bearing novel 3-aminooctahydrocyclopenta[c]pyrrole derivatives at the C-7 position was synthesized, and the pharmacological, physicochemical, and toxicological properties of the individual compounds were evaluated. Novel 8-methylquinolone 7, which includes a 3-amino-7-fluoro...

journal_title：Chemical & pharmaceutical bulletin

authors： Komoriya S,Odagiri T,Inagaki H,Nagamochi M,Miyauchi R,Yoshida KI,Kitamura T,Takahashi H

更新日期：2019-01-01 00:00:00