Synthesis and structure-activity relationships of thienylcyanoguanidine derivatives as potassium channel openers.

abstract：:Enzymatic functions are often altered during disease onset and progression, and therefore chemical-biological studies, which utilize chemical knowledge to discover novel protein functions, are often employed to find proteins with functions closely related to disease phenotypes. Such studies are known as forward chemic...

journal_title：Chemical & pharmaceutical bulletin

authors： Komatsu T

更新日期：2017-01-01 00:00:00

abstract：:It has been indicated that hydrophilic solid powder to which aqueous solution of a novel dehydrocondensing reagent DMT-MM is adsorbed becomes a simple solid-phase dehydrocondensing reagent of low cost. Reaction in a liquid--liquid biphasic system on the surface of a solid phase with a large area was accelerated by sus...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe Y,Fuji T,Hioki K,Tani S,Kunishima M

更新日期：2004-10-01 00:00:00

abstract：:Increase of lipophilicity of cationic doxorubicin (DOX) by its association with a fatty acid ion is of interest for pharmaceutical formulations and could have an impact on the drug delivery into cancer cells. On the basis of spectroscopic analysis of intrinsic DOX fluorescence, this study provides an experimental evid...

journal_title：Chemical & pharmaceutical bulletin

authors： Munnier E,Tewes F,Cohen-Jonathan S,Linassier C,Douziech-Eyrolles L,Marchais H,Soucé M,Hervé K,Dubois P,Chourpa I

更新日期：2007-07-01 00:00:00

abstract：:The tumor microenvironment is considered as one of the important targets for anticancer drug discovery. In particular, nutrient deficiency may be observed in tumor microenvironment; biakamides A-D (1-4) isolated from marine sponge Petrosaspongia sp. as growth inhibitors against cancer cells adapted to glucose-deprived...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida R,Matsumoto H,Ichii S,Kobayashi M,Arai M,Kotoku N

更新日期：2019-03-01 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：:Polyamines, especially spermine, inhibit N-methyl-D-aspartate (NMDA) receptors as open channel blockers. Two types of water-soluble NMDA receptor antagonist, ACCn (1) and TGCn (2), with a 1,4,7,10-tetraazacyclododecane cyclic polyamine group, were synthesized and the effects of both compounds on NMDA receptors were st...

journal_title：Chemical & pharmaceutical bulletin

authors： Masuko T,Metori K,Kizawa Y,Kusama T,Miyake M

更新日期：2005-04-01 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：: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：:The Pictet-Spengler reaction of tryptamine type 1,2-dihydropyridine 5c derived from the cycloaddition of the sec-nitrodienamine 3c with acetaldehyde afforded the indoloquinolizine derivatives 6 and 7. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koike T,Shinohara Y,Tobinaga S,Takeuchi N

更新日期：2000-12-01 00:00:00

abstract：:Peptides mimicking chemokine receptor CCR5 were synthesized and their anti-HIV-1 activities evaluated. Prepared compounds, especially a sulfated derivatives, showed significant anti-HIV-1 activities. Furthermore, a hybrid molecule linked to an N-carbomethoxycarbonyl-prolyl-phenylalanine (CPF) moiety had a greater effe...

journal_title：Chemical & pharmaceutical bulletin

authors： Konishi K,Ikeda K,Achiwa K,Hoshino H,Tanaka K

更新日期：2000-02-01 00:00:00

abstract：:A series of 2-(4-methylphenyl)benzothiazoles was synthesized and evaluated using an adjuvant-induced arthritic rat model. This class of desired compounds affecting the immune response was found using hemagglutination assay. 4-Acetoxy-2-(4-methylphenyl)benzothiazole (7m), KB-2683, was most potent in the adjuvant-induce...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori N,Tsukamoto G,Imamura A,Ohashi M,Saito T,Yoshino K

更新日期：1992-09-01 00:00:00

abstract：:The synthesis and structure-activity relationships of a series of new azabicycloalkanes as 5-HT3 (serotonin-3) receptor antagonists are described. Our study on the azabicycloalkaneacetamide derivatives showed that 2,3-dihydroindole as the aromatic ring moiety afforded potent 5-HT3 receptor antagonist activity, as judg...

journal_title：Chemical & pharmaceutical bulletin

authors： Kato M,Ito K,Nishino S,Yamakuni H,Takasugi H

更新日期：1995-08-01 00:00:00

abstract：:Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lo...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

更新日期：2016-01-01 00:00:00

abstract：:Caragana tibetica KOM. (Fabaceae) is a medicinal plant that has been traditionally used in western part of China. In the course of our screening study on antioxidant activity of medicinal plants, the 70% acetone extract of the stems of C. tibetica was found to have a potent superoxide anion scavenging activity. Tibeti...

journal_title：Chemical & pharmaceutical bulletin

authors： Xiang T,Uno T,Ogino F,Ai C,Duo J,Sankawa U

更新日期：2005-09-01 00:00:00

abstract：:We found a strong paraoxon-hydrolyzing activity (23.4 +/- 8.50 nmol/h/individual and 137 +/- 86.2 nmol/h/mg protein) in the crude extract from larvae of Culex tritaeniorhynchus Toyama 89, which is markedly resistant to organophosphorous insecticides. The activity was higher than those from Cx. tritaeniorhynchus re-e-a...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe M,Takebe S,Kobashi K

更新日期：1991-04-01 00:00:00

abstract：:The intercalation reaction of diclofenac sodium (DFS) with layered inorganic compounds, gamma-titanium phosphate (gamma-TiP), proton type titanium oxide (H-TiO2) and sodium type synthetic mica (Na-TSM), was examined on. The direct reaction of DFS in ethanol-water mixed solvent resulted in the large amount accommodatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Tajima T,Suzuki N,Watanabe Y,Kanzaki Y

更新日期：2005-11-01 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：:Seven antioxidative serotonin derivatives were isolated from safflower (Carthamus tinctorius L.) oil cake. Their structures were established as N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]ferulamide (1), N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-p-coumaramide (2), N,N'-[2,2'-(5,5'-dihydroxy-4,4'-bi-1H-indol-3,3'-yl)diethyl]- di-p-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang HL,Nagatsu A,Watanabe T,Sakakibara J,Okuyama H

更新日期：1997-12-01 00:00:00

abstract：:The aim of this study was to fabricate deformable chitosan (CS) microspheres for arterial embolization. CS microspheres containing poly(ethylene glycol) (PEG) were prepared by ionotropic gelation; PEG was then removed from the CS microspheres to produce the highly porous structure to allow deformability. The porosity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kang MJ,Park JM,Choi WS,Lee J,Kwak BK,Lee J

更新日期：2010-03-01 00:00:00

abstract：:A high-performance liquid chromatographic (HPLC) method for the determination of ornithine conjugation of some carboxylic acids in vitro has been developed. The ornithine conjugates of benzoic acid, p-nitrobenzoic acid, furancarboxylic acid and phenylacetic acid in an incubation mixture with kidney mitochondria were w...

journal_title：Chemical & pharmaceutical bulletin

authors： Igarashi K,Suzuki R,Kasuya F,Fukui M

更新日期：1992-08-01 00:00:00

abstract：:From the Fresh leaves of Hovenia dulcis Thunb. var. tomentella Makino, five five new dammarane glycosides named hodulosides VI-X (1-5) were isolated. Their structures were determined on the basis of chemical and spectral evidence. Hodulosides VII-X showed antisweet activities. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa K,Nagai Y,Yoshida M,Arihara S

更新日期：1993-10-01 00:00:00

abstract：:From the water extract of Brazilian Tabebuia avellanedae, two new iridoids (1, 2) and a new phenylethanoid glycoside (3) have been isolated together with twelve known compounds (4-15). Their structures were determined based on the spectroscopic data. The isolated compounds inhibited nitric oxide (NO) production in lip...

journal_title：Chemical & pharmaceutical bulletin

authors： Awale S,Kawakami T,Tezuka Y,Ueda JY,Tanaka K,Kadota S

更新日期：2005-06-01 00:00:00

abstract：:From the MeOH extract of the aerial part of Vietnamese Orthosiphon stamineus, five new isopimarane-type diterpenes [orthosiphols F-J (1-5)] and two new diterpenes [staminols A (6) and B (7)] with a novel carbon-framework, to which we proposed the name "staminane", and three new highly-oxygenated staminane-type diterpe...

journal_title：Chemical & pharmaceutical bulletin

authors： Tezuka Y,Stampoulis P,Banskota AH,Awale S,Tran KQ,Saiki I,Kadota S

更新日期：2000-11-01 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 hydrolysis of protopanaxadiol-type saponin mixture by various glycoside hydrolases was examined. Among these enzymes, crude preparations of lactase from Aspergillus oryzae, beta-galactosidase from A. oryzae, and cellulase from Trichoderma viride were found to produce ginsenoside F(2) [3-O-(beta-D-glucopyranosyl)-2...

journal_title：Chemical & pharmaceutical bulletin

authors： Ko SR,Suzuki Y,Suzuki K,Choi KJ,Cho BG

更新日期：2007-10-01 00:00:00

abstract：:A series of benzylidene 2-aminoimidazolones derivatives were synthesized. Most compounds displayed strong inhibitory activity on the proliferation of human HepG2 cells in vitro. The active compounds were further evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against five human ca...

journal_title：Chemical & pharmaceutical bulletin

authors： Ling Y,Wang ZQ,Xiao YA,Zhu C,Shen L,Wang XM,Hui Y,Wang XY

更新日期：2013-01-01 00:00:00

abstract：:Lembehsterols A (1) and B (2), two novel sulfated sterols, were isolated from the marine sponge Petrosia strongylata. Both sterols showed inhibitory activity against thymidine phosphorylase, which is an enzyme related to angiogenesis in solid tumors. The structures of these sulfated sterols were established on the bas...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoki S,Naka Y,Itoh T,Furukawa T,Rachmat R,Akiyama S,Kobayashi M

更新日期：2002-06-01 00:00:00

abstract：:Four new bicyclic hexapeptides, named as RA-XI, -XII, XIII and -XIV were isolated from Rubia cordifolia and showed potent antitumor activities against P-388. The structures were elucidated from spectroscopic and chemical evidences. RA-XII, XIII and -XIV were proved to be unique bicyclic hexapeptidic glucosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Yamamiya T,Takeya K,Itokawa H

更新日期：1992-05-01 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：:A series of aminomethylenebisphosphonate derivatives was synthesized and evaluated for their antiresorptive activities using a parathyroid hormone (PTH)-induced hypercalcemia model in rats (PIH model). Among these compounds, (cycloheptylamino)methylenebis(phosphonic acid) (3j) was finally selected for further investig...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi M,Sakamoto S,Yoshida M,Abe T,Isomura Y

更新日期：1993-04-01 00:00:00