Studies on disease-modifying antirheumatic drugs. IV. Synthesis of novel thieno[2,3-b:5,4-c']dipyridine derivatives and their anti-inflammatory effect.

abstract：:Xanthones and acridones were synthesized from 3,4-difluoronitrobenzene and 2-fluorobenzaldehydes in two or three steps. The key step was nucleophilic aroylation catalyzed by imidazolidenyl carbene. The nucleophilic aroylation of 3,4-difluoronitrobenzene afforded 2,2'-difluoro-4-nitrobenzophenones. The cyclization of t...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki Y,Toyota T,Miyashita A,Sato M

更新日期：2006-12-01 00:00:00

abstract：:Of 4-amino-5-chloro-2-methoxy-N-(1-ethyl-2-hydroxymethyl-4- pyrrolidinyl)benzamide, four optical isomers, (2S,4S)-1 (TKS159), (2S,4R)-25, (2R,4S)-26 and (2R,4R)-27, were prepared from optically active 4-amino-1-ethyl-2-hydroxymethylpyrrolidine di-p-toluenesulfonate [(2S,4S)-14, (2S,4R)-17, (2R,4S)-20 and (2R,4R)-23, r...

journal_title：Chemical & pharmaceutical bulletin

authors： Yanagi T,Kitajima A,Anzai K,Kodama K,Mizoguchi J,Fujiwara H,Sakiyama H,Kamoda O,Kamei C

更新日期：1999-11-01 00:00:00

abstract：:Cornusiin A (1), cornusiin B (2) and cornusiin C (3), new dimeric, monomeric and trimeric hydrolyzable tannins, were isolated from the fruits of Cornus officinalis (Cornaceae). Their structures, including the orientation of the valoneoyl group in 1 and 3, were established on the basis of chemical and spectroscopic dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Hatano T,Ogawa N,Kira R,Yasuhara T,Okuda T

更新日期：1989-08-01 00:00:00

abstract：:A novel series of quinoline azodyes (5-(4'-derivatives phenyldiazo)-8-hydroxy-7-quinolinecarboxaldehyde)) (HL1-HL5) has been prepared and characterized by elemental analyses, 1H-NMR and IR spectra. The IR spectral data indicate that the compounds can exist in two resonance structures. Proton-ligand dissociation consta...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Sonbati AZ,El-Bindary AA,Shoair AGF,Younes RM

更新日期：2001-10-01 00:00:00

abstract：:Acetohydroxy acid synthase (AHAS; EC 2.2.1.6, also referred to as acetolactate synthase, ALS) has been considered as an attractive target for the design of herbicides. In this work, an optimized pyrazole sulfonamide base scaffold was designed and introduced to derive novel potential AHAS inhibitors by introducing a py...

journal_title：Chemical & pharmaceutical bulletin

authors： Lv XH,Ren ZL,Liu H,Li HD,Li QS,Wang L,Zhang LS,Yao XK,Cao HQ

更新日期：2018-01-01 00:00:00

abstract：:The direct conversion of alpha-hydroxy ketones and alpha-keto oximes into quinoxaline derivatives in the presence of a catalytic amount of ceric ammonium nitrate via metal-catalyzed aerobic oxidation followed by in situ trapping with aromatic 1,2-diamines in water as a green and efficient reaction media, is reported. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Shaabani A,Maleki A

更新日期：2008-01-01 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：:From the ethyl acetate fraction of the stem bark of Camellia japonica, three new triterpenoids, 3beta-O-acetyl-16beta-hydroxy-12-oxoolean (6), 3beta-O-acetyl-16beta-hydroxy-11-oxoolean-12-ene (7), and 3beta-O-acetyl-16beta-hydroxyolean-12-ene (8), along with seven known compounds, 3alpha-hydroxy-1-oxofriedelan (1), fr...

journal_title：Chemical & pharmaceutical bulletin

authors： Thao NT,Hung TM,Lee MK,Kim JC,Min BS,Bae K

更新日期：2010-01-01 00:00:00

abstract：:A series of 5-(4-aryl- or 4-arylcarbonylpiperazin-1-yl)-5-deoxy-1,4: 3,6-dianhydro-L-iditol 2-nitrates was prepared in order to obtain orally active, nitrate-type vasodilators with reduced side effects. Our drug design was based on a small reduction in the lipophilicity compared to that of 5-deoxy-5-[4-(3-phenylthiopr...

journal_title：Chemical & pharmaceutical bulletin

authors： Hayashi H,Ikeda J,Kubo K,Moriyama T,Karasawa A,Suzuki F

更新日期：1993-06-01 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：:A 2,2'-[2,3-naphthylenebis(oxy)]-bis(N,N-diisopropyl(acetamide)) ligand (L) and its Gd(III) complex have been prepared and characterized. The crystal and molecular structure of the complex was determined by single-crystal X-ray diffraction. The interactions of complex with calf thymus DNA were investigated by UV-vis, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei K,Liu W,Huang X,Wang D

更新日期：2006-08-01 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：:The methanolic extracts from the wood and bark of Cotylelobium melanoxylon were found to inhibit plasma glucose elevation after sucrose loading in rats and triglyceride elevation after olive oil loading in mice. A new stilbene dimer, melanoxylin A, together with the known stilbene dimers [(+)-ampelopsin F, (+)-isoampe...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuda H,Asao Y,Nakamura S,Hamao M,Sugimoto S,Hongo M,Pongpiriyadacha Y,Yoshikawa M

更新日期：2009-05-01 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：:We designed and synthesized a new class of peptidomimetic human immunodeficiency virus protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl isostere as the active moiety. From a structure-activity relatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimoto T,Hattori N,Takaku H,Kisanuki S,Fukazawa T,Terashima K,Kato R,Nojima S,Misawa S,Ueno T,Imai J,Enomoto H,Tanaka S,Sakikawa H,Shintani M,Hayashi H,Kiso Y

更新日期：2000-09-01 00:00:00

abstract：:A series of [2-(omega-phenylalkyl)phenoxy]alkylamines was synthesized and their 5-hydroxytryptamine2 (5-HT2) and/or dopamine2 (D2) receptor antagonistic activities were examined in vitro. [2-(4-Phenylbutyl)phenoxy]alkylamines showed strong inhibition of both 5-HT2 and D2 receptors. In particular, [2-(4-Phenylbutyl)phe...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka N,Goto R,Ito R,Hayakawa M,Ogawa T,Fujimoto K

更新日期：1998-04-01 00:00:00

abstract：:Anion-exchange resins modified with metal-porphine (M-Pr) have been investigated to develop a solid catalyst in the oxidative reaction of phenols by O2 in air. Co-Pr, which is easily prepared and separable from the reaction mixture, has been proved to accelerate the oxidative reaction of phenols such as 3,5-di-tertbut...

journal_title：Chemical & pharmaceutical bulletin

authors： Iwado A,Mifune M,Kato J,Oda J,Chikuma M,Motohashi N,Saito Y

更新日期：2000-11-01 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：: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：:Three new carotenoids with a 3-methoxy-5-keto-5,6-seco-4,6-cyclo-beta end group (1-3) have been isolated from the seeds of Pittosporum tobira. Their structures were elucidated by detailed analyses of nuclear magnetic resonance and UV data. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujiwara Y,Maruwaka H,Toki F,Hashimoto K,Maoka T

更新日期：2001-08-01 00:00:00

abstract：:We have engineered a novel, non-viral, multifunctional gene vector (STR-CH(2)R(4)H(2)C) that contained stearoyl (STR) and a block peptide consisting of Cys (C), His (H), and Arg (R). STR-CH(2)R(4)H(2)C can form a stable nano-complex with plasmid DNA (pDNA) based on electronic interactions and disulfide cross linkages....

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Kanazawa T,Ogawa T,Suda Y,Takashima Y,Fukuda T,Okada H

更新日期：2011-01-01 00:00:00

abstract：:We describe herein a manganese(IV) oxide-mediated oxidation of N-p-methoxyphenyl (PMP)-protected glycine derivatives for the synthesis of α-imino carboxylic acid derivatives. Using this methodology, utilization of unstable glyoxic acid derivatives was avoided. Furthermore, using this methodology we synthesized novel α...

journal_title：Chemical & pharmaceutical bulletin

authors： Inokuma T,Jichu T,Nishida K,Shigenaga A,Otaka A

更新日期：2017-01-01 00:00:00

abstract：:The purpose of the present study was to determine the thermodynamic stability orders of co-crystals by co-crystal former (CCF) exchange reactions. Caffeine (CA) was employed as a model drug. The CCF exchange reaction was performed by liquid-assisted grinding using ethanol. When oxalic acid (OX) was added to CA-citric ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mukaida M,Sugano K,Terada K

更新日期：2015-01-01 00:00:00

abstract：:Chlorpheniramine (CPM) maleate was prepared as a series of resinates by the batch method. The several resinates were investigated by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and infrared (IR) spectrometry. The results from DSC and XRPD showed that the molecular state of the entrapped dr...

journal_title：Chemical & pharmaceutical bulletin

authors： Akkaramongkolporn P,Yonemochi E,Terada K

更新日期：2000-02-01 00:00:00

abstract：:Based on the result of X-ray crystallographic analysis of our peroxisome proliferator-activated receptor alpha and delta (PPARalpha/delta) co-agonist complexed with human PPAR ligand binding domain (LBD), we designed and synthesized an optically active fluorescent PPARalpha/delta co-agonist, which has a pyrene unit in...

journal_title：Chemical & pharmaceutical bulletin

authors： Araya Y,Kasuga J,Toyota K,Hirakawa Y,Oyama T,Makishima M,Morikawa K,Hashimoto Y,Miyachi H

更新日期：2008-09-01 00:00:00

abstract：:During a search for novel, orally-active inhibitors of upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1), we found a new series of 10H-pyrazino[2,3-b][1,4]benzothiazine derivatives to be potent ICAM-1 inhibitors. Of these compounds, N-[1-(10H-Pyrazino[2,3-b][1,4]benzothiazin-8-ylmet...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaneko T,Clark RS,Ohi N,Kawahara T,Akamatsu H,Ozaki F,Kamada A,Okano K,Yokohama H,Muramoto K,Ohkuro M,Takenaka O,Kobayashi S

更新日期：2002-07-01 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：:Novel hybrid L-ascorbic acid (vitamin C) derivatives with other biologically active substances, 5-hydroxy-2-hydroxymethyl-beta-pyrone (kojic acid) and alpha-tocopherol (vitamin E), linked at the C-2 or C-3 hydroxyl group were synthesized, and their thermal stability and inhibitory effects on tyrosinase activity, activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morisaki K,Ozaki S

更新日期：1996-09-01 00:00:00

abstract：:Eight new guaipyridine sesquiterpene alkaloids, rupestines F-M (1-8) were isolated from the leaves of Artemisia rupestris and their structures were elucidated on the basis of 2D-NMR data. The absolute configurations of 1-8 have been assigned by comparison of their experimental and calculated circular dichroism (CD) sp...

journal_title：Chemical & pharmaceutical bulletin

authors： He F,Nugroho AE,Wong CP,Hirasawa Y,Shirota O,Morita H,Aisa HA

更新日期：2012-01-01 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