Synthetic studies of vitamin D analogs. XXIV. Synthesis of active vitamin D3 analogs substituted at the 2 beta-position and their preventive effects on bone mineral loss in ovariectomized rats.

abstract：:When the beta-acyloxy esters (+/-)-10 and (+/-)-11 were exposed to the lipase OF-360 from Candida rugosa or immobilized lipase OF-360 in a water-saturated organic solvent, the hydrolyzed product (8aS)-6 was obtained in high chemical (40%) and optical (> 99% ee) yields. The absolute structure of (8aS)-6 was confirmed b...

journal_title：Chemical & pharmaceutical bulletin

authors： Akita H,Nozawa M,Futagami Y,Miyamoto M,Saotome C

更新日期：1997-05-01 00:00:00

abstract：:A new oleanan-type triterpene and three new cincholic acid glycosides were isolated from Peruvian "Una de Gato" (Cat's claw, plant of origin: Uncaria tomentosa), a traditional herbal medicine in Peru. Their structures were determined by spectroscopic analysis. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitajima M,Hashimoto K,Sandoval M,Aimi N,Takayama H

更新日期：2004-10-01 00:00:00

abstract：:This paper describes practical and selective hydrogenation methodologies using heterogeneous palladium catalysts. Chemoselectivity develops dependent on the catalyst activity based on the characteristic of the supports, derived from structural components, functional groups, and/or morphologies. We especially focus on ...

journal_title：Chemical & pharmaceutical bulletin

authors： Monguchi Y,Ichikawa T,Sajiki H

更新日期：2017-01-01 00:00:00

abstract：:The metabolites of clentiazem in the urine or bile of rats and dogs were investigated. Fifteen basic, 6 acidic, 2 neutral and 4 conjugated metabolites were isolated. In the present paper, fourteen reference compounds as shown in Charts 1, 2 and 3 were synthesized to identify the structures of the metabolites in proced...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue H,Nakamura S,Otsuka H,Gaino M,Harada T,Matsuki K,Takeda M

更新日期：1994-01-01 00:00:00

abstract：:C1q/tumor necrosis factor (TNF)-related protein 12 (CTRP12) is a secretory protein that participates in the regulation of glucose and lipid metabolism in obesity and diabetes. Its role in cardiovascular disease, particularly sepsis-induced cardiac injury, is unclear. Here, we stimulated cardiomyocytes with lipopolysac...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou MQ,Jin E,Wu J,Ren F,Yang YZ,Duan DD

更新日期：2020-01-01 00:00:00

abstract：:Microcrystalline cellulose (MCC) granules were prepared by wet granulation using a high-shear mixer. Physical characteristics of the granules were investigated using near IR spectrometry, thermogravimetry and isothermal water vapor adsorption. Near IR spectra of dried MCC granules prepared for various granulation time...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Kikuchi H,Yonemochi E,Terada K,Yamamoto K

更新日期：2001-04-01 00:00:00

abstract：:A series of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6,7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishikawa H,Tabusa F,Miyamoto H,Kano M,Ueda H,Tamaoka H,Nakagawa K

更新日期：1989-08-01 00:00:00

abstract：:A series of 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives was synthesized and evaluated for its ability to reverse a scopolamine-induced learned impairment in a one-trial passive avoidance task (antiamnestic activity). 2-(4-Allyl-1-piperazinyl)-4-pentyloxyquinazoline (4) showed more potent antiamnestic activity th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori M,Iemura R,Hara H,Sukamoto T,Ito K,Ohtaka H

更新日期：1991-02-01 00:00:00

abstract：:We designed and synthesized a new class of peptidomimetic human immunodeficiency virus protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl isostere as the active moiety. From a structure-activity relatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimoto T,Hattori N,Takaku H,Kisanuki S,Fukazawa T,Terashima K,Kato R,Nojima S,Misawa S,Ueno T,Imai J,Enomoto H,Tanaka S,Sakikawa H,Shintani M,Hayashi H,Kiso Y

更新日期：2000-09-01 00:00:00

abstract：:Two new flavonoid glycosides, 5-hydroxy-7,8-dimethoxy (2R)-flavanone-5-O-beta-D-glucopyranoside (1) and 5-hydroxy-7,8,2',5'-tetramethoxy-flavone-5-O-beta-D-glucopyranoside (2), and a new diterpenoid, andrographic acid (3), along with andrographidine A (4) were isolated from Andrographis paniculata, and their structure...

journal_title：Chemical & pharmaceutical bulletin

authors： Li W,Xu X,Zhang H,Ma C,Fong H,van Breemen R,Fitzloff J

更新日期：2007-03-01 00:00:00

abstract：:Silver loaded zeolite (Ag-Z) was previously found to have effective bactericidal activity against Escherichia coli. To understand the mechanisms of bactericidal activity of Ag-Z, role of light irradiation was focused and investigated in this study. In this study, we focused on light irradiation. Antibacterial assay an...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue Y,Kogure M,Matsumoto K,Hamashima H,Tsukada M,Endo K,Tanaka T

更新日期：2008-05-01 00:00:00

abstract：:Invasive fungal disease constitutes a growing health problem and development of novel antifungal drugs with high potency and selectivity against new fungal molecular targets are urgently needed. In order to develop potent antifungal agents, a novel series of 6-alkyl-indolo[3,2-c]-2H-thiochroman derivatives were synthe...

journal_title：Chemical & pharmaceutical bulletin

authors： Han XY,Zhong YF,Li SB,Liang GC,Zhou G,Wang XK,Chen BH,Song YL

更新日期：2016-09-01 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：:In addition to 19-dydroxybaccatin III, 1beta-hydroxy-5 alpha-deacetylbaccatin I, taxayuntin G and 13-O-deacetyltaxumairol Z (4), three new taxane diterpenoids, taxumairols X (1), Y (2), Z (3) have been isolated from extracts of the Formosan Taxus mairei (LEMEE & LEVL.) S. Y. HU. Compounds 1-2 belong to the 11(15-->1)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Shen YC,Chang YT,Wang SS,Lin YC,Chen CY

更新日期：2002-12-01 00:00:00

abstract：:A convenient and economical synthesis of 4-hydroxy-2,3-dimethoxybenzaldehyde has been developed. This was used as the starting material for the first total syntheses of (+/-)-isopiline, (+/-)-preocoteine, (+/-)-oureguattidine and (+/-)-3-methoxynordomesticine in which the key step involved formation of ring C of the a...

journal_title：Chemical & pharmaceutical bulletin

authors： Nimgirawath S,Udomputtimekakul P,Taechowisan T,Wanbanjob A,Shen Y

更新日期：2009-04-01 00:00:00

abstract：:Superoxide is involved in the pathogenesis of various diseases, such as inflammation, ischemia-reperfusion injury and carcinogenesis. Superoxide dismutases (SODs) catalyze the disproportionation reaction of superoxide to produce oxygen and hydrogen peroxide, and can protect living cells against the toxicity of free ra...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamura M,Urano Y,Kikuchi K,Higuchi T,Hirobe M,Nagano T

更新日期：2000-10-01 00:00:00

abstract：:Fe2+-dependent lipid peroxidation in phosphatidylcholine (PC) liposomes, assessed by thiobarbituric acid-reactive substances (TBARS) production, was stimulated in the presence of Fe3+ in a concentration-dependent manner. The rates of nitroblue tetrazolium (NBT) reduction and Fe2+ oxidation (Fe2+ disappearance and Fe3+...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohyashiki T,Kadoya A,Kushida K

更新日期：2002-02-01 00:00:00

abstract：:Racemic 1-acetoxy-2-phenylpropane (12) and 1-acetoxy-2-(2-naphthyl)propane (33) were hydrolyzed with lipase at 35-36 degrees C for 2 and 24 h to give predominantly (S)-2-phenyl-1-propanol (11) and (S)-2-(2-naphthyl)-1-propanol (32), respectively. However, racemic 1-acetoxy-2-(1-naphthyl)propane (25) was recovered inta...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto T,Takeda Y,Iwata E,Sakamoto M,Ishida T

更新日期：1994-06-01 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 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

abstract：:Three new monoterpenoids, called genipacetal, genipamide, and genipaol, were isolated from the fruit of Genipa americana L. (Rubiaceae), along with the four known iridoids genipin, gardendiol, deacetyl asperulosidic acid methyl ester, and shanzhiside. Their chemical structures were determined on the basis of spectrosc...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Ishimatsu N,Masuoka C,Yoshimitsu H,Tsuchihashi R,Okawa M,Kinjo J,Ikeda T,Nohara T

更新日期：2007-04-01 00:00:00

abstract：:Novel 1,2,3,4-tetrahydroisoquinoline derivatives bearing directly a cyclic amine at the 2-position were prepared and examined for their bradycardic activities in isolated right atria and in anesthetized rats. The structure-activity relationships (SAR) study revealed that the 2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinol...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakefuda A,Watanabe T,Taguchi Y,Masuda N,Tanaka A,Yanagisawa I

更新日期：2003-04-01 00:00:00

abstract：:A new series of 3-(5-3-methyl-5-[(3-methyl-7-5-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-1,3,4-thiadiazol-2-ylbenzo[b]furan-5-yl)methyl]benzo[b]furan-7-yl-1,3,4-thiadiazol-2-yl)-2-(aryl)-1,3-thiazolan-4-one 5a-j has been synthesized by the reaction of N2-[(E)-1-(4-methylphenyl)methylidene]-5-(3-methyl-5-[3-methyl-7-(5-[(E)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Reddy CS,Rao DC,Yakub V,Nagaraj A

更新日期：2010-06-01 00:00:00

abstract：:Two sesquiterpene lactones with the (9R)-eudesman-9,12-olide framework, wedelolides I and J, have been isolated together with five eudesmanolide sesquiterpenes and twelve ent-kaurene diterpenes from the aerial parts of Indonesian Wedelia prostrata. The absolute configurations of wedelolides I and J, proposed in the pr...

journal_title：Chemical & pharmaceutical bulletin

authors： Abdjul DB,Yamazaki H,Kanno SI,Kirikoshi R,Tomizawa A,Takahashi O,Maarisit W,Losung F,Rotinsulu H,Wewengkang DS,Sumilat DA,Kapojos MM,Namikoshi M

更新日期：2018-01-01 00:00:00

abstract：:Four vitamin D3 analogues (7a, 7b, 7c and 7d) bearing a hydroxyalkoxy group at the 2 beta-position were synthesized from the alpha-epoxide (5). The C-3 analogue (7b) showed the highest potency for elevating plasma calcium levels in rats. Furthermore, the 25-hydroxylated C-3 analogue (ED-71) (3), prepared from the 25-h...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyamoto K,Murayama E,Ochi K,Watanabe H,Kubodera N

更新日期：1993-06-01 00:00:00

abstract：:In the conventional method of mixer blending extraction, the yields of the tomato-saponin, esculeoside A, in the mini and middy tomatoes were found to be 0.043% and 0.046%, respectively. In order to improve the yields, we attempted a more efficient extraction using shock waves. The yields of esculeoside A were 0.0987%...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Takemoto A,Maehara H,Ohno M,Murakami Y,Itoh S,Nohara T

更新日期：2011-01-01 00:00:00

abstract：:Three new hydronaphthalenone derivatives (1-3) and one new dihydroramulosin derivative (4), were isolated from the endophytic fungus PSU-N24 together with eight known compounds. Their structures were elucidated by spectroscopic methods. Griseofulvin (9) displayed strong antifungal activity against Microsporum gypseum ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sommart U,Rukachaisirikul V,Sukpondma Y,Phongpaichit S,Sakayaroj J,Kirtikara K

更新日期：2008-12-01 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：:α,β-Unsaturated amides were incorporated as viable dipolarophiles in a catalytic asymmetric 1,3-dipolar cycloaddition of azomethine imines. The use of a 7-azaindoline auxiliary was essential to acquire sufficient reactivity with excellent diastereoselectivity, likely due to the chelating activation of the amide by the...

journal_title：Chemical & pharmaceutical bulletin

authors： Li Z,Kumagai N,Shibasaki M

更新日期：2020-01-01 00:00:00

abstract：:Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurashima H,Uchida S,Kashiwagura Y,Tanaka S,Namiki N

更新日期：2020-01-01 00:00:00