Stereocontrolled total synthesis of natural products with characteristic molecular structures and biological activities.

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 objective of this investigation was to clarify the influence of water-soluble polymers on the dissolution behavior of nifedipine from solid dispersions with combined carriers. All the solid dispersions of nifedipine were prepared by the fusion method using nicotinamide and 4 different water-soluble polymers, hydro...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki H,Sunada H

更新日期：1998-03-01 00:00:00

abstract：:Our aim is to test the characteristics and expression activity in brain capillary endothelial cells (BCECs) of DNA-loaded nanoparticles before and after the modification with Antennapedia peptide (Antp). Chitosan (CH), polyethylenimine (PEI) and polyamidoamine (PAMAM) were chosen to prepare the nanoparticles; Lipofect...

journal_title：Chemical & pharmaceutical bulletin

authors： Huang R,Yang W,Jiang C,Pei Y

更新日期：2006-09-01 00:00:00

abstract：:Analogues with the scaffolds of 3-cyano-4-alkoxyphenyl-6-bromoaryl-2-pyridone and 2-amino-3-cyano-4-alkoxyphenyl-6-bromoarylpyridine were synthesized. Cyclization of the 2-amino derivatives with formic acid and formamide gave the corresponding pyrido[2,3-d]pyrimidin-4(3H)-one and the pyrido[2,3-d]-pyrimidin-4-amine de...

journal_title：Chemical & pharmaceutical bulletin

authors： Abadi AH,Hany MS,Elsharif SA,Eissa AA,Gary BD,Tinsley HN,Piazza GA

更新日期：2013-01-01 00:00:00

abstract：:An effective procedure for decontamination of beta-lactam antibiotic residues or contaminants in the pharmaceutical manufacturing environment was investigated. Decontamination with solutions of hydrochloric acid, sodium hydroxide, hydrogen peroxide and hydroxylamine as agents for degradation was assessed. According to...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukutsu N,Kawasaki T,Saito K,Nakazawa H

更新日期：2006-09-01 00:00:00

abstract：:In the course of our search for bioactive metabolites from marine organisms, new hexylitaconic acid derivatives (1-4), along with (3S)-hexylitaconic acid (5), were isolated from a sponge-derived fungus Penicillium sp. Based on the NMR and MS data, the structures of compounds 1-4 were defined as α,β-dicarboxylic acid d...

journal_title：Chemical & pharmaceutical bulletin

authors： Li JL,Zhang P,Lee YM,Hong J,Yoo ES,Bae KS,Jung JH

更新日期：2011-01-01 00:00:00

abstract：:The hypoglycemic component, elatoside E, was isolated from the root cortex of Aralia elata SEEM. (Araliaceae) together with elatoside F and eight known oleanolic acid glycosides, elatosides A and C, oleanolic acid 3-O-[alpha-L-arabinofuranosyl (1-->4)]-beta-D-glucopyranosiduronic acid, oleanolic acid 3-O-beta-D-glucop...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Murakami T,Harada E,Murakami N,Yamahara J,Matsuda H

更新日期：1996-10-01 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：:Remote loading of insulin and bovine serum albumin (BSA) into neutral or positively-charged liposomes by incubation under a transmembrane pH gradient or non-pH gradient was investigated. Trapping efficiencies in several incubation conditions were compared with those of the conventional reverse-phase evaporation vesicl...

journal_title：Chemical & pharmaceutical bulletin

authors： Hwang SH,Maitani Y,Takayama K,Nagai T

更新日期：2000-03-01 00:00:00

abstract：:Eight dermorphin (DM) analogs extended at the C-terminus, based on the sequence of prepro-DM deduced from the cDNA, were synthesized by a simultaneous solid-phase method in which a pair of peptides was synthesized in a single vessel. Six peptides (three pairs) were obtained in satisfactory yields (17-37%). In the opio...

journal_title：Chemical & pharmaceutical bulletin

authors： Ambo A,Sasaki Y,Suzuki K

更新日期：1994-04-01 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：:A moisturizing cream mixed with a steroid ointment is frequently prescribed to patients suffering from atopic dermatitis. However, there is a concern that the mixing operation causes destabilization. The present study was performed to investigate the stability of such preparations closely using magnetic resonance imag...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Funatani C,Yamamoto Y,Fukami T,Koide T,Hayashi Y,Takayama K

更新日期：2017-01-01 00:00:00

abstract：:Two new acylated flavonol glycosides, named amurenosides A and B, together with quercetin 3-(2,6-di-O-alpha-rhamnopyranosyl-beta-galactopyranoside), have been isolated from the whole plant of Vicia amurensis. Their structures were elucidated as quercetin 3-O-alpha-L-(3-feruloylrhamnopyranosyl)(1-->6)-[alpha-L-rhamnopy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kang SS,Chang YS,Kim JS

更新日期：2000-08-01 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：:To learn whether glycation plays a role in insolubilization or in senile cataractogenesis, the reactivity of lens protein from normal and senile cataractous lenses and individual crystallin prepared from human lens with various sugars [glucose, glucose-1-phosphate (G-1-P), glucose-6-phosphate (G-6-P) and fructose], an...

journal_title：Chemical & pharmaceutical bulletin

authors： Kamei A

更新日期：1992-10-01 00:00:00

abstract：:The sequence Fourier analysis reported previously seems to be applicable to elucidating a simple and concerted interaction in Arabidopsis thaliana, similar to that in Homo sapiens. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Numao N,Miyama M,Hanagata N

更新日期：2004-08-01 00:00:00

abstract：:Thioglycosides are available donors in glycosylation due to the stability of the anomeric C-S bond under general reaction conditions of protection and deprotection, and offer orthogonality in their activation. We report now that the hypervalent iodine effectively induced glycosylation reaction of thioglycosides with v...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajimoto T,Morimoto K,Ogawa R,Dohi T,Kita Y

更新日期：2016-01-01 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：:Dissolution kinetics of a bilayer direct compress tablet was evaluated by using degassing cyclic flow UV-visible (Vis) spectroscopy with chemometrics. The model bilayer nicotinamide (NA)-pyridoxine hydrochloride (PH) 100.0 mg tablets were prepared via the dual compress method. The fast diffusion layer of the bilayer t...

journal_title：Chemical & pharmaceutical bulletin

authors： Otsuka Y,Ito A,Takahashi T,Matsumura S,Takeuchi M,Tanaka H

更新日期：2019-01-01 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：:Conjugates of 2-aminooxyethyliminodiacetic acid with estrone, testosterone, epiandrosterone, 17-alpha-hydroxy-progesterone and progesterone were synthesized and their complexes with Tc-99m were successfully prepared in good yields, which indicated the agent to be promising for metal-labeling of biomolecules and relate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoda R,Karube Y,Takata J,Nagata Y,Matsushima Y

更新日期：1999-03-01 00:00:00

abstract：:Two enkephalin-containing peptides, peptide E and dynorphin(1-24), were synthesized by conventional solution methods employing a new Trp derivative, Nin-(2,4,6-triisopropylphenylsulfonyl)tryptophan [Trp(Tps)]. All protecting groups employed including the Tps group were removed by treatment with 1 M trifluoromethanesul...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitagawa K,Kawamoto T,Futaki S,Kiyama S,Akita T,Moritoki H,Kiso Y

更新日期：1989-10-01 00:00:00

abstract：:Tumor necrosis factor (TNF), a cytokine produced in macrophages, also acts as an endogenous pyrogen (EP). To investigate whether TNF has a role in the fever induced by Nocardia rubra cell wall skeleton (N-CWS), the relationship between fever and TNF production was studied in guinea pigs. N-CWS injected i.v. to guinea ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohara K,Hirano Y,Ishida H,Mori J,Tensho A

更新日期：1989-10-01 00:00:00

abstract：:In this study we report the synthesis and pharmacological evaluation of four new progesterone derivatives; 17alpha-hydroxy-16beta-methylpregna-4,6-diene-3,20-dione 12, 17alpha-cyclopropylcarbonyloxy-16beta-methylpregna-4,6-diene-3,20-dione 13, 17alpha-cyclobutylcarbonyloxy-16beta-methylpregna-4,6-diene-3,20-dione 14, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ramírez E,Cabeza M,Bratoeff E,Heuze I,Pérez V,Valdez D,Ochoa M,Teran N,Jimenez G,Ramírez T

更新日期：2005-12-01 00:00:00

abstract：:A method for scale-up of a lubricant mixing process in a V-type blender was proposed. Magnesium stearate was used for the lubricant, and the lubricant mixing experiment was conducted using three scales of V-type blenders (1.45, 21 and 130 L) under the same fill level and Froude (Fr) number. However, the properties of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Horibe M,Sonoda R,Watano S

更新日期：2018-01-01 00:00:00

abstract：:A new fluorinated analog of vitamin D2, 24-epi-26,26,26,27,27,27-hexafluoro- 1 alpha,25-dihydroxyvitamin D2, was efficiently synthesized starting from (R)-4-isopropyl-3-propionyl-2- oxazolidinone with high stereochemical control. In all four physiological test systems, the fluorinate vitamin D2 analog was found to be ...

journal_title：Chemical & pharmaceutical bulletin

authors： Iseki K,Oishi S,Namba H,Taguchi T,Kobayashi Y

更新日期：1995-11-01 00:00:00

abstract：:Green tea and (-)-epigallocatechin gallate (EGCG: one of main components of green tea) are well known to have preventive activities against human cancers. Previously, using a galloyl group as a core structure derived from EGCG, we developed alkyl gallate and gallamide derivatives, which showed strong antiproliferative...

journal_title：Chemical & pharmaceutical bulletin

authors： Dodo K,Minato T,Hashimoto Y

更新日期：2009-02-01 00:00:00

abstract：:(+)-4(5)-[(2R,5R)-5-aminomethyltetrahydrofuran-2-yl]imidazole [(+)-1, imifuramine] and its 2R,5S-stereoisomer (+)-2 were expected as base compounds to develop selective human histamine H4-receptor ligands. The improved synthesis of (+)-1 was done via cyclization of a diazafulvene intermediate generated by Bu3P/N,N,N',...

journal_title：Chemical & pharmaceutical bulletin

authors： Harusawa S,Araki L,Terashima H,Kawamura M,Takashima S,Sakamoto Y,Hashimoto T,Yamamoto Y,Yamatodani A,Kurihara T

更新日期：2003-07-01 00:00:00

abstract：:Fourteen new bisnor- and norditerpene dilactones, makilactones E-R, having a 7alpha : 8alpha-epoxy-9,11-enolide substructure, were isolated from a methanolic extract of the root and the bark of Podocarpus macrophyllus D. DON (Podocarpaceae) with thirteen known bisnor- and norditerpenoids, and the structures of those n...

journal_title：Chemical & pharmaceutical bulletin

authors： Sato K,Inaba Y,Park HS,Akiyama T,Koyama T,Fukaya H,Aoyagi Y,Takeya K

更新日期：2009-07-01 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