Synthesis and pharmacological activities of novel bicyclic thiazoline derivatives as hepatoprotective agents. I. 8-Ethoxycarbonyl-5,6-dihydrothiazolo[2,3-c][1,4]thiazine derivatives.

abstract：:Bromination of 17-O-acetyltestosterone (17beta-acetoxyandrost-4-en-3-one) (1) was performed with 1, 5, and 10 eq of Br2 in AcOH-Et2O at room temperature. In all cases 2alpha,6beta- (2) and 2alpha,6beta-dibromo-17beta-acetoxyandrost-4-en-3-one (3) were obtained, although the yields were dependent upon the conditions us...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimizu T,Tobari A,Koyanagi J,Kawase M,Saito S

更新日期：2001-01-01 00:00:00

abstract：:Tin(IV) complexes 2a--q derived from pyridine Schiff bases were prepared and characterized. Four complexes of this series were evaluated in vitro against different carcinogenic cell lines; besides their anti-inflammatory and antioxidant properties were also tested. Combination of mass spectrometry, multinuclear NMR an...

journal_title：Chemical & pharmaceutical bulletin

authors： González A,Gómez E,Cortés-Lozada A,Hernández S,Ramírez-Apan T,Nieto-Camacho A

更新日期：2009-01-01 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：:To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng XW,Huang N,Xu H,Yang WB,Yang LM,Qu H,Zheng YT

更新日期：2010-07-01 00:00:00

abstract：:To investigate the effect of the hot water extract from Artemisia leaf (Artemisia princeps Panpanini) (AFE) on the proliferation of endothelial cells, the cells from bovine aorta were cultured for up to 96 h in the presence of 1, 5, 10 or 50 micrograms/ml AFE in RPMI1640 medium supplemented with 10% fetal bovine serum...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaji T,Kaga K,Miezi N,Ejiri N,Sakuragawa N

更新日期：1990-02-01 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：:Water-soluble porphyrins containing four platinum(II) complexes per molecule, [5alpha,10beta,15alpha,20beta-tetrakis(2-trans-(alpha,beta,alpha,beta-trans-Pt) and cis-(alpha,beta,alpha,beta-cis-Pt) [PtCl(NH(3))(2)]N-2-aminophenylporphyrin)], were synthesized and characterized. The binding of synthetic nucleotide polyme...

journal_title：Chemical & pharmaceutical bulletin

authors： Munakata H,Imai H,Nakagawa S,Osada A,Uemori Y

更新日期：2003-05-01 00:00:00

abstract：:Transfer of aprindine from the blood into the intestinal lumen or into the peritoneal cavity was examined after intravenous administration of the drug at a dose of 5 mg/kg in rats. The amount of the drug transferred from the blood into the intestinal lumen was much greater than into the peritoneal cavity. The average ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arimori K,Hashimoto Y,Nakano M

更新日期：1991-12-01 00:00:00

abstract：:We investigated the kinetics of in vitro transformation of a dichlorinated propyl paraben (2-propyl 3,5-dichloro-4-hydroxybenzoate; Cl2PP) by the rat liver S9 fraction and assessed the aryl hydrocarbon receptor (AhR) agonist activity of the metabolite products identified in HPLC and GC/MS analysis and by metabolite sy...

journal_title：Chemical & pharmaceutical bulletin

authors： Terasaki M,Wada T,Nagashima S,Makino M,Yasukawa H

更新日期：2016-01-01 00:00:00

abstract：:A novel γ-cyclodextrin (γ-CD) based carrier for molecular encapsulation of cancer chemotherapeutic agent doxorubicin (DOX) was synthesized and fully characterized by various analytical approaches. The γ-CD derivative, with a β-naphthyl alanine residue attached in its primary face, exhibits potent binding capacity with...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu D,Wang L,Gourevich D,Kabha E,Arditti F,Athamna M,Cochran S,Melzer A,Gnaim JM

更新日期：2014-01-01 00:00:00

abstract：:Three new 15,16-seco-cycloartane glycosides, which were constructed by a C-C bond cleavage in the D ring, have been isolated from Cimicifuga Rhizome for the first time. Their structures were determined by the use of 2D NMR techniques and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshimitsu H,Nishida M,Nohara T

更新日期：2007-05-01 00:00:00

abstract：:Two novel norhumulene-type sesquiterpenes, named mikaniahumulene I (1) and II (2) were isolated along with nine known compounds, seven kaurenic acid-type diterpenes (3-9), a coumarin (10) and a flavone (11), from the aerial parts of Mikania hirsutissima DC (Compositae). The structures of new norhumulenes were determin...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohkoshi E,Makino M,Fujimoto Y

更新日期：1999-10-01 00:00:00

abstract：:The stereoselective introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one was accomplished using Birch reduction and an enolate trapping reaction. It was determined that the allyl group was introduced via an unexpected conformation-flipped from the initi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hiroya K,Takahashi T,Shimomae K,Sakamoto T

更新日期：2005-02-01 00:00:00

abstract：:Values of inhibition constants, Ki, and concentrations required for 50% inhibition, IC50, for a collection of structurally diverse competitive inhibitors of calf spleen purine nucleoside phosphorylase have been determined employing inosine as substrate. These values have been employed to create predictive quantitative...

journal_title：Chemical & pharmaceutical bulletin

authors： Andricopulo AD,Yunes RA

更新日期：2001-01-01 00:00:00

abstract：:Different green synthesis of alkyl esters of acyclovir (acyclovir prodrugs) is described. Hexanoic, decanoic, dodecanoic and tetradecanoic acyclovir esters were synthesized reacting acyclovir and the respective acid anhydride in dimethyl sulfoxide (DMSO), in solvents from renewable sources and without solvent (T=30 °C...

journal_title：Chemical & pharmaceutical bulletin

authors： de Regil-Hernández R,Martínez-Lagos F,Rodríguez-Bayón A,Sinisterra JV

更新日期：2011-01-01 00:00:00

abstract：:A highly polar saponin mixture from pods of Acacia concinna (Leguminosae) was hydrolyzed with alkali to yield five new triterpenoidal prosapogenols named concinnosides A (6), B (3), C (7), D (4), and E (8), together with four known glycosides, acaciaside, (2), julibroside A1 (10) julibroside A3 (9), albiziasaponin C (...

journal_title：Chemical & pharmaceutical bulletin

authors： Abul Gafur M,Obata T,Kiuchi F,Tsuda Y

更新日期：1997-04-01 00:00:00

abstract：:Fifteen triterpenoid saponins were isolated from the berries of Hedera colchica and their structures established on the basis of chemical and spectroscopic evidence. Among them, two are new compounds: coichiside A (3) and colchiside B (15) and four are described for the first time in the berries of Hedera colchica (co...

journal_title：Chemical & pharmaceutical bulletin

authors： Mshvildadze V,Elias R,Faure R,Debrauwer L,Dekanosidze G,Kemertelidze E,Balansard G

更新日期：2001-06-01 00:00:00

abstract：:seco-Macrosphelide E has been isolated from a strain of Periconia byssoides originally separated from the sea hare Aplysia kurodai. Its absolute stereostructure, with the same configuration as that of macrosphelide E, have been elucidated on the basis of spectroscopic analyses and unambiguous synthesis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura H,Ono M,Yamada T,Numata A,Akita H

更新日期：2002-02-01 00:00:00

abstract：:Phytochemical investigation of the leaves of Umbilicus pendulinus afforded in addition to 2-O-caffeoyl malate, isoquercitrin and Z-venusol, the new isomer E-venusol. Special NMR experiments were carried out to elucidate the configuration of the two latter compounds. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Viornery L,Saliba C,Daskiewicz JB,Bayet C,Comte G,Fenet B,Gutierrez G,Barron D

更新日期：2000-11-01 00:00:00

abstract：:We developed a rapid and efficient analytical technique for cyclosporine A using HPLC on a column packed with 2-µm nonporous octadecylsilyl silica particles. Under optimized conditions, cyclosporine A was separated with high resolution from other cyclic peptides within 3 min, because the mass transfer resistance in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Kato K,Nanjo K,Goda Y

更新日期：2018-01-01 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：: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：:The complete amino acid sequence of a new abortifacient protein, karasurin, was determined. Karasurin, which was isolated from fresh root tubers of Trichosanthes kirilowii Maximowicz var, japonicum Kitamura (Cucurbitaceae), was a highly basic protein with pI 10.1 and molecular weight of 28,000. Intact karasurin was cl...

journal_title：Chemical & pharmaceutical bulletin

authors： Toyokawa S,Takeda T,Kato Y,Wakabayashi K,Ogihara Y

更新日期：1991-05-01 00:00:00

abstract：:The anti-anginal drug Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, is thought to modulate the metabolism during myocardial ischemia by activating pyruvate dehydrogenase activity to promote glucose oxidation. Ranolazine and its five principal metabolites: CVT-2512, CVT-2513, CVT-2514, CVT-2738 and CVT-4...

journal_title：Chemical & pharmaceutical bulletin

authors： Yao Z,Gong S,Guan T,Li Y,Wu X,Sun H

更新日期：2009-11-01 00:00:00

abstract：:Six new triterpenoid glycosides called julibrosides A1-A4, B1 and C1 were isolated from Albizziae Cortex, the dried stem bark of Albizzia julibrissin Durazz. Their structures were determined based on spectral and chemical evidence. Julibrosides B1 and C1 had new sapogenols, designated julibrogenin B and C, respectivel...

journal_title：Chemical & pharmaceutical bulletin

authors： Kinjo J,Araki K,Fukui K,Higuchi H,Ikeda T,Nohara T,Ida Y,Takemoto N,Miyakoshi M,Shoji J

更新日期：1992-12-01 00:00:00

abstract：:In our series of studies on potassium channel openers, several thienylcyanoguanidine derivatives were synthesized and evaluated for smooth muscle relaxation activity in vitro. Among the newly synthesized compounds, N-cyano-N'-(5-cyano-3-thienyl)-N"-tert-pentylguanidine (4b) and N-(5-bromo-3-thienyl)-N'-cyano-N"-tert-p...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshiizumi K,Ikeda S,Nishimura N,Yoshino K

更新日期：1997-12-01 00:00:00

abstract：:The aim of this study was to evaluate the effects of Magnolin (MGL) on inhibition of human breast cancer cells, and explore the underlying molecular mechanisms. The viability of the treated cells was assessed with the Cell Counting Kit-8 (CCK-8) assay, and the proliferation was analyzed in terms of EdU uptake, colony ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang J,Zhang S,Huang K,Shi L,Zhang Q

更新日期：2020-01-01 00:00:00

abstract：:Several E-ring-modified analogues of (RS)-camptothecin were synthesized by total synthesis via Friedländer condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camp...

journal_title：Chemical & pharmaceutical bulletin

authors： Ejima A,Terasawa H,Sugimori M,Ohsuki S,Matsumoto K,Kawato Y,Yasuoka M,Tagawa H

更新日期：1992-03-01 00:00:00

abstract：:The MeOH extract of the stem barks of Drypetes tessmanniana (Euphorbiaceae) afforded two new triterpene derivatives characterized as 3beta-O-(E)-3,5-dihydroxycinnamoyl-11-oxo-olean-12-ene and 3beta,6alpha-dihydroxylup-20(29)-ene together with seven known compounds. Their structures were established on the basis of spe...

journal_title：Chemical & pharmaceutical bulletin

authors： Dongfack MD,Van-Dufat HT,Lallemand MC,Wansi JD,Seguin E,Tillequin F,Wandji J

更新日期：2008-09-01 00:00:00

abstract：:Two new phenolic amides, pharnilatins A (1) and B (2), were isolated from the seeds of Pharbitis nil. These new compounds possess a p-coumaroyl unit with a structurally unique side chain, (2S,3S)-2,3-dihydroxyputrescine. The chemical structures and absolute stereochemistries of the new compounds were determined on the...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim KH,Choi SU,Son MW,Lee KR

更新日期：2010-11-01 00:00:00