Optically active cyclohexene derivative as a new antisepsis agent: an efficient synthesis of ethyl (6R)-6-[N-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242).

abstract：:A series of novel 3-substituted-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes in order to improve the in vitro and in vivo activity of our prototype 3-[4-(3-chlorophenyl)-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propene (2) were synthesized and evaluated by assays of growth inhib...

journal_title：Chemical & pharmaceutical bulletin

authors： Naito H,Ohsuki S,Sugimori M,Atsumi R,Minami M,Nakamura Y,Ishii M,Hirotani K,Kumazawa E,Ejima A

更新日期：2002-04-01 00:00:00

abstract：:The electrochemically oxidative lesion of the acetaldehyde-derived cyclic propano adduct 2 of 2'-deoxyguanosine 1 was identified as the cross-linked dimer 4 of adduct 2. Cross-link formation is explained by the nucleophilic preference of the exocyclic amino group in 2 to the carbocation 3 electrogenerated by 1-proton ...

journal_title：Chemical & pharmaceutical bulletin

authors： Murakami H,Esaka Y,Uno B

更新日期：2009-12-01 00:00:00

abstract：:Oligonucleotides containing a dG cluster, d(TmGnTm), are models of single-stranded parts of telomeric deoxyribonucleic acid and substitutes for poly(dG). Electrophoretic and spectroscopic analyses of the oligomers indicate that the oligomers can form two alternative structures, single- and quadruple-stranded helices, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Shida T,Yokoyama K,Tamai S,Sekiguchi J

更新日期：1991-09-01 00:00:00

abstract：:A new series of 11-substituted 6,11-dihydrodibenz[b,e]oxepin derivatives was synthesized and evaluated for antiallergic activity. Convenient methods for the preparation of sulfides from alcohols were developed. Structure-activity relationships are described. Compound 7, 11-[2-(dimethylamin)ethyl]thio-6,11-dihydrodiben...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohshima E,Kumazawa T,Takizawa H,Harakawa H,Sato H,Obase H,Oiji Y,Ishii A,Ishii H,Ohmori K

更新日期：1991-10-01 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：:Oiling-out is a unique phenomenon that the liquid phase is separated into two parts during crystallization. The emergence of new liquid phase changes the environment where crystals nucleate and grow, we call "mother phase," because target material and impurities become distributed to each phase according to their own ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Takiyama H

更新日期：2020-01-01 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：:Conferols A (1) and B (2), the new 4-hydroxyisoflavones, have been isolated from the dichloromethane sub-fraction of the methanolic extract of Caragana conferta along with 3',5'-dihydroxy, 7,4'-dimethoxyisoflavone (3), E-cinnamic acid (4), tetracosyl 3,4-dihydroxy-E-cinnamate (5), docosyl 3,4-dihydroxy-E-cinnamate (6)...

journal_title：Chemical & pharmaceutical bulletin

authors： Khan R,Malik A,Adhikari A,Qadir MI,Choudhary MI

更新日期：2009-04-01 00:00:00

abstract：:The 1-BuOH-soluble fraction of the methanol (MeOH) extract of Diospyros maritima was separated by chromatographic techniques to give three new oleanane-type and one new ursane-type triterpene glucoside, named ebenamariosides A-D (1-4); two megastigmanes were also isolated. The structures of triterpene glucosides was e...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawakami S,Miura E,Nobe A,Inagaki M,Nishimura M,Matsunami K,Otsuka H,Aramoto M

更新日期：2019-01-01 00:00:00

abstract：:New alkenyl-1,4-benzoquinones, ardisianones A (1) and B (2), and the known maesanin (3) as 5-lipoxygenase inhibitors have been isolated from the rhizome of Ardisia japonica. Their structures have been elucidated as 2-methoxy-6-[(Z)-10'-pentadecenyl]-1,4-benzoquinone and 5-hydroxy-2-methoxy-6-[(Z)-8'-tridecenyl]-1,4-be...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Kiriyama Y,Okino J,Kodama M,Iwaki H,Hosozawa S,Matsui K

更新日期：1993-03-01 00:00:00

abstract：:To reverse the adverse reactions of alkylxanthines and to develop novel inhibitors of cyclic AMP phosphodiesterase 4 (PDE4), a series of heterocycle [a]-, [b]-, [c,d]-, and [i]-condensed purines were designed and synthesized. Although all compounds did not display PDE1 and PDE3 inhibitory activities, several heterocyc...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki H,Yamamoto M,Shimura S,Miyamoto K,Yamamoto K,Sawanishi H

更新日期：2002-09-01 00:00:00

abstract：:A new 9,19-cyclolanostane-type triterpene xyloside (1), from the rhizomes of Cimicifuga racemosa, has been isolated together with four known saponins; cimiaceroside A, 25-O-methylcimigenol-3-O-beta-D-xylopyranoside, 27-deoxyactein and 23-O-acetylshengmanol-3-O-beta-D-xylopyranoside. The structure of the new compound w...

journal_title：Chemical & pharmaceutical bulletin

authors： Bedir E,Khan IA

更新日期：2000-03-01 00:00:00

abstract：:We prepared new antitumor active platinum complexes containing N,N'-bis(2-chloroethyl)ethylenediamine (ClEn) as an alkylating carrier ligand in order to obtain increased antitumor effects. Some of the platinum complexes synthesized showed enhanced antitumor activity. However, palladium(II) complexes containing ClEn we...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee K,Tashiro T,Noji M

更新日期：1994-03-01 00:00:00

abstract：:The synthesis and structure-activity-relationship (SAR) for a series of N-substituted piperazinyl carbamoyl 7-15 and piperazinyl acetyl 18-26 derivatives of tetrahydropapaverine have been carried out. The general synthetic methods of carbamoyl tetrahydropapaverine analogues involve N-substituted piperazines and carbam...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaur J,Ghosh NN,Talwar A,Chandra R

更新日期：2002-09-01 00:00:00

abstract：:Pyrrole-2,5-dicarboxylates were rapidly and selectively reduced to the corresponding mono-alcohol using 3 eq of diisobutylaluminum hydride at 0°C. Pyrrole-2,4-dicarboxylate showed the same reactivity; however, the selectivity decreased with pyrrole-3,4-dicarboxylate. When the nitrogen atom of the pyrrole-2,5-dicarboxy...

journal_title：Chemical & pharmaceutical bulletin

authors： Yasui E,Tsuda J,Ohnuki S,Nagumo S

更新日期：2016-01-01 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：:A new ent-kaurane diterpene glycoside, beta-D-glucopyranosyl 17-hydroxy-ent-kauran-19-oate-16-O-beta-D-glucopyranoside (4) was isolated from the dried leaves of Cussonia bojeri SEEM., together with four known compounds identified as 16beta,17-dihydroxy-kauran-19-oic acid (1), beta-D-glucopyranosyl 16beta,17-dihydroxy-...

journal_title：Chemical & pharmaceutical bulletin

authors： Harinantenaina L,Kasai R,Yamasaki K

更新日期：2002-08-01 00:00:00

abstract：:A new antibiotic indole trimer named trisindoline (1) was isolated, together with a known dioxopiperazine brevianamide F (2), from the culture of a bacterium of Vibrio sp., which was separated from the Okinawan marine sponge Hyrtios altum. The structure of trisindoline (1) has been determined on the bases of physicoch...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi M,Aoki S,Gato K,Matsunami K,Kurosu M,Kitagawa I

更新日期：1994-12-01 00:00:00

abstract：:Hyosgerin, a new optically active coumarinolignan, has been isolated and characterized along with three other coumarinolignans, venkatasin, cleomiscosin A and cleomiscosin B, from the seeds of Hyoscyamus niger L. The structure was determined on the basis of spectroscopic analysis and chemical conversion. The optical p...

journal_title：Chemical & pharmaceutical bulletin

authors： Sajeli B,Sahai M,Suessmuth R,Asai T,Hara N,Fujimoto Y

更新日期：2006-04-01 00:00:00

abstract：:The processing of biological raw materials is considered to have an important role in the therapeutic application in Traditional Chinese Medicine. The root of Rehmannia glutinosa has to be processed by nine cycles of rice wine immersing, steaming and drying before using in clinical applications. In order to understand...

journal_title：Chemical & pharmaceutical bulletin

authors： Chang WT,Choi YH,Van der Heijden R,Lee MS,Lin MK,Kong H,Kim HK,Verpoorte R,Hankemeier T,Van der Greef J,Wang M

更新日期：2011-01-01 00:00:00

abstract：:A series of 1,2,3,4-tetrahydroisoquinoline derivatives containing the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton were prepared and evaluated for their in vitro binding affinities to muscarinic receptors and for antagonism of bradycardia in vivo. Among them, compound 3f had the highest affinity for ...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe T,Kinoyama I,Takizawa K,Hirano S,Shibanuma T

更新日期：1999-05-01 00:00:00

abstract：:An investigation into the methanol extracts obtained from the stems of Dodonaea viscosa led to the isolation of one nor-clerodane diterpene (1) and two labdane diterpenes (2, 3), as well as 17 known compounds (4-20). The structures of these compounds were elucidated based on chemical and spectral evidence. The stereoc...

journal_title：Chemical & pharmaceutical bulletin

authors： Sagara T,Sugimoto S,Yamano Y,Nehira T,Masuda K,Otsuka H,Matsunami K

更新日期：2021-01-01 00:00:00

abstract：:Further isolation work on the water-soluble fraction of a MeOH extract of Tricalysia dubia afforded one new megastigmane gentiobioside, named tricalysionoside A (1), and three sulfates, named sulfatricalysines A-C (2-4). Extensive isolation work on the 1-BuOH-soluble fraction of a MeOH extract of T. dubia yielded sulf...

journal_title：Chemical & pharmaceutical bulletin

authors： Shitamoto J,Sugimoto S,Matsunami K,Otsuka H,Shinzato T,Takeda Y

更新日期：2011-01-01 00:00:00

abstract：:Effects of somatostatin on pepsinogen secretion was investigated in the rat in vivo and in vitro. In the perfused rat stomach, somatostatin inhibited secretagogue-induced acid secretion in dose-dependent manner. However, effects of somatostatin on secretagogue-induced pepsinogen secretion were obscure. To clarify the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tani S,Tanaka T

更新日期：1990-08-01 00:00:00

abstract：:In the course of our chemotaxonomic study of the liverworts growing in Madagascar, mastigophoric acid methyl ester, along with eleven known compounds were isolated from Mastigophora diclados. Isolated metabolites showed that the Malagasy Mastigophora is more related to the samples from Borneo and Japan than to the Tai...

journal_title：Chemical & pharmaceutical bulletin

authors： Harinantenaina L,Asakawa Y

更新日期：2004-11-01 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：: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：:We have developed a competitive enzyme immunoassay for a drug, which was a newly synthesized anti-ulcer agent, using an enzyme immunoassay. The polyclonal anti-drug antibody coupled to biotin, peroxidase labeled drug derivatives as a tracer, and a small column of Sepharose 4B covalently bound to avidin were used in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Okumura T,Asano T,Adachi T,Hirano K

更新日期：1991-07-01 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：:Snow hebes are the alpine cushion-forming plants of New Zealand Veronica, formerly classified as Chionohebe. The chemical compositions of Veronica pulvinaris and Veronica thomsonii were studied and 33 water-soluble compounds were isolated. The structures of 14 previously unknown esters of phenylethanoid glycosides wer...

journal_title：Chemical & pharmaceutical bulletin

authors： Taskova RM,Kokubun T,Ryan KG,Garnock-Jones PJ,Jensen SR

更新日期：2010-05-01 00:00:00