Studies on antibacterial agents. III. Synthesis and antibacterial activities of substituted 1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acids.

abstract：:From the bark of Cryptomeria japonica were isolated sugikurojins I (1) and J (2), and an abietane derivative (3) was obtained for the first time as a natural product. These structures were elucidated primarily through extensive NMR experiments. Sugikurojin I (1) has a unique skeleton incorporating an abietane diterpen...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa K,Suzuki K,Umeyama A,Arihara S

更新日期：2006-04-01 00:00:00

abstract：:A novel series of 2-acyl-3-carboxyl-tetrahydroisoquinoline derivatives were synthesized and biologically evaluated. Among them, (S)-2-{(E)-3-furan-2-ylacryloyl}-7-[(2E,4E)-5-(2,4,6-trifluorophenyl)penta-2,4-dienyloxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (compound 17u) was identified as a potent protein ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Morishita K,Shoji Y,Fukui M,Ito Y,Kitao T,Ozawa SI,Hirono S,Shirahase H

更新日期：2018-01-01 00:00:00

abstract：:A HPLC method for the simultaneous determination of 11 triterpene saponins with four-type aglycones (protopanaxadiol, protopanaxatriol, ocotillol and oleanolic acid types) in Ginseng drugs was developed and validated. Using a gradient of acetonitrile and 10 mM K-phosphate buffer (pH 5.80) as the mobile phase and UV de...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhu S,Zou K,Cai S,Meselhy MR,Komatsu K

更新日期：2004-08-01 00:00:00

abstract：:Nitroxyl (HNO), a one-electron-reduced form of nitric oxide, has various biological activities, including a cardioprotective effect. Here, we first synthesized another, more hydrophilic photocontrollable HNO donor (3), which can release HNO in a spatially and temporally controlled manner, and then examined the propert...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuo K,Nakagawa H,Adachi Y,Kameda E,Aizawa K,Tsumoto H,Suzuki T,Miyata N

更新日期：2012-01-01 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：:Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi S,Kojima T,Hashimoto K,Saito B,Sumi H,Ishikawa T,Ikeda Y

更新日期：2015-01-01 00:00:00

abstract：:Analytical studies were carried out, for the first time, to evaluate the use of N-bromosuccinimide (NBS) as an analytical reagent for the spectrophotometric determination of eleven therapeutically important fluoroquinolone antibiotics (FQA). The procedures involved the reaction of the FQA with NBS and subsequent measu...

journal_title：Chemical & pharmaceutical bulletin

authors： Askal H,Refaat I,Darwish I,Marzouq M

更新日期：2007-11-01 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：:N-Nitrosodialkylamines are alkylating carcinogens which are metabolically activated to alpha-hydroxy nitrosamines through oxidative dealkylation by cytochrome P450. In this study, the dealkylation step in the activation of N-nitrosodibenzylamine (NDBz) was investigated with metalloporphyrin/oxidant model systems under...

journal_title：Chemical & pharmaceutical bulletin

authors： Okochi E,Mochizuki M

更新日期：1995-12-01 00:00:00

abstract：:The purpose of this research is to investigate the applicability of terahertz (THz) reflectance spectroscopy for quantification of drug substance in tablets, so as to demonstrate the feasibility for applying this technique to tableting process monitoring. In order to acquire a suitable absorbance spectrum for this pur...

journal_title：Chemical & pharmaceutical bulletin

authors： Hisazumi J,Watanabe T,Suzuki T,Wakiyama N,Terada K

更新日期：2012-01-01 00:00:00

abstract：:In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have...

journal_title：Chemical & pharmaceutical bulletin

authors： Yi W,Cao R,Chen Z,Yu L,Wen H,Yan Q,Ma L,Song H

更新日期：2010-05-01 00:00:00

abstract：:5,15-Unsymmetrically disubstituted and beta-unsubstituted porphyrins such as 5-R, 15-(3,5-dimethoxyphenyl) porphyrins [where R=2-benzyloxy-1-naphthyl (1), 2-(2-naphthylmethoxy)-1-naphthyl (2), anthryl (3), or 2,4,6-triphenylphenyl (4)] and 5-(2-benzyloxy-1-naphthyl), 10,15,20-tri(3,5-dimethoxyphenyl) porphyrin (1') we...

journal_title：Chemical & pharmaceutical bulletin

authors： Tohara A,Sato M

更新日期：2008-07-01 00:00:00

abstract：:A one-pot conversion of allyl alcohols into selenochroman derivatives was achieved by treatment with a phenyl trimethylsilyl selenide (TMSSePh)-AIBr3 reagent system. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe H,Yamasaki A,Koshiba N,Takeuchi Y,Harayama T

更新日期：2001-09-01 00:00:00

abstract：:Melt pelletization of lactose 450 M was carried out in an 8-l high shear mixer using PEG 3000 as the meltable binder. The pore size and size distribution of the melt pellets were determined using mercury intrusion porosimetry. The pore size distribution of melt pellets was found to be bimodal. With a higher binder con...

journal_title：Chemical & pharmaceutical bulletin

authors： Wong TW,Chan LW,Heng PW

更新日期：2000-11-01 00:00:00

abstract：:In an investigation of a new class of deoxyribonucleic acid (DNA)-intercalating antitumor agents, novel acridinyl-substituted uracils have been synthesized and evaluated for activity against L1210 leukemia in vivo, and against bacteria and fungus. These compounds were prepared by the novel enamine reaction between 9-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Kimura M,Okabayashi I,Kato A

更新日期：1989-03-01 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：:The relationship between the product patterns and the configurations of 1,2-cycloheptane- and 1,2-cyclooctanediols 9 in the cyclocondensations with oxalyl chloride in the presence of triethylamine at 0 degrees C has been shown analogous to that obtained for 1,2-disubstituted acyclic ethylene glycols 1: cis-1,2-cyclooc...

journal_title：Chemical & pharmaceutical bulletin

authors： Itaya T,Iida T,Natsutani I,Ohba M

更新日期：2002-01-01 00:00:00

abstract：:Manidipine dihydrochloride or benidipine hydrochloride will change to hydrate form in part, when differential scanning calorimetric (DSC) measurement is carried out together with lactose monohydrate. This interaction was accelerated by compressing their mixture. It can be suggested that the interaction may cause by th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hosaka S,Sato M,Ozawa Y,Hamada C,Takahashi Y,Kitamori N

更新日期：2005-05-01 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：:We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Hirono S

更新日期：2019-01-01 00:00:00

abstract：:Mycalamide A and mycalamide B, isolated as antiviral and antitumor agents from a New Zealand sponge of the genus Mycale, converted the morphology of ras-transformed NRK-cells to normal morphology at 10 and 1 ng/ml, respectively. The effect on protein synthesis suggests that these agents converted the morphology by pre...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawara H,Higashi K,Uchino K,Perry NB

更新日期：1991-08-01 00:00:00

abstract：:Tumor necrosis factor related apoptosis-inducing ligand (TRAIL) has emerged as a promising anticancer agent as it selectively kills cancer cells. However, TRAIL resistance limits its use as a therapeutic agent. An understanding the mechanisms responsible for TRAIL resistance and strategies to overcome it are important...

journal_title：Chemical & pharmaceutical bulletin

authors： Ahmed F,Ishibashi M

更新日期：2016-01-01 00:00:00

abstract：:Structural optimization of 2-aminonicotinamide derivatives as ghrelin receptor inverse agonists is reported. So as to avoid mechanism-based inactivation (MBI) of CYP3A4, 1,3-benzodioxol ring of the lead compound was modified. Improvement of the main activity and lipophilicity was achieved simultaneously, leading to co...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi B,Funami H,Shibata M,Maruoka H,Koyama M,Kanki S,Muto T

更新日期：2015-01-01 00:00:00

abstract：:The title compound, PNU-97018 [systemic name: 2-butyl-3,6,7,8,9,11-hexahydro-6,9-dimethyl-3-([2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl)-6,9-ethano-4H-imidazo[4,5-d]-pyridazino[1,2-a]pyridazin-4-one] is a newly developed angiotensin II receptor antagonist. The compound and its methanolate and ethanolate were ch...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishii H,Yamaguchi K,Seki H,Sakamoto S,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2002-08-01 00:00:00

abstract：:The regioselective intramolecular 1,3-dipolar cycloaddition of the phenylsulfonylallene-nitrone derivatives has been developed. This reaction showed that the distal double bond of the allene exclusively reacted with the nitrone group to produce the bicyclic isoxazolidine derivatives regardless of the substitution patt...

journal_title：Chemical & pharmaceutical bulletin

authors： Inagaki F,Kobayashi H,Mukai C

更新日期：2012-01-01 00:00:00

abstract：:A new resveratrol dimer and a new C-glucosyl resveratrol were isolated from stem wood of Hopea utilis along with nine stilbenoid derivatives comprising bergenin and (+)-lyoniresinol. The structures have been elucidated on the basis of the spectroscopic evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka T,Ito T,Ido Y,Nakaya K,Iinuma M,Chelladurai V

更新日期：2001-06-01 00:00:00

abstract：:Clotrimazole (CT)-containing proliposomes were prepared by penetrating an ethanol solution of CT and Egg phosphatidylcholine (PC) into microporous sorbitol particles, followed by vacuum evaporation of the solvent. As a result, CT proliposomes with free-flowing flowability were obtained. On contact with water, the prol...

journal_title：Chemical & pharmaceutical bulletin

authors： Ning MY,Guo YZ,Pan HZ,Yu HM,Gu ZW

更新日期：2005-06-01 00:00:00

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：:The dissolution of oval soft gelatin capsules containing 5 mg of nifedipine dissolved in a water soluble vehicle was evaluated by the rotating dialysis cell (RDC) method and the paddle (PD) method as described in the Japanese Pharmacopoiea (JP) XI. The dissolution pattern of nifedipine obtained by the PD method was li...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi M,Mochizuki M,Itoh T,Ohta M

更新日期：1994-02-01 00:00:00

abstract：:A new lanostane-type triterpene, 29-hydroxypolyporenic acid C (8), was isolated from the dried sclerotia of Poria cocos together with eight other known compounds pachymic acid (1), dehydropachymic acid (2), 3-acetyloxy-16alpha-hydroxytrametenolic acid (3), polyporenic acid C (4), 3-epi-dehydropachymic acid (5), 3-epi-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou L,Zhang Y,Gapter LA,Ling H,Agarwal R,Ng KY

更新日期：2008-10-01 00:00:00