Identification of indoline-2-thione analogs as novel potent inhibitors of α-melanocyte stimulating hormone induced melanogenesis.

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：:Two new synthetic methods were established for the efficient synthesis of optically active cyclohexene antisepsis agent, ethyl (6R)-6-[N-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate [(R)-1: TAK-242)]. The first method involved recrystallization from methanol of the diastereomeric mixture (6RS,1'R)-7...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada M,Ichikawa T,Yamano T,Kikumoto F,Nishikimi Y,Tamura N,Kitazaki T

更新日期：2006-01-01 00:00:00

abstract：:2-(5-Arylidene-4-oxo-3-phenyl-thiazolidin-2-ylidene)-3-oxo-propionitriles 4a-j were prepared via condensation of aromatic aldehydes with 4-thiazolidinones 3a,b. The latter was obtained via electrophilic attack of phenylisothiocyanate on 3-oxo-propionitriles 1a,b followed by reaction with chloroacetyl chloride under ba...

journal_title：Chemical & pharmaceutical bulletin

authors： Hanna MM,George RF

更新日期：2012-01-01 00:00:00

abstract：:We synthesize optically active (R)-terbutaline 2, which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of...

journal_title：Chemical & pharmaceutical bulletin

authors： Uchimoto H,Ikeda M,Tanida S,Ohhashi K,Chihara Y,Shigeta T,Arimitsu K,Yamashita M,Nishide K,Kawasaki I

更新日期：2017-01-01 00:00:00

abstract：:The absorption of insulin (from porcine pancreas) from the rectum of rabbits after the administration of hollow-type suppositories containing insulin and five kinds of cyclodextrins (CyDs) was investigated. Three types of suppositories were employed: suppository I containing insulin (approximately 26 IU/mg) and variou...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe Y,Matsumoto Y,Seki M,Takase M,Matsumoto M

更新日期：1992-11-01 00:00:00

abstract：:From Puerariae Radix, the root of Pueraria lobata (Leguminosae), six new oleanene-type triterpene glycosides, called kudzusaponins A1 (1), A2 (2), Ar (3), SA4 (5), and SB1 (6) were isolated together with kudzusaponin A3 (7), soyasaponins SA3 (8), and I (9). The structures of 1-6 were determined to be 3-O-alpha-L-rhamn...

journal_title：Chemical & pharmaceutical bulletin

authors： Arao T,Kinjo J,Nohara T,Isobe R

更新日期：1997-02-01 00:00:00

abstract：:A new spiroketallactone, epi-danshenspiroketallactone A (1) and a new C18-norditerpenoid, normiltioane (2) along with 21 known compounds, were isolated from cell cultures of Salvia miltiorrhiza. Their structures were elucidated on the basis of extensive spectroscopic analyses. In the in vitro assays, the compounds 9-1...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang DW,Liu X,Xie D,Chen R,Tao XY,Zou JH,Dai J

更新日期：2013-01-01 00:00:00

abstract：:The structures of new neo-lignans, isoamericanol A (1) and americanol A (2) isolated from the seeds of Phytolacca americana have been elucidated on the basis of spectroscopic data and then confirmed by chemical correlation with the previously known isoamericanin A (3) and americanin A (4). Isoamericanol A, americanol ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Hasegawa T,Toda M,Kodama M,Okazaki H

更新日期：1992-01-01 00:00:00

abstract：:Novel sialosyl donors, 4-pentenoic acid ester of N-acetylneuraminic acids (Neu5Ac) and 4-pentenyl glycoside of Neu5Ac were successfully prepared from the corresponding per-O-acetylated 2-hydroxy and 2-chloro derivatives of Neu5Ac, respectively and applied to the synthesis of O-sialosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda K,Fukuyo J,Sato K,Sato M

更新日期：2005-11-01 00:00:00

abstract：:A series of substituted 4-oxoquinoline-3-carboxylic acids having a methyl group at the 8-position was prepared and tested for their antibacterial activity. 7-(trans-3-Amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-1,4-dihydro-6- fluoro-8-methyl-4-oxoquinoline-3-carboxylic acid (21) exhibited highly potent antibacterial ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyamoto H,Ueda H,Otsuka T,Aki S,Tamaoka H,Tominaga M,Nakagawa K

更新日期：1990-09-01 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：:The amount of adsorption of bovine serum albumin (BSA) by hydroxyapatite (HAP) increased with a concentration of CaCl2 due to the bridging effect of Ca2+ between adsorbate BSA and adsorbent HAP. On the other hand, it decreased remarkably with a concentration of K2HPO4. This was explained in terms of the effects of ion...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimabayashi S,Tanizawa Y,Ishida K

更新日期：1991-09-01 00:00:00

abstract：:A series of 43 stilbene derivatives that showed cytotoxicity against human lung carcinoma (A549) was analyzed using comparative molecular field analysis (CoMFA) for defining the hypothetic pharmacophore model. The polyoxylated stilbenes were found to be active inhibitors of tubulin polymerization. Several cis-stilbene...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim S,Min SY,Lee SK,Cho WJ

更新日期：2003-05-01 00:00:00

abstract：:The decomposition products and mutagenic activity in Salmonella typhimurium strains TA98, TA100 and TA104 in the presence and absence of S9 mix of linear dodecylbenzenesulfonate (DBS) in aqueous solution after ozone treatment alone or simultaneous treatment with ozone and ultraviolet (UV) irradiation (ozone/UV treatme...

journal_title：Chemical & pharmaceutical bulletin

authors： Murakami K,Matsumoto H,Kinouchi T,Ohnishi Y

更新日期：1992-06-01 00:00:00

abstract：:Jellies for oral administration are dosage forms that contain water, as stipulated in the Japanese Pharmacopeia, and heat is generally applied to the jellies during the manufacturing process. Therefore, it is difficult to formulate drugs that may be affected adversely by water and/or heat. To solve this problem, we tr...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakino Y,Hishikawa Y,Onodera R,Tahara K,Takeuchi H

更新日期：2017-01-01 00:00:00

abstract：:Herein we report the development of novel, potent and non-peptide luteinizing hormone releasing hormone (LHRH) antagonists. The optimization towards derivatives free from mechanism-based CYP3A4 inhibition is described. The identification of a main metabolite guided us towards structural modifications of the benzyl moi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hashimoto K,Kataoka M,Tatsuta M,Yasoshima K,Yamamoto M,Yura T,Yamamoto N,Urbahns K,Gupta JB,Li Y

更新日期：2005-10-01 00:00:00

abstract：:Sixteen derivatives of 1-(beta-D-arabinofuranosyl)-2-thiocytosine (araSC), including five 5'-esters, three 3'-esters, five N4-amides and three 5'-phosphodiesters, were synthesized and their reactivity to mouse tissue homogenates, including plasma, liver and intestine, and antitumor activity in mice bearing P388 cells ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawaguchi T,Ichikawa T,Hasegawa T,Saneyoshi M,Wakayama T,Kato H,Yukita A,Nagata T

更新日期：2000-04-01 00:00:00

abstract：:In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-(spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Kakefuda A,Nagaoka H,Yamamoto O,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:Microdialysis sampling method coupled to high-performance liquid chromatography with UV detection was applied to continuous monitoring of in vivo unbound flomoxef concentration in rat blood. By comparison with ultrafiltration method, it was demonstrated that it gave reliable results for the unbound drug monitoring in ...

journal_title：Chemical & pharmaceutical bulletin

authors： Saisho Y,Umeda T

更新日期：1991-03-01 00:00:00

abstract：:A series of N-(trifluoromethyl-2-pyridinyl)alkane- and arenesulfonamides 2-5 have been synthesized by the substitution reaction of 2-chloro(trifluoromethyl)pyridines 6 with alkane- and arenesulfonamides 7. Their inhibitory activities against secretory phospholipase A₂ of porcine pancreas were examined and the analog N...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakayama H,Morita Y,Kimura H,Ishihara K,Akiba S,Uenishi J

更新日期：2011-01-01 00:00:00

abstract：:The crystal of bovine trypsin complexed with a potent inhibitor, 4-[4-(N,N- dimethylcarbamoylmethoxycarbonylmethyl)phenoxycarbonylphenyl ]guanidinium (FOY-305) in the novel orthorhombic from with a low molecular packing density was studied by the X-ray diffraction method. Using synchrotron radiation, the intensity dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto O,Taga T,Matsushima M,Higashi T,Machida K

更新日期：1990-08-01 00:00:00

abstract：:A new glucocerebroside, linckiacerebroside A (1) and a known glucocerebroside S-2a-3 (2), have been isolated from the cerebroside molecular species obtained from the less polar fraction of the CHCl3/MeOH extract of the starfish Linckia laevigata, together with three pseudo homogeneous glucocerebroside, 3, 4, and 5. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Maruta T,Saito T,Inagaki M,Shibata O,Higuchi R

更新日期：2005-10-01 00:00:00

abstract：:The pharmacokinetic profiles of the hypoglycemic agent, acetohexamide (AH) and its major active metabolite, hydroxyhexamide (HH) were studied in three species of laboratory animals after intraperitoneal (ipl) administration in comparison with those after intravenous (iv) administration of AH and of the preformed metab...

journal_title：Chemical & pharmaceutical bulletin

authors： Asada S,Nagamine S,Nakae H

更新日期：1989-03-01 00:00:00

abstract：:Ten biscembranoids (1-10), including the two new compounds sarcophytolides M and N (1 and 2), were isolated from the methanol extract of the Vietnamese soft coral Sarcophyton pauciplicatum. Their structures were elucidated by spectroscopic methods including one dimensional (1D)- and 2D-NMR, high-resolution electrospra...

journal_title：Chemical & pharmaceutical bulletin

authors： Nam NH,Tung PT,Ngoc NT,Hanh TT,Thao NP,Thanh NV,Cuong NX,Thao do T,Huong TT,Thung do C,Kiem PV,Kim YH,Minh CV

更新日期：2015-01-01 00:00:00

abstract：:A series of benzylamides of N-alkylated, N-acylated or free nine cyclic and one linear amino acids as potential anticonvulsants have been synthesized. The structures of the obtained compounds were designed on the basis of the previously determined structure and physicochemical properties/anticvonvulsant activity relat...

journal_title：Chemical & pharmaceutical bulletin

authors： Paruszewski R,Strupińska M,Stables JP,Swiader M,Czuczwar S,Kleinrok Z,Turski W

更新日期：2001-05-01 00:00:00

abstract：:Two new friedelane-type triterpenes named 12alpha-hydroxyfriedelane-3,15-dione and 3beta-hydroxyfriedelan-25-al, together with six known compounds were isolated from the stems of Drypetes paxii Hutch. (Euphorbiaceae). Their structures were established on the basis of conventional 1 dimensional (1D) NMR methods, 2D shi...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiozem DD,Trinh-Van-Dufat H,Wansi JD,Mbazoa Djama C,Fannang VS,Seguin E,Tillequin F,Wandji J

更新日期：2009-10-01 00:00:00

abstract：:From the quaternary alkaloidal fraction of the dried tubers of Stephania cepharantha, two new isoquinoline alkaloids, stecepharine and tetradehydroreticuline have been isolated along with the known compounds, magnoflorine, menisperine, steponine, cyclanoline, oblongine, cis-N-methylcapaurine and 2'-N-methylisotetrandr...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanahashi T,Su U,Nagakura N,Nayeshiro H

更新日期：2000-03-01 00:00:00

abstract：:This study reports the results of applying the time-temperature superposition principle (TTSP) to the prediction of color changes in liquid formulations. A sample solution consisting of L-tryptophan and glucose was used as the model liquid formulation for the Maillard reaction. After accelerated aging treatment at ele...

journal_title：Chemical & pharmaceutical bulletin

authors： Mochizuki K,Takayama K

更新日期：2014-01-01 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：:The generation of a different type of beta-kallikrein, designated C beta-kallikrein, from alpha-kallikrein by chymotryptic action was ascertained by the following observations: 1) When alpha-kallikrein was incubated with chymotrypsin, an increase of esterolytic activity of kallikrein was observed. 2) In sodium dodecyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Kamada M,Ikekita M,Kurahashi T,Aoki K,Kizuki K,Moriya H,Sweeley CC,Kamo M,Tsugita A

更新日期：1990-04-01 00:00:00