Statistical Analysis of the Impact of Molecular Descriptors on Cytotoxicity of Thiourea Derivatives Incorporating 2-Aminothiazole Scaffold.

abstract：:Two series of new pyridines bearing thiazoline (3a--n) and thiazolidinone (5a--e) moieties were prepared via the cyclization of the corresponding substituted pyridyl thiourea (2a--g) with an appropriately substituted phenacyl bromide or chloroacetic acid, respectively. The antimicrobial activity was determined for rep...

journal_title：Chemical & pharmaceutical bulletin

authors： Hassan HY,el-Koussi NA,Farghaly ZS

更新日期：1998-05-01 00:00:00

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：:Four new ursane-type triterpenes, 3beta-acetoxy-11alpha-methoxy-12-ursene (1), 3beta-acetoxy-11alpha-ethoxy-12-ursene (2), 3beta-acetoxy-11alpha-hydroperoxy-12-ursene (3), 3beta-hydroxy-11alpha-hydroperoxy-12-ursene (4), and two new oleanane-type triterpenes, 3beta-acetoxy-11alpha-ethoxy-12-oleanene (5), 3beta-acetoxy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chiang YM

更新日期：2000-05-01 00:00:00

abstract：:A novel in-die evaluation method of tablet capping tendency was proposed based on a force-displacement curve and stress relaxation parameter in a tableting process. In our previous study (Chem. Pharm. Bull., 59, 2011, Nakamura et al.), the phase diagram consisting of elastic recovery energy (E(e)) and plastic deformat...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura H,Sugino Y,Watano S

更新日期：2012-01-01 00:00:00

abstract：:Stereoisomers of thiol proteinase inhibitor (TPI) were synthesized by a conventional solution method. Among them, iNoc-D-Gln-Val-Val-Ala-Ala-pNA weakly inhibited the amidolytic activity of papain, although iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited papain activity fairly potently. However, the other five D-amino acid-cont...

journal_title：Chemical & pharmaceutical bulletin

authors： Iguchi S,Hirano K,Okamoto H,Okamoto Y,Okada Y

更新日期：1996-08-01 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：:The admixture of a steroid ointment and a moisturizing cream is frequently prescribed to patients suffering from atopic dermatitis. For the mixing operation, a revolution/rotation-type hybrid mixer is widely used in pharmacy. The purpose of this study was to monitor the mixed state of the admixtures during the mixing ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokokawa M,Setoyama H,Okada K,Hayashi Y,Machida Y,Onuki Y,Obata Y

更新日期：2018-01-01 00:00:00

abstract：:Diabetic embryopathy is a diabetic complication, in which maternal hyperglycemia in early pregnancy causes birth defects in newborn infants. Under maternal diabetic conditions, hyperglycemia disturbs intracellular molecular activities and organelles functions. These include protein misfolding in the endoplasmic reticu...

journal_title：Chemical & pharmaceutical bulletin

authors： Han L,Jiang Z,Zheng X,Qiu J,Hu Y,Li X

更新日期：2019-01-01 00:00:00

abstract：:From the herb of Luffa acutangula ROXB. (Cucurbitaceae), seven oleanane-type triterpene saponins, acutosides A--G, were isolated and their structures were determined. Acutoside A is oleanolic acid 3-O-beta-D-glucopyranosyl-(1----2)-beta-D-glucopyranoside. Acutosides B, D, E, F and G have a common prosapogenin structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagao T,Tanaka R,Iwase Y,Hanazono H,Okabe H

更新日期：1991-03-01 00:00:00

abstract：:Poorly water-soluble drugs N-5159, griseofulvin (GFV), glibenclamide (GBM) and nifedipine (NFP) were ground in a dry process with polyvinylpyrrolidone (PVP) and sodium dodecyl sulfate (SDS). Different crystallinity behavior of each drug during grinding was shown in the ternary Drug/PVP/SDS system. However, when each t...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh K,Pongpeerapat A,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2003-02-01 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：:Oxidative stress plays a crucial role in neurological diseases, resulting in excessive production of reactive oxygen species, mitochondrial dysfunction and cell death. In this work, we designed and synthesized a series of tetramethylpyrazine (TMP) derivatives and investigated their abilities for scavenging free radica...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen H,Tan G,Cao J,Zhang G,Yi P,Yu P,Sun Y,Zhang Z,Wang Y

更新日期：2017-01-01 00:00:00

abstract：:In the present study, a novel series of 2-(2-(3-aryl-5-substituted-1,3,4-thiadiazol-2(3H)-ylidene)hydrazinyl)-4,4-diphenyl-1H-imidazol-5(4H)-one derivatives were designed and prepared via the reaction of the most versatile, hitherto unreported 2-(5-oxo-4,4-diphenyl-4,5-dihydro-1H-imidazol-2-yl)-N-phenylhydrazinecarbot...

journal_title：Chemical & pharmaceutical bulletin

authors： Gomha SM,Abdel-Aziz HM,Khalil KD

更新日期：2016-01-01 00:00:00

abstract：:Chitosan-alginate polyelectrolyte complex (PEC) have been prepared in situ in beads and microspheres. This study examines the preparation of suitable chitosan-alginate coacervates for casting into homogeneous PEC films for potential applications in packaging, controlled release systems and wound dressings. Coacervatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yan X,Khor E,Lim LY

更新日期：2000-07-01 00:00:00

abstract：:We studied the possibility of using ursodeoxycholic acid (UDCA) as an excipient to create an amorphous composite that can be administered to animals in preclinical studies of experimental drugs. Three UDCA-based amorphous samples composed of nifedipine (NIF), indomethacin (IND), and naproxen (NAP) were found by screen...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanida S,Yoshimoto A,Yoshida M,Uchiyama H,Kadota K,Tozuka Y

更新日期：2019-01-01 00:00:00

abstract：:Investigation of an acetone extract of the leaves and twigs of Taxus sumatrana has resulted in the isolation of two new bicyclic taxoids, tasumatrols M (1), and N (2) and a new baccatin III derivative, tasumatrol O (3) together with the previous known 7-deacetylcanadensene (4) and 2alpha,7beta,13alpha-triacetoxy-5alph...

journal_title：Chemical & pharmaceutical bulletin

authors： Shen YC,Hsu SM,Lin YS,Cheng KC,Chien CT,Chou CH,Cheng YB

更新日期：2005-07-01 00:00:00

abstract：:The metabolism of 2,4-dinitrotoluene (2,4-DNT), 2,4-dinitrobenzyl alcohol (2,4-DNB), 2,4-dinitrobenzaldehyde (2,4-DNBAl), 2,6-DNT, 2,6-DNB and 2,6-DNBAl in the microsomal and cytosol fractions prepared from unfortified male Wistar and male Sprague-Dawley (S.D.) rat livers was investigated. Data obtained by high-perfor...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori M,Kawajiri T,Sayama M,Miyahara T,Kozuka H

更新日期：1989-07-01 00:00:00

abstract：:A high-performance liquid chromatographic method involving postcolumn fluorescence derivatization is described for the quantification of five fragment peptides (methionine-enkephalin-Thr-Ser-Glu-Lys, methionine-enkephalin-Lys, methionine-enkephalin-Arg, leucine-enkephalin-Lys and leucine-enkephalin-Arg) released by tr...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang GQ,Kai M,Ohkura Y

更新日期：1991-09-01 00:00:00

abstract：:Detailed chemical studies on the cytotoxic fraction from the leaves of Dysoxylum cumingianum have resulted in the isolation of two new triterpene glucosides, cumingianosides P (18) and Q (19), with an apotirucallane-type skeleton. The structures of 18 and 19 were determined by spectral examinations, and by conversion ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujioka T,Sakurai A,Mihashi K,Kashiwada Y,Chen IS,Lee KH

更新日期：1997-01-01 00:00:00

abstract：:Polymorphic behaviours of paracetamol and propyphenazone and interaction between these two compounds were investigated using differential scanning calorimetry (DSC), X-ray powder diffraction and Fourier transform-infrared (FT-IR)-spectroscopy. Binary mixtures containing various ratios of the compounds were prepared as...

journal_title：Chemical & pharmaceutical bulletin

authors： Zalac S,Khan MZ,Gabelica V,Tudja M,Mestrović E,Romih M

更新日期：1999-03-01 00:00:00

abstract：:To investigate the possible mechanism of the stimulatory effect of a hot water extract from Artemisia leaf (Artemisia princeps PANPANINI) (AFE) on the proliferation of endothelial cells, cells from bovine aorta were cultured for 72 h in RPMI1640 medium supplemented with 10% fetal calf serum in the presence of 5 microg...

journal_title：Chemical & pharmaceutical bulletin

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

更新日期：1990-09-01 00:00:00

abstract：:Two new cangorosin A type triterpene dimers, which composed of two triterpene units jointed by two ether linkages between the A and B rings, were isolated from the Brazilian medicinal plant "xuxuá" (Maytenus chuchuhuasca). Structures of new isolates, xuxuasins A (1) and B (2), were established based on several spectro...

journal_title：Chemical & pharmaceutical bulletin

authors： Shirota O,Sekita S,Satake M,Morita H,Takeya K,Itokawa H

更新日期：2004-09-01 00:00:00

abstract：:Lipid peroxidation of erythrocyte membrane was caused by phorbol myristate acetate (PMA)-stimulated polymorphonuclear leukocytes (PMN) in the presence of ferritin. PMN themselves were not peroxidized. A lag period was observed before the start of the peroxidation reaction. In contrast, ferritin iron was continuously r...

journal_title：Chemical & pharmaceutical bulletin

authors： Miura T,Ogiso T

更新日期：1991-06-01 00:00:00

abstract：:N-Terminal tripeptide analogs of fibrin alpha-chain were synthesized and their inhibitory effect on fibrinogen/thrombin clotting was examined. A new water-soluble active ester, 3-pyridinium ester, was used for the synthesis. Among the synthetic peptides, H-Gly-Pro-Arg-hexamethyleneimine exhibited the highest inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawasaki K,Tsuji T,Hirase K,Miyano M,Imoto Y,Iwamoto M

更新日期：1991-03-01 00:00:00

abstract：:Chemical investigations on the marine soft coral Lobophytum sp., collected from the Andaman and Nicobar Islands, yielded two new acyl glycerol monoalkyl ethers along with two known compounds of this series (1a-d), and a new ceramide (4a). The structures of the new and known compounds were elucidated on the basis of ex...

journal_title：Chemical & pharmaceutical bulletin

authors： Radhika P,Rao VL,Laatsch H

更新日期：2004-11-01 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：:The structures of the adducts derived from the reactions of substituted ketenes with dihydropyridine derivatives have been clarified by single crystal X-ray analyses and the formation mechanism is discussed on the basis of the reaction-path calculations by semiempirical and density functional theory (DFT) molecular or...

journal_title：Chemical & pharmaceutical bulletin

authors： Oiso S,Eto M,Yoshitake Y,Harano K

更新日期：2003-09-01 00:00:00

abstract：:The novel hydroxamates containing purine scaffold were designed, synthesized and screened for their biological activities as histone deacetylase (HDAC) inhibitors. Some of them exhibited excellent acti-HDACs activities and antiproliferative activities, the most promising compound was 7m'. Western blot analysis indicat...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu Z,Yang Y,Mai X,Liu B,Xiong Y,Feng L,Liao Y,Zhang Y,Wang H,Ouyang L,Liu S

更新日期：2018-01-01 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：:A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PA...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki H,Ogiku T,Sai H,Moritani Y,Ohtani A,Ohmizu H

更新日期：2009-09-01 00:00:00